Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
10952349 78614 0 None 3467 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143434 78614 0 None 3467 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
11072401 64418 0 None 12882 2 Human 9.0 pEC50 = 9 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL139603 64418 0 None 12882 2 Human 9.0 pEC50 = 9 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
734373 39174 16 None 1000 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1021/acs.jmedchem.5c00678
CHEMBL1212983 39174 16 None 1000 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1021/acs.jmedchem.5c00678
9937709 77589 0 None 239 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL142538 77589 0 None 239 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
156246105 387622 4 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 402 4 0 4 3.0 COc1ccc(F)cc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5399732 387622 4 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 402 4 0 4 3.0 COc1ccc(F)cc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
187 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
187 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 524 25 None 1 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
162665337 356103 0 None None None Human 8.0 pEC50 = 8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4783881 356103 0 None None None Human 8.0 pEC50 = 8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162675795 366756 0 None None None Human 8.0 pEC50 = 8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
CHEMBL4798497 366756 0 None None None Human 8.0 pEC50 = 8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
137643460 314145 0 None None None Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 314145 0 None None None Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
172456153 388580 0 None 1 2 Human 7.0 pEC50 = 7 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 404 4 0 5 2.0 COc1ccc(F)cc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5419622 388580 0 None 1 2 Human 7.0 pEC50 = 7 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 404 4 0 5 2.0 COc1ccc(F)cc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
42598358 39992 0 None -100 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 39992 0 None -100 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137656230 314902 0 None None None Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 314902 0 None None None Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
162651352 354187 0 None None None Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
CHEMBL4751034 354187 0 None None None Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
89445242 348702 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4558571 348702 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
155518224 334826 0 None None None Human 5.0 pEC50 = 5 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4446144 334826 0 None None None Human 5.0 pEC50 = 5 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
155510640 348101 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 348101 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155510640 348101 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 348101 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137641943 314349 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 314349 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777104 314976 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4097819 314976 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
140830673 390661 0 None -28 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncn3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5556081 390661 0 None -28 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncn3)C1)C2 10.1021/acs.jmedchem.4c00293
53382504 177209 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 177209 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
155539719 346996 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 346996 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 349510 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 349510 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
53382504 177209 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 177209 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
89768734 329634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 329634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137645408 313794 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 313794 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
89768734 329634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 329634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
127043639 277793 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 277793 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
155539719 346996 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 346996 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 349510 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 349510 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
177646392 390829 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccn3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5558507 390829 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccn3)C1)C2 10.1021/acs.jmedchem.4c00293
137635723 312008 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 312008 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
725544 39176 13 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 261 2 2 4 2.4 Cc1cc(C)c2c(N)c(C(=O)NC3CC3)sc2n1 10.1021/acs.jmedchem.4c00293
CHEMBL1212988 39176 13 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 261 2 2 4 2.4 Cc1cc(C)c2c(N)c(C(=O)NC3CC3)sc2n1 10.1021/acs.jmedchem.4c00293
9893054 251119 13 None -46 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(-c3ccccc3)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616501 251119 13 None -46 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(-c3ccccc3)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
135126271 329136 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 329136 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
53382512 177189 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 177189 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382512 177189 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 177189 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382528 177206 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 177206 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145977993 328538 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 328538 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
145977993 328538 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 328538 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
135126271 329136 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 329136 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
145966725 329280 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 329280 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
53382528 177206 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 177206 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145966725 329280 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 329280 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137645408 313794 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 313794 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
132254780 428815 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.3 Cc1nc2oc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5891643 428815 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.3 Cc1nc2oc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145970522 329724 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 329724 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
145970522 329724 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 329724 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
78319052 335881 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human M4 receptor stably expressed in CHO-K1 cellsAgonist activity at human M4 receptor stably expressed in CHO-K1 cells
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acs.jmedchem.5c00678
CHEMBL4461438 335881 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human M4 receptor stably expressed in CHO-K1 cellsAgonist activity at human M4 receptor stably expressed in CHO-K1 cells
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acs.jmedchem.5c00678
78319052 335881 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4461438 335881 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
137643460 314145 0 None None None Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 314145 0 None None None Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777143 309930 1 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 309930 1 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777143 309930 1 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 309930 1 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777151 314443 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 314443 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207697 348336 0 None 10 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4549515 348336 0 None 10 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207701 348684 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4558111 348684 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
132254780 428815 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.3 Cc1nc2oc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5891643 428815 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.3 Cc1nc2oc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
9958728 78634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143468 78634 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
155552432 348229 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4547008 348229 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
89445225 335479 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4455343 335479 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
29262717 277764 7 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 277764 7 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127043639 277793 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 277793 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
122190994 251680 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618436 251680 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL5080134 478850 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 419 5 1 7 4.3 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(CN4CCOCC4)cc3)ncnc12 10.1016/j.bmcl.2021.128416
43989253 157717 1 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057394 157717 1 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
135126568 329387 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 329387 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122189499 251417 0 None -4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
CHEMBL3616504 251417 0 None -4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
135126568 329387 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 329387 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL5087350 479257 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 362 3 1 6 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc4c(c3)COC4)ncnc12 10.1016/j.bmcl.2021.128416
29262717 277764 7 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 277764 7 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145973325 329648 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 329648 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
59654579 251683 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618440 251683 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156017590 351771 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644084 351771 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
145973325 329648 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 329648 0 None None None Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
162658616 354914 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4759565 354914 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
127044706 277731 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 277731 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
132254511 392293 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 396 4 2 6 4.9 Cc1nc2oc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5594174 392293 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 396 4 2 6 4.9 Cc1nc2oc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
134207678 335762 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4459622 335762 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
134207707 336848 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4475459 336848 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
13626 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
140830653 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
CHEMBL5314557 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
DB18706 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
24967746 39945 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 39945 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
682264 83644 13 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 83644 13 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89452242 349438 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
CHEMBL4576513 349438 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
134207717 335834 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4460701 335834 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
134207690 348689 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4558206 348689 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207705 349884 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4587040 349884 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
162647361 353569 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4743571 353569 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
132254495 411387 4 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 2 1 5 3.6 Cc1nc2oc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5806953 411387 4 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 2 1 5 3.6 Cc1nc2oc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89452686 335220 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4451608 335220 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207730 347179 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4519541 347179 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
127044706 277731 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 277731 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
132254511 392293 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 396 4 2 6 4.9 Cc1nc2oc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5594174 392293 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 396 4 2 6 4.9 Cc1nc2oc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254668 406596 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 3 1 7 3.8 Cc1ncc(CNc2ncnc3c2oc2nc(C)c(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
CHEMBL5756940 406596 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 3 1 7 3.8 Cc1ncc(CNc2ncnc3c2oc2nc(C)c(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
132254791 465109 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068912 465109 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
16309462 59870 2 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 59870 2 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
132254495 411387 4 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 2 1 5 3.6 Cc1nc2oc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5806953 411387 4 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 2 1 5 3.6 Cc1nc2oc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382518 177190 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 177190 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155543990 347420 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4526419 347420 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
45501061 312692 12 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 312692 12 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
132254791 465109 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068912 465109 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
137641943 314349 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 314349 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382518 177190 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 177190 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5087948 479301 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 297 2 1 4 4.8 Cc1cc(C)c2c(n1)sc1c(NC3CCCC3)nccc12 10.1016/j.bmcl.2021.128416
156011081 351023 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632962 351023 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
25199525 39971 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223807 39971 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137659901 315385 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 315385 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
53382505 177198 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 177198 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382505 177198 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 177198 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137654582 314859 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 314859 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
56592910 157716 1 None -5 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057392 157716 1 None -5 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
137659901 315385 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 315385 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
140830586 390673 0 None -1 2 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 321 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5556199 390673 0 None -1 2 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 321 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccc3)C1)C2 10.1021/acs.jmedchem.4c00293
137654582 314859 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 314859 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
71533671 221513 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289442 221513 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
89777151 314443 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 314443 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207699 349381 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4574990 349381 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
734373 39174 16 None -1000 2 Rat 5.9 pEC50 = 5.9 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212983 39174 16 None -1000 2 Rat 5.9 pEC50 = 5.9 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
141761390 392090 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 402 4 1 6 5.3 COc1ccc(CNc2nncc3c2sc2nc(C)c(Cl)c(C)c23)cc1F 10.1021/acsmedchemlett.4c00249
CHEMBL5590370 392090 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 402 4 1 6 5.3 COc1ccc(CNc2nncc3c2sc2nc(C)c(Cl)c(C)c23)cc1F 10.1021/acsmedchemlett.4c00249
178318496 466323 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 372 4 0 4 5.4 FC1(Cn2cc(-c3cccnc3-c3ccc4cccnc4c3)cn2)CCCC1 10.1021/acs.jmedchem.5c00678
CHEMBL6142661 466323 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 372 4 0 4 5.4 FC1(Cn2cc(-c3cccnc3-c3ccc4cccnc4c3)cn2)CCCC1 10.1021/acs.jmedchem.5c00678
137650228 313172 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 313172 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
141761390 392090 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 402 4 1 6 5.3 COc1ccc(CNc2nncc3c2sc2nc(C)c(Cl)c(C)c23)cc1F 10.1021/acsmedchemlett.4c00249
CHEMBL5590370 392090 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 402 4 1 6 5.3 COc1ccc(CNc2nncc3c2sc2nc(C)c(Cl)c(C)c23)cc1F 10.1021/acsmedchemlett.4c00249
156022087 352115 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4649459 352115 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
2159295 157714 9 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057376 157714 9 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
122191004 251413 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616497 251413 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
156016090 351625 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4641848 351625 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
53382500 177197 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 177197 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
44448421 26606 0 None None None Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185269 26606 0 None None None Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
682264 83644 13 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 83644 13 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777181 290890 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 290890 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
132254801 463259 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 1 0 5 3.1 Cc1nc2oc3c(N(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6047819 463259 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 1 0 5 3.1 Cc1nc2oc3c(N(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382500 177197 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 177197 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156019946 351908 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4646110 351908 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777181 290890 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 290890 0 None None None Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
169494113 389461 2 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 370 5 0 3 4.1 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)CC)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5440079 389461 2 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 370 5 0 3 4.1 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)CC)C3)CC1 10.1021/acsmedchemlett.3c00331
178303044 466704 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 368 4 0 4 5.7 CC1(Cn2cc(-c3cccnc3-c3ccc4cccnc4c3)cn2)CCCC1 10.1021/acs.jmedchem.5c00678
CHEMBL6152443 466704 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 368 4 0 4 5.7 CC1(Cn2cc(-c3cccnc3-c3ccc4cccnc4c3)cn2)CCCC1 10.1021/acs.jmedchem.5c00678
302 6062 14 None 1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
4630 6062 14 None 1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
CHEMBL7634 6062 14 None 1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
129277684 328522 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4202966 328522 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
135154616 329508 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4215436 329508 0 None None None Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
134207682 347733 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4534301 347733 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207728 348727 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4559283 348727 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
162659751 355147 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4762280 355147 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
140830660 389938 0 None -7 3 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 372 4 0 4 3.4 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5505749 389938 0 None -7 3 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 372 4 0 4 3.4 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
132254801 463259 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 1 0 5 3.1 Cc1nc2oc3c(N(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6047819 463259 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 276 1 0 5 3.1 Cc1nc2oc3c(N(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5089790 479396 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 336 3 1 7 3.6 Cc1cc(C)c2c(n1)sc1c(NCc3cnc(C)nc3)ncnc12 10.1016/j.bmcl.2021.128416
137650228 313172 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 313172 0 None None None Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
53382493 177188 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 177188 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 315257 5 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 315257 5 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
53382493 177188 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 177188 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 315257 5 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 315257 5 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
156016031 351570 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4641135 351570 0 None None None Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777316 313771 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 313771 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5077997 478716 3 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 312 1 0 6 2.7 Cc1cc(C)c2c(n1)sc1c(N3CC4(COC4)C3)ncnc12 10.1016/j.bmcl.2021.128416
682264 83644 13 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 83644 13 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777316 313771 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 313771 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
155539604 346969 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 346969 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
145972844 329604 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 329604 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
155539604 346969 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 346969 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
156012013 351317 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4637785 351317 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
145972844 329604 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 329604 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137653138 314779 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 314779 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 177216 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 177216 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137653138 314779 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 314779 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 177216 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 177216 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156013272 351432 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4639222 351432 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156014779 351480 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4640119 351480 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5088165 479311 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 414 3 1 7 4.4 Cc1cc(C)c2c(n1)oc1c(NC3CN(c4cc(Cl)ncc4Cl)C3)ncnc12 10.1016/j.bmcl.2021.128416
156014138 351194 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4635779 351194 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
71528087 178450 0 None None None Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
CHEMBL2336056 178450 0 None None None Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
145966439 329216 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4211671 329216 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
137656783 315518 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 315518 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777266 294600 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acs.jmedchem.5c00678
CHEMBL3933538 294600 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acs.jmedchem.5c00678
162657433 355021 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
CHEMBL4760902 355021 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
162663713 355805 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4780059 355805 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
141761377 465103 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068884 465103 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5079861 478835 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 430 3 1 7 4.6 Cc1cc(C)c2c(n1)sc1c(NC3CN(c4ncc(C(F)(F)F)cn4)C3)nccc12 10.1016/j.bmcl.2021.128416
683024 104539 17 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 104539 17 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
117916889 335026 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4448985 335026 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
117910878 348459 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4552552 348459 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
132254441 410472 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 Cc1nc2oc3c(NCC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5796855 410472 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 Cc1nc2oc3c(NCC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
177641002 465131 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 395 3 1 6 5.3 Cc1nc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069089 465131 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 395 3 1 6 5.3 Cc1nc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145966183 329188 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 329188 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145966183 329188 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 329188 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
141761377 465103 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068884 465103 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145964807 329231 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 329231 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
683024 104539 17 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 104539 17 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
145964807 329231 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 329231 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
132254668 406596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 3 1 7 3.8 Cc1ncc(CNc2ncnc3c2oc2nc(C)c(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
CHEMBL5756940 406596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 3 1 7 3.8 Cc1ncc(CNc2ncnc3c2oc2nc(C)c(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
177641002 465131 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 395 3 1 6 5.3 Cc1nc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069089 465131 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 395 3 1 6 5.3 Cc1nc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5085861 479168 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 299 1 0 5 3.8 Cc1cc(C)c2c(n1)sc1c(C3CCOCC3)ncnc12 10.1016/j.bmcl.2021.128416
53382480 177207 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 177207 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 177208 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 177208 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632847 312360 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 312360 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
132254441 410472 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 Cc1nc2oc3c(NCC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5796855 410472 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 Cc1nc2oc3c(NCC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5090162 479414 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 387 4 1 8 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(-n4ccnc4)nc3)ncnc12 10.1016/j.bmcl.2021.128416
156013904 351191 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635732 351191 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
42599068 39969 0 None -50 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 39969 0 None -50 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598360 39994 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 39994 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137649420 313419 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 313419 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598359 39996 0 None -125 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 39996 0 None -125 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598586 40013 0 None -7 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 40013 0 None -7 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
89777262 312596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 312596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
25162692 106892 2 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 106892 2 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137656230 314902 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 314902 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5088899 479354 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 268 2 1 5 3.4 Cc1cc(C)c2c(n1)oc1c(NC3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
155524827 335461 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4455058 335461 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207713 334874 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4446894 334874 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
137656783 315518 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 315518 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137646286 313704 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 313704 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
155557669 348706 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4558665 348706 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207694 334854 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
CHEMBL4446559 334854 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
134207702 336881 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4475984 336881 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
53382480 177207 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 177207 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 177208 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 177208 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
16309462 59870 2 None 4 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 59870 2 None 4 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
25162692 106892 2 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 106892 2 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL5082166 478969 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 376 4 1 6 4.8 COc1ccc(C2CC2Nc2ncnc3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2021.128416
155510640 348101 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 348101 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137647620 313494 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 313494 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89777262 312596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 312596 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137646601 313885 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 313885 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
155510640 348101 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 348101 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
140830536 390642 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 2 1 4 2.0 Cc1cc(C)c2c(n1)CN(C(=O)NC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555814 390642 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 2 1 4 2.0 Cc1cc(C)c2c(n1)CN(C(=O)NC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
137640564 312953 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 312953 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
26441386 277658 1 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 277658 1 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
134207723 349389 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4575270 349389 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137646286 313704 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 313704 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
129277689 328980 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4208543 328980 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
12301 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 298274 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 298274 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
12301 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 298274 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 298274 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162644740 353316 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4740272 353316 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
26441386 277658 1 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 277658 1 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137632847 312360 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 312360 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020948 352039 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4648135 352039 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL5082904 479011 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 270 1 0 5 3.1 Cc1cc(C)c2c(n1)sc1c(N3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
156020141 351980 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647288 351980 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
127043636 277772 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 277772 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382478 177212 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 177212 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382478 177212 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 177212 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137646601 313885 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 313885 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
89777147 312301 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 312301 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777355 329552 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 329552 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
1506223 177210 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 177210 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777355 329552 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 329552 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777147 312301 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 312301 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
3652 8876 57 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
57 8876 57 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809 8876 57 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
CHEMBL21536 8876 57 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
DB15357 8876 57 None 1 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
135154300 328924 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4207853 328924 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
135171475 328943 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4208024 328943 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
135171550 329121 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4210497 329121 0 None None None Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
137658662 315273 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101054 315273 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137635043 311956 18 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 311956 18 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155522181 335235 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4451787 335235 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
162650513 353931 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4747706 353931 0 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
1506223 177210 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 177210 9 None None None Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043636 277772 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 277772 0 None None None Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155540233 347025 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 347025 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
89768749 315138 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 315138 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
5204148 77487 10 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL1424504 77487 10 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
155540233 347025 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 347025 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
45142487 59640 0 None None None Rat 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
CHEMBL1354105 59640 0 None None None Rat 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
156017839 351790 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644300 351790 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
137649420 313419 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 313419 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137640564 312953 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 312953 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
127043450 277683 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 277683 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
89768749 315138 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 315138 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137635043 311956 18 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 311956 18 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
140830660 389938 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 372 4 0 4 3.4 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5505749 389938 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 372 4 0 4 3.4 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
44253016 161911 2 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 161911 2 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
141761370 465120 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 336 5 1 6 4.0 COCCCNc1nncc2c1sc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL6069019 465120 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 336 5 1 6 4.0 COCCCNc1nncc2c1sc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
141761370 465120 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 336 5 1 6 4.0 COCCCNc1nncc2c1sc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL6069019 465120 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 336 5 1 6 4.0 COCCCNc1nncc2c1sc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
134207681 349650 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4581412 349650 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
127043450 277683 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 277683 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
132254594 465099 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 2 1 5 4.7 Cc1nc2sc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068811 465099 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 2 1 5 4.7 Cc1nc2sc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254594 465099 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 2 1 5 4.7 Cc1nc2sc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068811 465099 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 2 1 5 4.7 Cc1nc2sc3c(NC4CC4(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
45142483 105854 0 None None None Rat 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
CHEMBL1593296 105854 0 None None None Rat 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
155563393 349332 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 349332 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
155563393 349332 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 349332 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
137647620 313494 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1021/acs.jmedchem.5c00678
CHEMBL4080878 313494 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1021/acs.jmedchem.5c00678
137647620 313494 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 313494 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
42598828 39993 0 None -158 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 39993 0 None -158 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 40015 0 None -79 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 40015 0 None -79 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16038385 161912 1 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL2146598 161912 1 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
145978398 328921 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 328921 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
53382534 177215 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313403 177215 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
172454238 388416 0 None None None Human 8.6 pEC50 = 8.6 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 424 3 0 2 5.1 O=C(N1CC2(CC[C@@H](N3CCC(c4cc(Cl)ccc4Cl)CC3)C2)C1)C1(F)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5416536 388416 0 None None None Human 8.6 pEC50 = 8.6 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 424 3 0 2 5.1 O=C(N1CC2(CC[C@@H](N3CCC(c4cc(Cl)ccc4Cl)CC3)C2)C1)C1(F)CC1 10.1021/acsmedchemlett.3c00331
155519300 334926 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4447724 334926 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
171092502 466471 0 None None None Human 7.7 pEC50 = 7.7 Functional
Modulatory activity at M4 receptor (unknown origin) expressed in CHO-K1 cells assessed as cAMP production by TR-FRET analysisModulatory activity at M4 receptor (unknown origin) expressed in CHO-K1 cells assessed as cAMP production by TR-FRET analysis
ChEMBL 455 4 1 7 3.0 CCOC(=O)N1CC2(CC[C@H](N3CCC(O)(c4cc(F)cnc4-c4cnccn4)CC3)C2)C1 10.1021/acsmedchemlett.4c00512
CHEMBL6146401 466471 0 None None None Human 7.7 pEC50 = 7.7 Functional
Modulatory activity at M4 receptor (unknown origin) expressed in CHO-K1 cells assessed as cAMP production by TR-FRET analysisModulatory activity at M4 receptor (unknown origin) expressed in CHO-K1 cells assessed as cAMP production by TR-FRET analysis
ChEMBL 455 4 1 7 3.0 CCOC(=O)N1CC2(CC[C@H](N3CCC(O)(c4cc(F)cnc4-c4cnccn4)CC3)C2)C1 10.1021/acsmedchemlett.4c00512
134207721 334376 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4439440 334376 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
162643836 355558 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4776981 355558 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162661731 355703 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4778766 355703 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
162664667 355986 0 None 54 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4782416 355986 0 None 54 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162665586 356220 1 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4785432 356220 1 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
135154593 328579 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4203670 328579 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
135150478 328880 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
CHEMBL4207315 328880 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
135150406 329251 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
CHEMBL4212205 329251 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
122387448 275684 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1021/acs.jmedchem.5c00678
CHEMBL3770968 275684 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1021/acs.jmedchem.5c00678
145978398 328921 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 328921 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89445258 348746 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4559841 348746 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207685 334627 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4443127 334627 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
9936450 78636 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143469 78636 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
53382534 177215 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313403 177215 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5078186 478730 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 257 1 0 4 3.5 Cc1cc(C)c2c(n1)sc1c(N(C)C)nccc12 10.1016/j.bmcl.2021.128416
137642025 314012 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 314012 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137642025 314012 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 314012 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
53382508 177194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 177194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632597 312248 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4065706 312248 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89768736 291044 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 291044 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382508 177194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 177194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89768736 291044 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 291044 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768736 291044 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 291044 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
117917124 335337 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4453085 335337 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
41358726 336321 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4467950 336321 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
134207706 348488 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4553231 348488 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
137646437 313532 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4081305 313532 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137641641 314194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4089170 314194 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
137656749 315448 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4103287 315448 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
306 7028 17 None 2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 7028 17 None 2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 7028 17 None 2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 7028 17 None 2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
650899 117263 6 None -7 5 Rat 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 117263 6 None -7 5 Rat 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
89777237 312238 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 312238 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777237 312238 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 312238 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207726 349098 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4568327 349098 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
135153778 329319 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4212929 329319 0 None None None Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
89777060 313031 0 None 114 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 313031 0 None 114 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777160 310047 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 310047 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777160 310047 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 310047 0 None None None Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155562860 349203 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4570659 349203 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
162650410 353976 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 400 3 2 9 1.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncncc4C#N)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4748261 353976 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 400 3 2 9 1.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncncc4C#N)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89445250 335708 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4458842 335708 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
155540893 347080 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039
CHEMBL4517529 347080 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039
137656749 315448 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4103287 315448 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137632597 312248 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4065706 312248 0 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
1505736 177170 8 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313073 177170 8 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135126266 329166 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210986 329166 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155544229 347469 0 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 347469 0 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777224 329011 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4209023 329011 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
155544229 347469 0 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 347469 0 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777224 329011 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4209023 329011 0 None None None Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
11536903 4875 52 None -5 3 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
3262 4875 52 None -5 3 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
CHEMBL3770346 4875 52 None -5 3 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
3263 8727 47 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
864492 8727 47 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
CHEMBL1978713 8727 47 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
12301 8771 38 None 7 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
73774630 8771 38 None 7 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
CHEMBL3915634 8771 38 None 7 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
56592910 157716 1 None 5 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2017.10.016
CHEMBL2057392 157716 1 None 5 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2017.10.016
127044078 277662 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL3808485 277662 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.10.016
89777239 328915 33 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2017.10.016
CHEMBL4207737 328915 33 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2017.10.016
135126266 329166 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210986 329166 0 None None None Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
1505736 177170 8 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313073 177170 8 None None None Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
122191002 251688 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
CHEMBL3618445 251688 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
155551015 348038 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 379 4 0 6 3.1 COc1cccnc1C1CCN(C2CC3(CCN(c4cnccn4)C3)C2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4541697 348038 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 379 4 0 6 3.1 COc1cccnc1C1CCN(C2CC3(CCN(c4cnccn4)C3)C2)CC1 10.1021/acsmedchemlett.9b00106
3652 8876 57 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
57 8876 57 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809 8876 57 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
CHEMBL21536 8876 57 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
DB15357 8876 57 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
137650402 313071 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075391 313071 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
145963804 329029 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4209311 329029 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
145963804 329029 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4209311 329029 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
127043637 277811 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810300 277811 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155518790 334869 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 5 0 5 3.1 CCOC(=O)N1CCC(CN2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4446791 334869 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 5 0 5 3.1 CCOC(=O)N1CCC(CN2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
89777060 313031 0 None 114 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 313031 0 None 114 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777113 295682 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942363 295682 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777113 295682 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942363 295682 0 None None None Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777226 315319 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101598 315319 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89452445 347309 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 320 3 1 5 4.3 Cc1nc2sc3c(NCC4CC4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
CHEMBL4522777 347309 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 320 3 1 5 4.3 Cc1nc2sc3c(NCC4CC4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
137641641 314194 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4089170 314194 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
162664650 355935 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 421 5 2 9 2.4 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4nnc(CC(C)C)o4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4781873 355935 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 421 5 2 9 2.4 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4nnc(CC(C)C)o4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
16371349 277742 3 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809384 277742 3 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127043637 277811 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810300 277811 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137646437 313532 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4081305 313532 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5091043 479457 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 396 4 2 6 4.8 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3F)ncnc12 10.1016/j.bmcl.2021.128416
CHEMBL5075610 478584 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 283 1 0 4 4.1 Cc1cc(C)c2c(n1)sc1c(N3CCCC3)nccc12 10.1016/j.bmcl.2021.128416
CHEMBL5083833 479064 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 380 2 0 5 4.4 Cc1cc(C)c2c(n1)sc1c(C3CCN(C(=O)C4(C)CC4)CC3)ncnc12 10.1016/j.bmcl.2021.128416
137658427 315558 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104561 315558 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
16371349 277742 3 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809384 277742 3 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
56592905 157715 1 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3cccnc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057391 157715 1 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3cccnc3)nc12 10.1016/j.bmcl.2012.05.109
122189495 251415 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616499 251415 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156016660 351647 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642156 351647 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155563393 349332 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 349332 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
132254437 392326 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 315 1 0 6 3.2 Cc1c(Cl)cnc2sc3c(N4CC(C#N)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5594533 392326 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 315 1 0 6 3.2 Cc1c(Cl)cnc2sc3c(N4CC(C#N)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
140830668 390855 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 388 5 0 5 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(OC(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5558931 390855 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 388 5 0 5 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(OC(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
89777356 311810 0 None 72 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4060475 311810 0 None 72 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
140830563 390149 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5517958 390149 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
155563393 349332 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 349332 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
134207710 335960 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nccn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4462813 335960 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nccn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
132254437 392326 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 315 1 0 6 3.2 Cc1c(Cl)cnc2sc3c(N4CC(C#N)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5594533 392326 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 315 1 0 6 3.2 Cc1c(Cl)cnc2sc3c(N4CC(C#N)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
156012527 351254 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 2 6 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4636668 351254 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 2 6 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156014224 351209 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4636061 351209 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
156011921 351348 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638291 351348 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
178314266 466909 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 320 6 1 4 4.1 CC(C)CCn1cc(-c2cccnc2-c2ccc(CN)cc2)cn1 10.1021/acs.jmedchem.5c00678
CHEMBL6163922 466909 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 320 6 1 4 4.1 CC(C)CCn1cc(-c2cccnc2-c2ccc(CN)cc2)cn1 10.1021/acs.jmedchem.5c00678
137650402 313071 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075391 313071 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
53382492 177211 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313397 177211 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777356 311810 0 None 72 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4060475 311810 0 None 72 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
177642427 392410 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 2 1 5 3.8 Cc1c(Cl)cnc2sc3c(NC4CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595674 392410 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 2 1 5 3.8 Cc1c(Cl)cnc2sc3c(NC4CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
135153922 329586 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 364 5 1 7 2.4 COc1ccc(OC2CCN(c3nc(CO)nc(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4216650 329586 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 364 5 1 7 2.4 COc1ccc(OC2CCN(c3nc(CO)nc(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
155524827 335461 0 None 12 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4455058 335461 0 None 12 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
177642427 392410 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 2 1 5 3.8 Cc1c(Cl)cnc2sc3c(NC4CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595674 392410 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 2 1 5 3.8 Cc1c(Cl)cnc2sc3c(NC4CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
134207724 336296 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 495 3 2 8 3.8 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(C(F)(F)F)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4467568 336296 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 495 3 2 8 3.8 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(C(F)(F)F)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
132254814 450532 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 1 0 5 3.6 Cc1nc2oc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6016154 450532 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 1 0 5 3.6 Cc1nc2oc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89768534 298274 0 None -14 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 298274 0 None -14 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
16071018 39944 15 None -56 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 39944 15 None -56 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
155546031 347620 0 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 347620 0 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
89768534 298274 0 None -14 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 298274 0 None -14 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382492 177211 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313397 177211 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155532238 336238 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 403 5 0 8 3.2 COc1cccnc1C1CCN(C2CCCN(c3nsnc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4466730 336238 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 403 5 0 8 3.2 COc1cccnc1C1CCN(C2CCCN(c3nsnc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
44422692 26127 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 26127 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
132254814 450532 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 1 0 5 3.6 Cc1nc2oc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6016154 450532 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 1 0 5 3.6 Cc1nc2oc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
44422699 26125 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182272 26125 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
155546031 347620 0 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 347620 0 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
156020148 351982 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 425 3 1 5 3.5 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)c(F)c2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4647297 351982 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 425 3 1 5 3.5 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)c(F)c2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL5085198 479133 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 361 3 1 6 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccc4c(n3)CCC4)ncnc12 10.1016/j.bmcl.2021.128416
140830554 390554 0 None -3 3 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 352 4 0 5 2.5 COc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
CHEMBL5549827 390554 0 None -3 3 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 352 4 0 5 2.5 COc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
134207711 335702 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4458791 335702 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
89777258 312682 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4070692 312682 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
75203027 334902 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 445 4 3 6 2.7 Cc1c[nH]c(=O)c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4447294 334902 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 445 4 3 6 2.7 Cc1c[nH]c(=O)c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
132254609 391984 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 412 4 2 6 5.3 Cc1nc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5584081 391984 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 412 4 2 6 5.3 Cc1nc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5088044 479305 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 254 2 1 5 3.0 Cc1cc(C)c2c(n1)oc1c(NC3CC3)ncnc12 10.1016/j.bmcl.2021.128416
177659177 390743 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 336 3 0 4 2.8 Cc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
CHEMBL5557262 390743 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 336 3 0 4 2.8 Cc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
89777269 313942 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086111 313942 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132254609 391984 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 412 4 2 6 5.3 Cc1nc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5584081 391984 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 412 4 2 6 5.3 Cc1nc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89777269 313942 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086111 313942 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382484 177202 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313388 177202 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137645473 313492 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4080834 313492 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207712 347711 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 462 3 2 9 2.6 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ncc(C(F)(F)F)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4533701 347711 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 462 3 2 9 2.6 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ncc(C(F)(F)F)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207731 349231 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.3 Cc1cc2nccn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4571349 349231 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.3 Cc1cc2nccn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
41528344 334840 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 340 4 1 4 4.2 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4446337 334840 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 340 4 1 4 4.2 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
117916916 348463 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 402 5 1 5 3.8 CCc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)sc2nc(C)cc(C)c12 10.1016/j.bmcl.2018.12.039
CHEMBL4552714 348463 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 402 5 1 5 3.8 CCc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)sc2nc(C)cc(C)c12 10.1016/j.bmcl.2018.12.039
53382484 177202 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313388 177202 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
44251554 21388 0 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 21388 0 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
156016190 351639 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642055 351639 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5086238 479187 1 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 284 1 0 5 3.5 Cc1cc(C)c2c(n1)sc1c(N3CCCC3)ncnc12 10.1016/j.bmcl.2021.128416
57664406 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
6938 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
CHEMBL4089376 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
137645473 313492 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4080834 313492 0 None None None Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
57664406 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.4c00293
6938 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.4c00293
CHEMBL4089376 4877 44 None 123 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.4c00293
137656219 314897 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4096833 314897 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132254778 392211 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 6 3.0 Cc1c(Cl)cnc2sc3c(N4CC5(COC5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5592710 392211 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 6 3.0 Cc1c(Cl)cnc2sc3c(N4CC5(COC5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
132063677 315084 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098874 315084 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
24865895 193604 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL259662 193604 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
17413870 157720 4 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 285 3 1 5 3.0 COc1cccc2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057416 157720 4 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 285 3 1 5 3.0 COc1cccc2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
132063677 315084 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098874 315084 0 None None None Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL5075538 478581 0 None None None Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 229 0 0 4 3.2 Cc1cc(C)c2c(n1)sc1c(C)ncnc12 10.1016/j.bmcl.2021.128416
53382526 177184 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313370 177184 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382526 177184 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313370 177184 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
71719475 178452 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
CHEMBL2336059 178452 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
137658662 315273 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101054 315273 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132254778 392211 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 6 3.0 Cc1c(Cl)cnc2sc3c(N4CC5(COC5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5592710 392211 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 6 3.0 Cc1c(Cl)cnc2sc3c(N4CC5(COC5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
2551 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
5831 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 1644 11 None -5 9 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
89768736 291044 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 291044 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162651426 354079 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 340 2 3 6 2.2 Cc1c(O)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4749546 354079 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 340 2 3 6 2.2 Cc1c(O)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5071551 478468 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 398 4 1 7 3.9 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(S(C)(=O)=O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
53382497 177201 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313387 177201 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155543990 347420 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4526419 347420 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
89777257 315574 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4104862 315574 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382497 177201 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313387 177201 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640924 312994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
CHEMBL4074322 312994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
155538474 347356 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 5 0 6 3.0 COc1cccnc1C1CCN(CC2CCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4524686 347356 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 5 0 6 3.0 COc1cccnc1C1CCN(CC2CCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
155561780 349749 0 None 1698 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 406 4 0 5 3.5 CCOC(=O)N1CCC2(CC(N3C[C@@H]4[C@H](c5nccn5-c5ccccc5)[C@@H]4C3)C2)C1 10.1021/acsmedchemlett.9b00106
CHEMBL4583597 349749 0 None 1698 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 406 4 0 5 3.5 CCOC(=O)N1CCC2(CC(N3C[C@@H]4[C@H](c5nccn5-c5ccccc5)[C@@H]4C3)C2)C1 10.1021/acsmedchemlett.9b00106
137656219 314897 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4096833 314897 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777226 315319 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101598 315319 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
162673538 366414 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 442 3 2 7 3.6 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4794104 366414 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 442 3 2 7 3.6 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89768546 295697 0 None 18 2 Rat 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 295697 0 None 18 2 Rat 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
44208359 40589 0 None -23 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 40589 0 None -23 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
16757565 39177 0 None -1 2 Rat 6.5 pEC50 = 6.5 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212989 39177 0 None -1 2 Rat 6.5 pEC50 = 6.5 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1038/nchembio.2007.55
134207684 348624 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4556741 348624 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
53382530 177199 0 None None None Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313385 177199 0 None None None Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640924 312994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
CHEMBL4074322 312994 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
53382515 177185 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313371 177185 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135125815 329447 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214738 329447 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156010562 351000 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010562 351000 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4632555 351000 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632555 351000 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
53382515 177185 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313371 177185 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135125815 329447 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214738 329447 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
132254950 465107 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068906 465107 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
42599070 39968 0 None -79 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 39968 0 None -79 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
134207727 349012 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 4 2 6 3.4 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nccn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4566449 349012 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 4 2 6 3.4 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nccn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
132254950 465107 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068906 465107 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.7 Cc1nc2sc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89777449 328978 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4208486 328978 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
89777449 328978 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4208486 328978 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
177643835 392377 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 341 3 1 6 4.2 Cc1c(Cl)cnc2sc3c(NCc4ccncc4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595335 392377 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 341 3 1 6 4.2 Cc1c(Cl)cnc2sc3c(NCc4ccncc4)ncnc3c12 10.1021/acsmedchemlett.4c00249
137634025 312554 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4069218 312554 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
89777257 315574 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4104862 315574 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137649175 313334 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4078814 313334 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
71528088 178451 0 None None None Human 6.5 pEC50 = 6.5 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 387 4 1 5 1.6 CCOC(=O)N1CCC(O)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
CHEMBL2336057 178451 0 None None None Human 6.5 pEC50 = 6.5 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 387 4 1 5 1.6 CCOC(=O)N1CCC(O)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
177643835 392377 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 341 3 1 6 4.2 Cc1c(Cl)cnc2sc3c(NCc4ccncc4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595335 392377 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 341 3 1 6 4.2 Cc1c(Cl)cnc2sc3c(NCc4ccncc4)ncnc3c12 10.1021/acsmedchemlett.4c00249
132254735 404872 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 CCC1CC1Nc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5740059 404872 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 CCC1CC1Nc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
132254735 404872 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 CCC1CC1Nc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5740059 404872 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 3 1 5 4.3 CCC1CC1Nc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
53382502 177204 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313390 177204 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145976573 328646 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204671 328646 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137658427 315558 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104561 315558 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137634025 312554 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4069218 312554 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
53382502 177204 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313390 177204 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5076867 478656 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 377 4 2 5 5.3 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3)nccc12 10.1016/j.bmcl.2021.128416
89777179 312767 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4071560 312767 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137650247 313216 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4077183 313216 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155554015 349681 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 349681 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
145976835 328672 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4204950 328672 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
155554015 349681 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 349681 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
145976835 328672 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4204950 328672 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
135125818 328926 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4207861 328926 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
135125818 328926 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4207861 328926 0 None None None Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
89777179 312767 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4071560 312767 0 None None None Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
140830612 390471 0 None -4 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5542486 390471 0 None -4 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5075035 478554 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 361 3 1 6 4.6 Cc1cc(C)c2c(n1)sc1c(NC3CC(c4ccncc4)C3)ncnc12 10.1016/j.bmcl.2021.128416
CHEMBL5085187 479131 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 298 1 0 6 4.0 Cc1cc(C)c2c(n1)sc1c(-c3nccs3)ncnc12 10.1016/j.bmcl.2021.128416
155520521 335068 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4449608 335068 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
885513 347383 6 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 347383 6 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777238 312937 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4073549 312937 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132254540 448316 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 3 1 5 3.9 CCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5992480 448316 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 3 1 5 3.9 CCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
53382540 177196 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313382 177196 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156013434 351455 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 6 1.6 Cc1c2c(N)c(C(=O)NC3CN(c4ncccc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4639628 351455 0 None None None Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 6 1.6 Cc1c2c(N)c(C(=O)NC3CN(c4ncccc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
155560153 348981 0 None -3 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 348981 0 None -3 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
122191001 251687 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
CHEMBL3618444 251687 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
885513 347383 6 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 347383 6 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155520521 335068 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4449608 335068 0 None None None Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
155560153 348981 0 None -3 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 348981 0 None -3 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
53382540 177196 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313382 177196 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
140830622 390142 0 None -8 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 347 3 0 5 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C#N)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5517849 390142 0 None -8 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 347 3 0 5 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C#N)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5089635 479388 0 None None None Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 284 2 1 5 3.8 Cc1cc(C)c2c(n1)sc1c(NC3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
89777258 312682 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4070692 312682 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
140830673 390661 0 None 28 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncn3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5556081 390661 0 None 28 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncn3)C1)C2 10.1021/acs.jmedchem.4c00293
132254994 426310 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 1 0 5 3.3 Cc1nc2oc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5863136 426310 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 1 0 5 3.3 Cc1nc2oc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254792 445861 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 320 5 1 6 3.5 COCCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5966002 445861 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 320 5 1 6 3.5 COCCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
132254540 448316 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 3 1 5 3.9 CCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5992480 448316 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 290 3 1 5 3.9 CCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
156020077 352065 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4648817 352065 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
89777192 329352 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4213420 329352 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777261 299518 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 299518 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777192 329352 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4213420 329352 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777261 299518 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 299518 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
132254994 426310 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 1 0 5 3.3 Cc1nc2oc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5863136 426310 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 288 1 0 5 3.3 Cc1nc2oc3c(N4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254792 445861 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 320 5 1 6 3.5 COCCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
CHEMBL5966002 445861 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 320 5 1 6 3.5 COCCCNc1ncnc2c1oc1nc(C)c(Cl)c(C)c12 10.1021/acsmedchemlett.4c00249
156013280 351439 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4639387 351439 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
155540233 347025 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 347025 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
155522645 335322 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4452874 335322 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137649175 313334 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4078814 313334 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
156014638 351177 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4635575 351177 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
672747 347024 10 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 347024 10 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
672747 347024 10 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 347024 10 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
122191005 251690 0 None -23 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618447 251690 0 None -23 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156018661 351765 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4644004 351765 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156020827 351993 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1nn(C)c2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
CHEMBL4647393 351993 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1nn(C)c2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
156013839 351127 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4634770 351127 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
137650247 313216 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4077183 313216 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137640000 312654 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4070423 312654 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
141761375 465114 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068969 465114 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
3263 8727 47 None 2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.5c00678
864492 8727 47 None 2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.5c00678
CHEMBL1978713 8727 47 None 2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.5c00678
155546031 347620 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 347620 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
885513 347383 6 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 347383 6 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155554015 349681 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 349681 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155546031 347620 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 347620 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
885513 347383 6 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 347383 6 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155554015 349681 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 349681 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
135126273 328846 2 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL4206946 328846 2 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
155546304 347633 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 300 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCC3CCCC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4531650 347633 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 300 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCC3CCCC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
24979170 45218 2 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1314270 45218 2 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
24979170 45218 2 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1314270 45218 2 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126273 328846 2 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL4206946 328846 2 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
156009502 351056 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4c(C)n(C)nc4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4633344 351056 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4c(C)n(C)nc4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
30270932 277700 7 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808920 277700 7 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126256 329503 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4215358 329503 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
11536903 4875 52 None 5 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
3262 4875 52 None 5 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
CHEMBL3770346 4875 52 None 5 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1021/acs.jmedchem.5c00678
141761375 465114 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068969 465114 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 354 2 1 5 4.7 Cc1nc2sc3c(NC4CC(F)(F)C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
42598591 39967 0 None -79 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 39967 0 None -79 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
30270932 277700 7 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808920 277700 7 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
11081520 237756 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cellsAgonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cells
ChEMBL 420 7 0 10 2.3 CN1CCC=C(c2nsnc2OCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL342400 237756 0 None None None Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cellsAgonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cells
ChEMBL 420 7 0 10 2.3 CN1CCC=C(c2nsnc2OCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL5094699 479668 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 255 1 0 4 3.7 Cc1cc(C)c2c(n1)sc1c(C3CC3)ncnc12 10.1016/j.bmcl.2021.128416
135126256 329503 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4215358 329503 0 None None None Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122191007 251692 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618449 251692 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
122189496 251416 0 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616500 251416 0 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
734374 39175 24 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 301 3 2 5 3.0 Cc1cc(C)c2c(N)c(C(=O)NCc3ccco3)sc2n1 10.1021/acs.jmedchem.5c00678
CHEMBL1212984 39175 24 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 301 3 2 5 3.0 Cc1cc(C)c2c(N)c(C(=O)NCc3ccco3)sc2n1 10.1021/acs.jmedchem.5c00678
141761387 465119 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 3 1 5 4.7 Cc1nc2sc3c(NCC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069007 465119 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 3 1 5 4.7 Cc1nc2sc3c(NCC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145964223 329396 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214008 329396 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
19571628 349384 0 None -7 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 349384 0 None -7 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
2551 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
298 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
488 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
5831 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
CHEMBL965 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
DB00411 1644 11 None -5 9 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
19571628 349384 0 None -7 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 349384 0 None -7 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
10952416 78631 0 None 323 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143466 78631 0 None 323 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
3652 8876 57 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
57 8876 57 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
60809 8876 57 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
CHEMBL21536 8876 57 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
DB15357 8876 57 None 1 7 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
87057216 336774 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 4 1 7 3.8 COc1ccc(CNc2nn(C)c3c2sc2nnc(C)c(C)c23)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4474325 336774 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 4 1 7 3.8 COc1ccc(CNc2nn(C)c3c2sc2nnc(C)c(C)c23)cc1 10.1016/j.bmcl.2018.12.039
135409468 4159 52 None -8 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 4159 52 None -8 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 4159 52 None -8 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
154733029 8711 48 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1021/acs.jmedchem.5c00678
7633 8711 48 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1021/acs.jmedchem.5c00678
CHEMBL1212994 8711 48 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1021/acs.jmedchem.5c00678
154733029 8711 48 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
7633 8711 48 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
CHEMBL1212994 8711 48 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
132254295 392274 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.2 Cc1c(Cl)cnc2sc3c(NC4(C)CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5593824 392274 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.2 Cc1c(Cl)cnc2sc3c(NC4(C)CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
132254775 410546 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 338 2 1 5 4.3 Cc1nc2oc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5797755 410546 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 338 2 1 5 4.3 Cc1nc2oc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
141761387 465119 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 3 1 5 4.7 Cc1nc2sc3c(NCC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069007 465119 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 3 1 5 4.7 Cc1nc2sc3c(NCC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145964223 329396 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214008 329396 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL5085688 479156 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 386 5 1 6 5.1 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(OC(F)F)cc3)ncnc12 10.1016/j.bmcl.2021.128416
1541501 8725 30 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5c00678
3256 8725 30 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5c00678
CHEMBL4461667 8725 30 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5c00678
122191008 251693 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618450 251693 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
145973064 329584 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216633 329584 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145976573 328646 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204671 328646 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145973064 329584 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216633 329584 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
132254295 392274 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.2 Cc1c(Cl)cnc2sc3c(NC4(C)CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5593824 392274 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.2 Cc1c(Cl)cnc2sc3c(NC4(C)CC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
132254775 410546 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 338 2 1 5 4.3 Cc1nc2oc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5797755 410546 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 338 2 1 5 4.3 Cc1nc2oc3c(NC4CC(F)(F)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
137640000 312654 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4070423 312654 0 None None None Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207729 348244 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 424 4 2 10 2.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C6CC6)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4547561 348244 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 424 4 2 10 2.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C6CC6)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
16309462 59870 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 59870 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155539719 346996 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 346996 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 349510 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 349510 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
89777032 328727 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4205587 328727 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
53382513 177186 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
CHEMBL2313372 177186 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
89777190 280176 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3894866 280176 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155539719 346996 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 346996 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155553146 348143 0 None -5 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4544318 348143 0 None -5 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
155564640 349510 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 349510 0 None -3 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
89777032 328727 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4205587 328727 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
89777190 280176 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3894866 280176 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382513 177186 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
CHEMBL2313372 177186 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
89777238 312937 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4073549 312937 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
169450433 388764 2 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 356 4 0 3 3.7 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(C)=O)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5423866 388764 2 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 356 4 0 3 3.7 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(C)=O)C3)CC1 10.1021/acsmedchemlett.3c00331
140830622 390142 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 347 3 0 5 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C#N)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5517849 390142 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 347 3 0 5 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C#N)c3)C1)C2 10.1021/acs.jmedchem.4c00293
156010493 351037 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4633152 351037 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2nn1C 10.1016/j.bmcl.2019.126812
141761379 465112 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068956 465112 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
127044525 277803 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810183 277803 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
187 524 25 None 1 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
294 524 25 None 1 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
65 524 25 None 1 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
CHEMBL667 524 25 None 1 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
DB03128 524 25 None 1 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
172463125 388965 0 None None None Human 6.4 pEC50 = 6.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 424 3 0 2 5.1 O=C(N1CC2(CC[C@H](N3CCC(c4cc(Cl)ccc4Cl)CC3)C2)C1)C1(F)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5428504 388965 0 None None None Human 6.4 pEC50 = 6.4 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 424 3 0 2 5.1 O=C(N1CC2(CC[C@H](N3CCC(c4cc(Cl)ccc4Cl)CC3)C2)C1)C1(F)CC1 10.1021/acsmedchemlett.3c00331
156014184 351149 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4635170 351149 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
141761379 465112 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068956 465112 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
127044525 277803 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810183 277803 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
89768704 314313 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090463 314313 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
145971419 329608 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4216930 329608 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127043632 277659 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808442 277659 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
89768704 314313 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090463 314313 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777222 297236 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3955059 297236 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777222 297236 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3955059 297236 0 None None None Rat 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
140830676 390610 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 307 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)C[C@@H]1C[C@H]1c1cccnc1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555232 390610 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 307 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)C[C@@H]1C[C@H]1c1cccnc1)C2 10.1021/acs.jmedchem.4c00293
145971419 329608 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4216930 329608 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127043632 277659 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808442 277659 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
89777270 328617 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204144 328617 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145975083 328606 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203977 328606 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
89777270 328617 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204144 328617 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145975083 328606 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203977 328606 0 None None None Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156019934 351891 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 3 2 7 1.2 Cn1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4645945 351891 0 None None None Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 3 2 7 1.2 Cn1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
132254868 465132 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 356 3 1 7 3.9 Cc1ncc(CNc2ncnc3c2sc2ncc(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
CHEMBL6069105 465132 0 None None None Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 356 3 1 7 3.9 Cc1ncc(CNc2ncnc3c2sc2ncc(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
CHEMBL5082438 478982 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 296 1 0 5 3.3 Cc1cc(C)c2c(n1)sc1c(N3CC4CC4C3)ncnc12 10.1016/j.bmcl.2021.128416
145965409 329013 0 None None None Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4209083 329013 0 None None None Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156012624 351368 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4638506 351368 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL5073777 478511 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 306 1 0 5 3.3 Cc1cc(C)c2c(n1)sc1c(N3CC(F)(F)C3)ncnc12 10.1016/j.bmcl.2021.128416
145968703 329716 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4218342 329716 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
145968703 329716 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4218342 329716 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
132254868 465132 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 356 3 1 7 3.9 Cc1ncc(CNc2ncnc3c2sc2ncc(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
CHEMBL6069105 465132 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 356 3 1 7 3.9 Cc1ncc(CNc2ncnc3c2sc2ncc(Cl)c(C)c23)cn1 10.1021/acsmedchemlett.4c00249
145965409 329013 0 None None None Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4209083 329013 0 None None None Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
134207719 349865 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4586356 349865 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
156010345 351028 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 8 1.1 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4633013 351028 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 8 1.1 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156022245 351174 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 1 0 4 3.4 Cc1c2c(ccc3c(CC(C)(C)C)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635539 351174 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 1 0 4 3.4 Cc1c2c(ccc3c(CC(C)(C)C)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156011257 351280 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4637175 351280 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
72945087 239183 2 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3545481 239183 2 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
89777278 298553 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3966208 298553 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777278 298553 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3966208 298553 0 None None None Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155523539 335434 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 387 4 0 7 3.5 COc1cccnc1C1CCN(C2CCCN(c3nsnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4454446 335434 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 387 4 0 7 3.5 COc1cccnc1C1CCN(C2CCCN(c3nsnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
156014219 351199 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4635909 351199 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
156012754 351263 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636845 351263 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155520162 347347 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 347347 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
698706 349534 16 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 349534 16 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
155520162 347347 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 347347 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
698706 349534 16 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 349534 16 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
140830668 390855 0 None -1 3 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 388 5 0 5 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(OC(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5558931 390855 0 None -1 3 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 388 5 0 5 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(OC(F)F)c3)C1)C2 10.1021/acs.jmedchem.4c00293
187 524 25 None 1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 524 25 None 1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 524 25 None 1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 524 25 None 1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 524 25 None 1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
89777463 314675 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4094439 314675 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
698706 349534 16 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 349534 16 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
137652430 313424 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4079953 313424 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
698706 349534 16 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 349534 16 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
156019515 351906 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 392 3 1 5 3.9 Cc1nc2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2s1 10.1016/j.bmcl.2019.126812
CHEMBL4646040 351906 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 392 3 1 5 3.9 Cc1nc2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2s1 10.1016/j.bmcl.2019.126812
3263 8727 47 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
864492 8727 47 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
CHEMBL1978713 8727 47 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
9809330 234933 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL335542 234933 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
306 7028 17 None 2 5 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
3536 7028 17 None 2 5 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
9577995 7028 17 None 2 5 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
CHEMBL134641 7028 17 None 2 5 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
137653452 314474 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
CHEMBL4092128 314474 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
140830533 390323 0 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 324 2 0 5 2.4 Cc1cc(C)c2c(n1)CN(C(=O)OC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5527951 390323 0 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 324 2 0 5 2.4 Cc1cc(C)c2c(n1)CN(C(=O)OC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
45142486 105586 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
CHEMBL1589763 105586 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
42598829 39970 0 None -63 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 39970 0 None -63 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 40014 0 None -199 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 40014 0 None -199 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 39944 15 None -56 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 39944 15 None -56 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
137653452 314474 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
CHEMBL4092128 314474 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
140830533 390323 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 324 2 0 5 2.4 Cc1cc(C)c2c(n1)CN(C(=O)OC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5527951 390323 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 324 2 0 5 2.4 Cc1cc(C)c2c(n1)CN(C(=O)OC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
89777261 299518 0 None 7 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 299518 0 None 7 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777261 299518 0 None 7 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 299518 0 None 7 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162655852 354591 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 4 2 8 2.6 CCc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4755728 354591 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 4 2 8 2.6 CCc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
141761384 465125 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 330 1 0 5 4.0 Cc1nc2sc3c(N4CC5CC5C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069043 465125 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 330 1 0 5 4.0 Cc1nc2sc3c(N4CC5CC5C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
117916853 348256 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 4 1 4 3.9 COc1ccc(CNC(=O)c2cc3c(C)cc(C)nc3s2)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4547995 348256 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 4 1 4 3.9 COc1ccc(CNC(=O)c2cc3c(C)cc(C)nc3s2)cc1 10.1016/j.bmcl.2018.12.039
137652430 313424 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4079953 313424 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
141761384 465125 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 330 1 0 5 4.0 Cc1nc2sc3c(N4CC5CC5C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069043 465125 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 330 1 0 5 4.0 Cc1nc2sc3c(N4CC5CC5C4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382498 177214 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313402 177214 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382498 177214 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313402 177214 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156019814 351334 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 295 1 0 6 1.7 Cc1c2c(ccc3c(N4CC5(COC5)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638044 351334 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 295 1 0 6 1.7 Cc1c2c(ccc3c(N4CC5(COC5)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155520162 347347 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 347347 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
141761385 392187 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 420 5 1 6 5.7 Cc1nc2sc3c(NCc4ccc(OC(F)F)cc4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5592234 392187 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 420 5 1 6 5.7 Cc1nc2sc3c(NCc4ccc(OC(F)F)cc4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
137637726 311817 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
CHEMBL4060527 311817 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
11498 6149 38 None 24 2 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
4995951 6149 38 None 24 2 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
CHEMBL59898 6149 38 None 24 2 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
137633999 312477 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4068328 312477 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
155520162 347347 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 347347 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
162667175 356226 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 451 4 2 8 3.1 Cc1c(C(C)C)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4785538 356226 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 451 4 2 8 3.1 Cc1c(C(C)C)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
141761385 392187 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 420 5 1 6 5.7 Cc1nc2sc3c(NCc4ccc(OC(F)F)cc4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5592234 392187 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 420 5 1 6 5.7 Cc1nc2sc3c(NCc4ccc(OC(F)F)cc4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89768546 295697 0 None -18 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 295697 0 None -18 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768546 295697 0 None -18 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 295697 0 None -18 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
156013700 351227 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636269 351227 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
137633999 312477 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4068328 312477 0 None None None Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382523 157721 8 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 157721 8 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382523 157721 8 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 157721 8 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
172443792 387430 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 386 4 0 5 1.9 COc1ccccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5396126 387430 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 386 4 0 5 1.9 COc1ccccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
117917123 336223 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 5 1 5 4.3 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C2CC2)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4466551 336223 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 5 1 5 4.3 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C2CC2)cc1F 10.1016/j.bmcl.2018.12.039
19571628 349384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 349384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
19571628 349384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 349384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
53002564 313050 5 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075147 313050 5 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
89777274 314618 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4093866 314618 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137653326 314709 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4094821 314709 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137657888 315523 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4104193 315523 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
89777274 314618 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4093866 314618 0 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137637726 311817 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
CHEMBL4060527 311817 0 None None None Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
53002564 313050 5 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075147 313050 5 None None None Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
145973726 329560 0 None 36 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216213 329560 0 None 36 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
187 524 25 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
294 524 25 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
65 524 25 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
CHEMBL667 524 25 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
DB03128 524 25 None 1 5 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
145973726 329560 0 None 36 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216213 329560 0 None 36 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777153 290021 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3896591 290021 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777153 290021 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3896591 290021 0 None None None Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
18204435 80902 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
CHEMBL1455259 80902 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
137653326 314709 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4094821 314709 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
18204435 80902 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
CHEMBL1455259 80902 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
127044078 277662 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 277662 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
137657888 315523 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4104193 315523 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
89777463 314675 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4094439 314675 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
71683155 313100 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4075751 313100 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
156016804 351661 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 403 4 1 5 3.5 CCc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4642310 351661 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 403 4 1 5 3.5 CCc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
145975343 328650 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4204738 328650 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155544229 347469 0 None 3 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 347469 0 None 3 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
45501063 313116 9 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4076022 313116 9 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
132254751 432753 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.4 Cc1nc2oc3c(NC4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5930897 432753 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.4 Cc1nc2oc3c(NC4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
145975343 328650 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4204738 328650 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
132254915 465135 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069141 465135 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
155544229 347469 0 None 3 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 347469 0 None 3 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
140830563 390149 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5517958 390149 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
132254751 432753 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.4 Cc1nc2oc3c(NC4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5930897 432753 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 316 2 1 5 4.4 Cc1nc2oc3c(NC4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
117916866 348912 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 3 1 4 4.1 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)CCO4)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4563934 348912 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 3 1 4 4.1 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)CCO4)sc2n1 10.1016/j.bmcl.2018.12.039
132254915 465135 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069141 465135 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 1 0 5 4.1 Cc1nc2sc3c(N4CCCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
156017788 351747 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 1 7 2.7 COc1ccc(CNc2ncnc3c2ccc2nnn(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4643687 351747 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 1 7 2.7 COc1ccc(CNc2ncnc3c2ccc2nnn(C)c23)cc1F 10.1016/j.bmcl.2019.126811
3263 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
864492 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
CHEMBL1978713 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
973723 39173 10 None 1000 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1021/acs.jmedchem.5c00678
CHEMBL1212982 39173 10 None 1000 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1021/acs.jmedchem.5c00678
3652 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
57 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
CHEMBL21536 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
DB15357 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
156246205 387697 2 None 4 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 384 4 0 4 2.9 COc1ccccc1C1CCN(C2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5401679 387697 2 None 4 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 384 4 0 4 2.9 COc1ccccc1C1CCN(C2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
3652 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 8876 57 None 1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
156246132 388573 4 None 4 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 398 5 0 4 3.3 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5419462 388573 4 None 4 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 398 5 0 4 3.3 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
86292822 335709 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 1 8 3.6 Cc1nnc2sc3c(NCc4ccc5c(c4)OCCO5)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4458844 335709 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 1 8 3.6 Cc1nnc2sc3c(NCc4ccc5c(c4)OCCO5)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207680 347673 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 2 2 7 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4532897 347673 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 2 2 7 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
162652818 354256 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 324 2 2 5 2.5 Cc1cnnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4751679 354256 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 324 2 2 5 2.5 Cc1cnnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
134265583 355845 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 443 3 2 8 2.7 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4780651 355845 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 443 3 2 8 2.7 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89777143 309930 1 None -5 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 309930 1 None -5 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777143 309930 1 None -5 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 309930 1 None -5 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
127044078 277662 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 277662 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
127043635 277716 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809096 277716 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
132254870 462792 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 3 1 5 4.1 Cc1nc2oc3c(NCC(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6043443 462792 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 3 1 5 4.1 Cc1nc2oc3c(NCC(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382520 177192 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313378 177192 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
973723 39173 10 None -1000 2 Rat 5.2 pEC50 = 5.2 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212982 39173 10 None -1000 2 Rat 5.2 pEC50 = 5.2 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1038/nchembio.2007.55
132254479 392382 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.8 Cc1c(Cl)cnc2sc3c(N4CCCC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595406 392382 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.8 Cc1c(Cl)cnc2sc3c(N4CCCC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
2551 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5831 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 1644 11 None -5 9 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
89777146 315511 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104033 315511 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
127043635 277716 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809096 277716 2 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
132254870 462792 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 3 1 5 4.1 Cc1nc2oc3c(NCC(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6043443 462792 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 3 1 5 4.1 Cc1nc2oc3c(NCC(C)C)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382520 177192 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313378 177192 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
132254479 392382 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.8 Cc1c(Cl)cnc2sc3c(N4CCCC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5595406 392382 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 1 0 5 3.8 Cc1c(Cl)cnc2sc3c(N4CCCC4)ncnc3c12 10.1021/acsmedchemlett.4c00249
53382524 177193 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
CHEMBL2313379 177193 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
53382524 177193 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
CHEMBL2313379 177193 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
172452791 388442 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 404 4 0 5 2.0 COc1cc(F)ccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5416951 388442 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 404 4 0 5 2.0 COc1cc(F)ccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5085621 479152 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 298 1 1 5 3.3 Cc1cc(C)c2c(n1)sc1c(C3CCNCC3)ncnc12 10.1016/j.bmcl.2021.128416
135126264 329452 0 None None None Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214822 329452 0 None None None Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137633344 312228 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4065477 312228 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
45501064 312280 11 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
CHEMBL4065963 312280 11 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
55485382 277693 3 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808847 277693 3 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126264 329452 0 None None None Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214822 329452 0 None None None Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137633344 312228 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4065477 312228 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
156017195 351636 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 5 2.4 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642005 351636 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 5 2.4 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
140830575 390649 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cncnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555879 390649 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cncnc3)C1)C2 10.1021/acs.jmedchem.4c00293
87057214 350115 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 3 1 6 3.0 Cc1nnc2sc3c(NCC4CC4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4592523 350115 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 3 1 6 3.0 Cc1nnc2sc3c(NCC4CC4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207689 350100 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 440 3 2 10 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C(C)(C)C)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4592120 350100 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 440 3 2 10 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C(C)(C)C)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
3263 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
864492 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL1978713 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL5089728 479393 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 366 2 0 5 4.0 Cc1cc(C)c2c(n1)sc1c(C3CCN(C(=O)C4CC4)CC3)ncnc12 10.1016/j.bmcl.2021.128416
55485382 277693 3 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808847 277693 3 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156012048 351352 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 7 1.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(F)cn4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638318 351352 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 7 1.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(F)cn4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010237 350995 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 267 1 0 5 2.4 Cc1c2c(ccc3c(N4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632514 350995 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 267 1 0 5 2.4 Cc1c2c(ccc3c(N4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156015762 351490 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4640254 351490 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
89777104 314976 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4097819 314976 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
89777437 315353 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4102040 315353 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
16123945 161913 10 None -125 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 161913 10 None -125 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
137647278 313808 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
CHEMBL4084404 313808 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
12301 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
53002537 312975 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4074092 312975 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
12301 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89777437 315353 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4102040 315353 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
141761368 465104 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068885 465104 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
117916898 347413 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 5 3.6 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc(S(C)(=O)=O)cc3)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4526215 347413 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 5 3.6 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc(S(C)(=O)=O)cc3)sc2n1 10.1016/j.bmcl.2018.12.039
53002537 312975 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4074092 312975 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
177646392 390829 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccn3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5558507 390829 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccn3)C1)C2 10.1021/acs.jmedchem.4c00293
155539604 346969 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 346969 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
49674582 311995 10 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4062718 311995 10 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
155539604 346969 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 346969 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
137647278 313808 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
CHEMBL4084404 313808 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
141761368 465104 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068885 465104 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
45501063 313116 9 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4076022 313116 9 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
49674582 311995 10 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4062718 311995 10 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
156014753 351203 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2n1C 10.1016/j.bmcl.2019.126812
CHEMBL4635969 351203 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2n1C 10.1016/j.bmcl.2019.126812
CHEMBL5086464 479202 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 431 3 1 8 4.0 Cc1cc(C)c2c(n1)sc1c(NC3CN(c4ncc(C(F)(F)F)cn4)C3)ncnc12 10.1016/j.bmcl.2021.128416
45501064 312280 11 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
CHEMBL4065963 312280 11 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
53382516 177195 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313381 177195 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
25067048 26602 0 None None None Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185245 26602 0 None None None Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
71683155 313100 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4075751 313100 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
162665373 356165 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 425 3 3 9 1.7 Cc1c(O)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4784478 356165 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 425 3 3 9 1.7 Cc1c(O)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
156010821 351018 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
156010821 351018 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4632855 351018 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
CHEMBL4632855 351018 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
53382516 177195 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313381 177195 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5092998 479562 0 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 297 1 0 4 4.9 Cc1cc(C)c2c(n1)sc1c(C3CCCCC3)ncnc12 10.1016/j.bmcl.2021.128416
3263 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
864492 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
CHEMBL1978713 8727 47 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
87057213 349737 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 313 3 1 7 3.4 Cc1nnc2sc3c(NCc4ccco4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4583475 349737 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 313 3 1 7 3.4 Cc1nnc2sc3c(NCc4ccco4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
127043638 277713 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809076 277713 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
672747 347024 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 347024 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
127043638 277713 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809076 277713 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
132254579 427519 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 2 1 5 4.0 Cc1nc2oc3c(NC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5876923 427519 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 2 1 5 4.0 Cc1nc2oc3c(NC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
672747 347024 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 347024 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
155539410 346984 0 None 58 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 412 4 0 6 3.4 c1ccc(-n2ccnc2[C@H]2[C@H]3CN(C4CC5(CCN(c6cnccn6)C5)C4)C[C@H]32)cc1 10.1021/acsmedchemlett.9b00106
CHEMBL4515088 346984 0 None 58 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 412 4 0 6 3.4 c1ccc(-n2ccnc2[C@H]2[C@H]3CN(C4CC5(CCN(c6cnccn6)C5)C4)C[C@H]32)cc1 10.1021/acsmedchemlett.9b00106
162667825 356334 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 426 3 2 7 3.0 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccnc(F)c4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4787099 356334 0 None None None Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 426 3 2 7 3.0 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccnc(F)c4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
140830676 390610 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 307 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)C[C@@H]1C[C@H]1c1cccnc1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555232 390610 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 307 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)C[C@@H]1C[C@H]1c1cccnc1)C2 10.1021/acs.jmedchem.4c00293
132254579 427519 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 2 1 5 4.0 Cc1nc2oc3c(NC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL5876923 427519 0 None None None Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 302 2 1 5 4.0 Cc1nc2oc3c(NC4CCC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
56592932 157718 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 305 3 2 4 3.7 COc1ccc(C)c2sc(NC(=O)NC3CCCC3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057406 157718 1 None None None Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 305 3 2 4 3.7 COc1ccc(C)c2sc(NC(=O)NC3CCCC3)nc12 10.1016/j.bmcl.2012.05.109
16757564 39178 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 379 3 2 4 4.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(C(F)(F)F)cc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212992 39178 0 None None None Rat 6.2 pEC50 = 6.2 Functional
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 379 3 2 4 4.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(C(F)(F)F)cc3)sc2n1 10.1038/nchembio.2007.55
89777050 329173 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211076 329173 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
132254699 465111 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068932 465111 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89777050 329173 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211076 329173 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
132254699 465111 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068932 465111 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 304 2 1 5 4.1 Cc1nc2sc3c(NC4CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
156015582 351489 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 3 1 5 3.3 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)cc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4640242 351489 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 3 1 5 3.3 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)cc2nn1C 10.1016/j.bmcl.2019.126812
137659727 315049 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098593 315049 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132254896 465098 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4(C)CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068793 465098 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4(C)CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254837 465123 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 1 0 6 3.5 Cc1nc2sc3c(N4CC(C#N)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069033 465123 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 1 0 6 3.5 Cc1nc2sc3c(N4CC(C#N)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254896 465098 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4(C)CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068793 465098 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4(C)CC4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
132254837 465123 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 1 0 6 3.5 Cc1nc2sc3c(N4CC(C#N)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6069033 465123 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 1 0 6 3.5 Cc1nc2sc3c(N4CC(C#N)C4)ncnc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
156017640 351753 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nn(C)c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
CHEMBL4643858 351753 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nn(C)c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
155540233 347025 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 347025 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
137646732 313679 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4083081 313679 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155553146 348143 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4544318 348143 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
682264 83644 13 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 83644 13 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
137646732 313679 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4083081 313679 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL5083633 479057 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 314 3 0 6 2.9 COCC1CN(c2ncnc3c2sc2nc(C)cc(C)c23)C1 10.1016/j.bmcl.2021.128416
53382523 157721 8 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1021/acs.jmedchem.5c00678
CHEMBL2057417 157721 8 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1021/acs.jmedchem.5c00678
53382542 177191 0 None 1 6 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 177191 0 None 1 6 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382542 177191 0 None 1 6 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 177191 0 None 1 6 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777146 315511 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104033 315511 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777513 312111 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
CHEMBL4064060 312111 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
56592911 157779 0 None None None Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 262 3 1 4 2.5 COc1ccc(C)c2sc(C(=O)NC3CC3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057683 157779 0 None None None Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 262 3 1 4 2.5 COc1ccc(C)c2sc(C(=O)NC3CC3)nc12 10.1016/j.bmcl.2012.05.109
137659727 315049 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098593 315049 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
3263 8727 47 None -2 2 Rat 4.1 pEC50 = 4.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
864492 8727 47 None -2 2 Rat 4.1 pEC50 = 4.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
CHEMBL1978713 8727 47 None -2 2 Rat 4.1 pEC50 = 4.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/acs.jmedchem.4c00293
89777239 328915 33 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acs.jmedchem.5c00678
CHEMBL4207737 328915 33 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acs.jmedchem.5c00678
42598357 39995 0 None -251 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 39995 0 None -251 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 40016 0 None -79 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 40016 0 None -79 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
134207720 349559 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 2 2 6 3.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4579086 349559 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 2 2 6 3.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137631537 312322 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066508 312322 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137631537 312322 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066508 312322 0 None None None Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777239 328915 33 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4207737 328915 33 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2018.12.039
53382482 177205 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313391 177205 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
13626 3199 32 None -3 3 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
140830653 3199 32 None -3 3 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
CHEMBL5314557 3199 32 None -3 3 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
DB18706 3199 32 None -3 3 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
177644406 392265 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 381 3 1 6 5.0 Cc1c(Cl)cnc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5593743 392265 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 381 3 1 6 5.0 Cc1c(Cl)cnc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
177644406 392265 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 381 3 1 6 5.0 Cc1c(Cl)cnc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
CHEMBL5593743 392265 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 381 3 1 6 5.0 Cc1c(Cl)cnc2sc3c(NC4CC(c5ccncc5)C4)ncnc3c12 10.1021/acsmedchemlett.4c00249
53382482 177205 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313391 177205 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
140830554 390554 0 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 352 4 0 5 2.5 COc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
CHEMBL5549827 390554 0 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 352 4 0 5 2.5 COc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
53382503 177203 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313389 177203 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043631 277752 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809482 277752 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382503 177203 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313389 177203 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145974738 329662 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217609 329662 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156017866 351832 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.6 Cn1nnc2ccc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4644929 351832 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.6 Cn1nnc2ccc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
140830536 390642 0 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 2 1 4 2.0 Cc1cc(C)c2c(n1)CN(C(=O)NC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555814 390642 0 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 2 1 4 2.0 Cc1cc(C)c2c(n1)CN(C(=O)NC1CN(c3cccnc3)C1)C2 10.1021/acs.jmedchem.4c00293
127043631 277752 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809482 277752 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156012231 351353 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 2 1 6 2.3 Cn1nnc2ccc3c(NC4CCCC4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4638335 351353 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 2 1 6 2.3 Cn1nnc2ccc3c(NC4CCCC4)ncnc3c21 10.1016/j.bmcl.2019.126811
145974738 329662 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217609 329662 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
141761382 465106 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068903 465106 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
89777468 312448 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4067974 312448 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
141761382 465106 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068903 465106 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 318 2 1 5 4.5 Cc1nc2sc3c(NC4CCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
134207679 336329 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 4 2 7 3.1 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4468120 336329 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 4 2 7 3.1 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
89777468 312448 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4067974 312448 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
140830612 390471 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5542486 390471 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 322 3 0 4 2.5 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccncc3)C1)C2 10.1021/acs.jmedchem.4c00293
71792 159969 34 None -2 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 159969 34 None -2 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
DB12287 159969 34 None -2 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
53382544 177200 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313386 177200 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156020885 352083 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 281 2 1 5 3.2 Cc1c2c(ccc3c(NC4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4649056 352083 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 281 2 1 5 3.2 Cc1c2c(ccc3c(NC4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156013305 351440 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2ncc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4639394 351440 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2ncc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL5078961 478783 2 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 283 2 1 4 4.4 Cc1cc(C)c2c(n1)sc1c(NC3CCC3)nccc12 10.1016/j.bmcl.2021.128416
30299339 277673 2 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808592 277673 2 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145965320 329303 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
CHEMBL4212735 329303 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
145965320 329303 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
CHEMBL4212735 329303 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
30299339 277673 2 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808592 277673 2 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
141761369 465105 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 5 4.5 Cc1nc2sc3c(N4CCCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068893 465105 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 5 4.5 Cc1nc2sc3c(N4CCCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
53382544 177200 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313386 177200 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145978470 328572 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203579 328572 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
145978470 328572 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203579 328572 0 None None None Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122195090 252142 0 None -6 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assayPartial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
CHEMBL3633184 252142 0 None -6 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assayPartial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
155521109 335091 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4449879 335091 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
141761369 465105 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 5 4.5 Cc1nc2sc3c(N4CCCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
CHEMBL6068893 465105 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing chimeric Gqi5 in presence of acetylcholine by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 332 1 0 5 4.5 Cc1nc2sc3c(N4CCCCC4)nncc3c2c(C)c1Cl 10.1021/acsmedchemlett.4c00249
140830575 390649 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cncnc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555879 390649 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 323 3 0 5 1.9 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3cncnc3)C1)C2 10.1021/acs.jmedchem.4c00293
137653737 314561 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4093138 314561 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL5077425 478690 0 None None None Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 379 4 1 6 4.7 Cc1cc(C)c2c(n1)sc1c(OCc3ccc(C(C)(C)O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
177659177 390743 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 336 3 0 4 2.8 Cc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
CHEMBL5557262 390743 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 336 3 0 4 2.8 Cc1cc(N2CC(CC(=O)N3Cc4nc(C)cc(C)c4C3)C2)ccn1 10.1021/acs.jmedchem.4c00293
140830600 390656 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 230 2 0 2 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CC1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5555981 390656 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 230 2 0 2 2.3 Cc1cc(C)c2c(n1)CN(C(=O)CC1CC1)C2 10.1021/acs.jmedchem.4c00293
156013700 351227 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636269 351227 0 None None None Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
134207687 347530 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nncn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4528914 347530 0 None None None Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nncn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
13626 3199 32 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
140830653 3199 32 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
CHEMBL5314557 3199 32 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
DB18706 3199 32 None 3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human M4 receptorAgonist activity at human M4 receptor
ChEMBL 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 10.1021/acs.jmedchem.4c00293
140830586 390673 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 321 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccc3)C1)C2 10.1021/acs.jmedchem.4c00293
CHEMBL5556199 390673 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assayPositive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay
ChEMBL 321 3 0 3 3.1 Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccccc3)C1)C2 10.1021/acs.jmedchem.4c00293
683024 104539 17 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 104539 17 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
155560153 348981 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 348981 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
683024 104539 17 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 104539 17 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
155560153 348981 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 348981 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
45501061 312692 12 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 312692 12 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
155552304 348107 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 5 3.3 CCOC(=O)N1CCC2(CC(N3CCC(c4ncccc4OC)CC3)C2)C1 10.1021/acsmedchemlett.9b00106
CHEMBL4543638 348107 0 None None None Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 5 3.3 CCOC(=O)N1CCC2(CC(N3CCC(c4ncccc4OC)CC3)C2)C1 10.1021/acsmedchemlett.9b00106
302 6062 14 None 1 6 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
4630 6062 14 None 1 6 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
CHEMBL7634 6062 14 None 1 6 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
44589681 368585 0 None 1 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 368585 0 None 1 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 370315 1 None -4 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 370315 1 None -4 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
156246208 389325 4 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 402 4 0 4 3.0 COc1cc(F)ccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5436967 389325 4 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Activation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M4 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 402 4 0 4 3.0 COc1cc(F)ccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
134263768 366500 10 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4795177 366500 10 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
162674698 366635 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 423 3 2 8 2.3 Cc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4796921 366635 0 None 12 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 423 3 2 8 2.3 Cc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
137646585 313883 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4085356 313883 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
178301679 466630 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 393 3 2 6 4.3 Cc1nnc2sc(C(=O)Nc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1021/acs.jmedchem.5c00678
CHEMBL6150651 466630 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 393 3 2 6 4.3 Cc1nnc2sc(C(=O)Nc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1021/acs.jmedchem.5c00678
12301 8771 38 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
73774630 8771 38 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
CHEMBL3915634 8771 38 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
89777151 314443 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 314443 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020012 352020 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647876 352020 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
137635723 312008 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 312008 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777151 314443 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 314443 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5074747 478531 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 378 4 2 6 4.7 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
137653737 314561 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4093138 314561 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
137646585 313883 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4085356 313883 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
53382541 177187 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313373 177187 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
73672762 221512 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289440 221512 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
137645044 313984 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086665 313984 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137657309 315449 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4103312 315449 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
53382541 177187 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313373 177187 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145963925 329273 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212428 329273 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137645044 313984 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086665 313984 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
145963925 329273 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212428 329273 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137657309 315449 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4103312 315449 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
156009865 351064 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 439 4 1 6 3.3 COc1cc(N2CC(NC(=O)c3ccc4nc(C(F)(F)F)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4633549 351064 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 439 4 1 6 3.3 COc1cc(N2CC(NC(=O)c3ccc4nc(C(F)(F)F)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
45142486 105586 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.5c00678
CHEMBL1589763 105586 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysisAgonist activity at human recombinant M4 muscarinic acetylcholine receptor assessed as calcium mobilization by FLIPR analysis
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.5c00678
155547285 347714 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4ncnn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4533756 347714 0 None None None Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4ncnn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
45142486 105586 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 nan
CHEMBL1589763 105586 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 nan
127044078 277662 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 277662 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
55661332 277741 6 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809378 277741 6 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156010835 351044 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 416 5 2 6 4.2 Cc1c2c(ccc3c(NCc4ccc(C(=O)NCC(C)(C)C)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4633191 351044 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 416 5 2 6 4.2 Cc1c2c(ccc3c(NCc4ccc(C(=O)NCC(C)(C)C)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
55661332 277741 6 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809378 277741 6 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145975851 328697 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4205221 328697 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127044539 277706 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808983 277706 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127044539 277706 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808983 277706 0 None None None Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145975851 328697 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4205221 328697 0 None None None Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155561871 349805 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3cncc(C)n3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4584879 349805 0 None None None Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3cncc(C)n3)CC2)CC1 10.1021/acsmedchemlett.9b00106
44626302 101402 0 None None None Rat 7.0 pEC50 = 7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 434 7 2 7 4.1 COc1ccc(CNC(=O)c2sc3nc(OCc4ccncc4)cc(C)c3c2N)cc1 nan
CHEMBL1551487 101402 0 None None None Rat 7.0 pEC50 = 7 Functional
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 434 7 2 7 4.1 COc1ccc(CNC(=O)c2sc3nc(OCc4ccncc4)cc(C)c3c2N)cc1 nan
155531483 336210 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 469 4 2 8 3.1 Cc1cc2nncn2c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4466365 336210 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 469 4 2 8 3.1 Cc1cc2nncn2c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
89777513 312111 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
CHEMBL4064060 312111 0 None None None Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
2551 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5831 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 1644 11 None -1 5 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
9795428 196826 4 None -1 5 Human 7.3 pED50 = 7.3 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 196826 4 None -1 5 Human 7.3 pED50 = 7.3 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
5487543 461855 2 None -2 5 Human 7.0 pED50 = 7.0 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 461855 2 None -2 5 Human 7.0 pED50 = 7.0 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
138578326 369503 0 None 870 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 369503 0 None 870 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 369503 0 None 870 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 369503 0 None 870 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 369503 0 None 870 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 369503 0 None 870 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 369503 0 None 870 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 369503 0 None 870 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
156493644 368365 0 None 1737 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4855467 368365 0 None 1737 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
156493644 368365 0 None 1737 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4855467 368365 0 None 1737 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
138578970 368955 0 None 1862 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4864914 368955 0 None 1862 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578970 368955 0 None 1862 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4864914 368955 0 None 1862 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578683 368112 0 None 1318 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccccc1-c1ccc(N[C@H]2C[C@@H]3CN(CC4CCOCC4)C[C@@H]3C2)nn1 10.1021/acsmedchemlett.1c00363
CHEMBL4851711 368112 0 None 1318 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccccc1-c1ccc(N[C@H]2C[C@@H]3CN(CC4CCOCC4)C[C@@H]3C2)nn1 10.1021/acsmedchemlett.1c00363
137408729 373823 0 None 870 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5182783 373823 0 None 870 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137408729 373823 0 None 870 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5182783 373823 0 None 870 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137637944 311745 0 None 2 5 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4059829 311745 0 None 2 5 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
52176747 314886 0 None -2 8 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat muscarinic M4 receptor by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 314886 0 None -2 8 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat muscarinic M4 receptor by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137634235 312569 0 None None None Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4069356 312569 0 None None None Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
156015807 352214 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 352214 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
137634235 312569 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4069356 312569 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137638270 312793 0 None 2 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 312793 0 None 2 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
9815331 468153 1 None 4 3 Rat 8.0 pIC50 = 8.0 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 468153 1 None 4 3 Rat 8.0 pIC50 = 8.0 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
152072967 375273 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 375273 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137641287 312958 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4073915 312958 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658248 315462 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4103428 315462 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137641287 312958 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4073915 312958 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
152072967 375273 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 375273 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
9913341 163586 3 None -28 2 Human 7.9 pIC50 = 7.9 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 163586 3 None -28 2 Human 7.9 pIC50 = 7.9 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137638270 312793 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 312793 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
168279172 373974 0 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5185022 373974 0 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137655063 314828 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096143 314828 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168279172 373974 0 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5185022 373974 0 None None None Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
168289751 374863 0 None 47 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
CHEMBL5198423 374863 0 None 47 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
44418764 163587 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 163587 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
121053110 314377 1 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4091144 314377 1 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
121053110 314377 1 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4091144 314377 1 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137655063 314828 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096143 314828 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168289751 374863 0 None 47 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
CHEMBL5198423 374863 0 None 47 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
137647734 313732 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4083681 313732 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137660952 315192 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 443 4 0 6 3.3 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2017.05.042
CHEMBL4100202 315192 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 443 4 0 6 3.3 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2017.05.042
137655354 314505 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 444 4 0 7 2.7 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nc1 10.1016/j.bmcl.2017.05.042
CHEMBL4092457 314505 0 None None None Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 444 4 0 7 2.7 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nc1 10.1016/j.bmcl.2017.05.042
156016041 352162 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650627 352162 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
71451570 163376 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)[C@@](F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
CHEMBL2164905 163376 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)[C@@](F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
137647734 313732 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4083681 313732 0 None 2 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137658248 315462 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4103428 315462 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
127045035 277699 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 6 0 6 5.3 CCCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
CHEMBL3808906 277699 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 6 0 6 5.3 CCCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
46830362 22211 0 None -3 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090097 22211 0 None -3 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
11584660 184062 7 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 184062 7 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
137641843 314139 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4088672 314139 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
137641843 314139 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4088672 314139 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658023 315549 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4104456 315549 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137408799 374014 0 None 12 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5185664 374014 0 None 12 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
2986945 195432 5 None -16 5 Rat 4.8 pIC50 = 4.8 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255169 195432 5 None -16 5 Rat 4.8 pIC50 = 4.8 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
152278786 366136 1 None -12 4 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 366136 1 None -12 4 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
137658023 315549 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4104456 315549 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137649829 313319 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078634 313319 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
156493565 368290 0 None 1318 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4854289 368290 0 None 1318 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
156493565 368290 0 None 1318 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4854289 368290 0 None 1318 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578253 369723 0 None 1230 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4876599 369723 0 None 1230 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
138578253 369723 0 None 1230 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4876599 369723 0 None 1230 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
137649829 313319 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078634 313319 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
44455159 198068 0 None -17 5 Rat 4.7 pIC50 = 4.7 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271704 198068 0 None -17 5 Rat 4.7 pIC50 = 4.7 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
152278786 366136 1 None -12 4 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 366136 1 None -12 4 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
137408799 374014 0 None -12 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5185664 374014 0 None -12 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137655902 314684 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4094531 314684 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137639216 312625 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4070135 312625 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
2551 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
5831 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 1644 11 None -2 8 Rat 6.6 pIC50 = 6.6 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
137639216 312625 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4070135 312625 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137647376 313487 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4080796 313487 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647376 313487 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4080796 313487 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137635985 312003 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
CHEMBL4062851 312003 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
137655902 314684 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4094531 314684 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
127045185 277701 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 395 5 0 6 4.9 CCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
CHEMBL3808947 277701 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 395 5 0 6 4.9 CCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
137635985 312003 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
CHEMBL4062851 312003 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
3652 8876 57 None -3 5 Human 7.6 pIC50 = 7.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 8876 57 None -3 5 Human 7.6 pIC50 = 7.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 8876 57 None -3 5 Human 7.6 pIC50 = 7.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 8876 57 None -3 5 Human 7.6 pIC50 = 7.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 8876 57 None -3 5 Human 7.6 pIC50 = 7.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
162646559 353528 0 None -19 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4742997 353528 0 None -19 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
10109893 163593 0 None -3162 2 Human 4.6 pIC50 = 4.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 163593 0 None -3162 2 Human 4.6 pIC50 = 4.6 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
137659030 315076 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4098838 315076 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137659030 315076 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4098838 315076 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658151 315542 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4104377 315542 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
137654928 314569 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4093252 314569 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137655967 314879 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
CHEMBL4096649 314879 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
137648504 313894 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4085498 313894 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137408797 373536 0 None 18 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 373536 0 None 18 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137654928 314569 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4093252 314569 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648504 313894 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4085498 313894 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137658151 315542 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4104377 315542 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
168294040 375228 0 None None None Human 6.6 pIC50 = 6.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5204478 375228 0 None None None Human 6.6 pIC50 = 6.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137408797 373536 0 None 18 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 373536 0 None 18 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168294040 375228 0 None None None Human 6.6 pIC50 = 6.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5204478 375228 0 None None None Human 6.6 pIC50 = 6.6 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137655967 314879 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
CHEMBL4096649 314879 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
137661476 315301 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4101349 315301 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137644574 313968 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4086480 313968 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
142611618 374261 0 None None None Human 5.5 pIC50 = 5.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5189221 374261 0 None None None Human 5.5 pIC50 = 5.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
137661476 315301 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4101349 315301 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137644574 313968 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4086480 313968 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
142611618 374261 0 None None None Human 5.5 pIC50 = 5.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5189221 374261 0 None None None Human 5.5 pIC50 = 5.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
137636810 311843 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4060844 311843 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648177 313718 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4083448 313718 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137636810 311843 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4060844 311843 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648177 313718 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4083448 313718 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
53303986 156016 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024407 156016 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
137654353 314871 0 None 1 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 314871 0 None 1 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168276820 373203 0 None 63 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 373203 0 None 63 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168276820 373203 0 None 63 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 373203 0 None 63 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137641912 314257 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4089875 314257 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137641912 314257 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4089875 314257 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137654353 314871 0 None 1 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 314871 0 None 1 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
49663949 313913 8 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 313913 8 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
156015978 352238 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 352238 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
46883796 22210 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090096 22210 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
46830363 22335 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090759 22335 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
1421986 22581 2 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 357 4 1 3 4.0 CCN1CCN(c2ccc(NC(=O)c3ccc(C)cc3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092461 22581 2 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 357 4 1 3 4.0 CCN1CCN(c2ccc(NC(=O)c3ccc(C)cc3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
49663949 313913 8 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 313913 8 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
162657046 354711 0 None -6 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4757103 354711 0 None -6 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
16094788 279100 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 279100 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137634274 312428 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4067738 312428 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
164606754 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 368011 17 None 33 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
137634274 312428 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4067738 312428 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
121053122 313710 1 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4083366 313710 1 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647522 313821 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4084528 313821 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
168276820 373203 0 None 63 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 373203 0 None 63 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137647522 313821 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4084528 313821 0 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
168276820 373203 0 None 63 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 373203 0 None 63 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
52176747 314886 0 None 2 8 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 314886 0 None 2 8 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
121053122 313710 1 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4083366 313710 1 None None None Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
52176747 314886 0 None 2 8 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 314886 0 None 2 8 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137636570 311814 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4060501 311814 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
137635323 312070 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4063633 312070 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137636570 311814 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4060501 311814 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
9308 41623 17 None 2 4 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 41623 17 None 2 4 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
137654353 314871 0 None -1 6 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 314871 0 None -1 6 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
10092649 385614 38 None 1 10 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 385614 38 None 1 10 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
10092649 385614 38 None 1 10 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 385614 38 None 1 10 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
1201549 1234 18 None -6 18 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
333 1234 18 None -6 18 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
7601 1234 18 None -6 18 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL1201203 1234 18 None -6 18 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
DB00245 1234 18 None -6 18 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
138578974 367907 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4848896 367907 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578974 367907 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4848896 367907 0 None None None Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
2551 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
5831 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 1644 11 None 1 8 Human 7.3 pIC50 = 7.3 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
137635323 312070 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4063633 312070 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137659754 315109 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4099192 315109 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168272462 373260 0 None 51 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5173887 373260 0 None 51 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137659754 315109 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4099192 315109 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
2066745 195626 6 None -10 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 337 7 1 3 4.0 CCCCCC(=O)Nc1ccc(N2CCN(CC)CC2)c(Cl)c1 10.1016/j.bmcl.2007.12.051
CHEMBL256202 195626 6 None -10 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 337 7 1 3 4.0 CCCCCC(=O)Nc1ccc(N2CCN(CC)CC2)c(Cl)c1 10.1016/j.bmcl.2007.12.051
71718588 177438 0 None -1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315675 177438 0 None -1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
168272462 373260 0 None 51 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5173887 373260 0 None 51 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137637971 311807 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4060443 311807 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
71718588 177438 0 None -1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315675 177438 0 None -1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
137637971 311807 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4060443 311807 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
49671356 313325 11 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 313325 11 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408797 373536 0 None -18 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 373536 0 None -18 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168292831 375135 0 None None None Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5203077 375135 0 None None None Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
49671356 313325 11 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 313325 11 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408797 373536 0 None -18 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 373536 0 None -18 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
121053081 311922 1 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4061815 311922 1 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
168292831 375135 0 None None None Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5203077 375135 0 None None None Human 7.3 pIC50 = 7.3 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
121053081 311922 1 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4061815 311922 1 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137654353 314871 0 None -1 6 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 314871 0 None -1 6 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
49663949 313913 8 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 313913 8 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137640923 312986 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
CHEMBL4074229 312986 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
52176746 313698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4083307 313698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137640923 312986 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
CHEMBL4074229 312986 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
49663949 313913 8 None -1 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 313913 8 None -1 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
52176746 313698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4083307 313698 0 None None None Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
49663929 311915 10 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4061637 311915 10 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
16094793 164733 0 None None None Human 5.2 pIC50 = 5.2 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 164733 0 None None None Human 5.2 pIC50 = 5.2 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
49663929 311915 10 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4061637 311915 10 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137636004 312043 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4063271 312043 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
952858 198031 2 None -20 3 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 343 4 1 3 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271519 198031 2 None -20 3 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 343 4 1 3 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL4519018 478300 7 None -3 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
ChEMBL 308 2 1 2 3.9 CN1C2CCCC1CC(Nc1ccccc1Br)C2 10.1021/acs.jmedchem.2c01562
25070582 124212 27 None -4 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 124212 27 None -4 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
137639344 312820 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4072231 312820 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
156493614 368691 0 None 338 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4860985 368691 0 None 338 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
164621386 369003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
CHEMBL4865665 369003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
156493614 368691 0 None 338 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4860985 368691 0 None 338 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
164621386 369003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
CHEMBL4865665 369003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
137408738 374297 3 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 374297 3 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
1726 5075 9 None 2 4 Rat 6.2 pIC50 = 6.2 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 5075 9 None 2 4 Rat 6.2 pIC50 = 6.2 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 5075 9 None 2 4 Rat 6.2 pIC50 = 6.2 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 5075 9 None 2 4 Rat 6.2 pIC50 = 6.2 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 5075 9 None 2 4 Rat 6.2 pIC50 = 6.2 Functional
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
137642171 314369 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4091095 314369 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408738 374297 3 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 374297 3 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137639344 312820 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4072231 312820 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168296286 375404 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
CHEMBL5207446 375404 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
168296286 375404 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
CHEMBL5207446 375404 0 None None None Human 7.1 pIC50 = 7.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
142562194 374719 0 None None None Human 6.1 pIC50 = 6.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5196196 374719 0 None None None Human 6.1 pIC50 = 6.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
137636004 312043 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4063271 312043 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
142562194 374719 0 None None None Human 6.1 pIC50 = 6.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5196196 374719 0 None None None Human 6.1 pIC50 = 6.1 Functional
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
10092649 385614 38 None -1 10 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 385614 38 None -1 10 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
10092649 385614 38 None -1 10 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 385614 38 None -1 10 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
137642171 314369 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4091095 314369 0 None None None Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137642731 314095 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4088103 314095 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
2067745 197847 2 None -13 2 Rat 5.1 pIC50 = 5.1 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 415 8 1 4 4.9 CCCCOc1cccc(C(=O)Nc2ccc(N3CCN(CC)CC3)c(Cl)c2)c1 10.1016/j.bmcl.2007.12.051
CHEMBL270580 197847 2 None -13 2 Rat 5.1 pIC50 = 5.1 Functional
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 415 8 1 4 4.9 CCCCOc1cccc(C(=O)Nc2ccc(N3CCN(CC)CC3)c(Cl)c2)c1 10.1016/j.bmcl.2007.12.051
16094791 164669 0 None -2 2 Human 5.1 pIC50 = 5.1 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 164669 0 None -2 2 Human 5.1 pIC50 = 5.1 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
16094783 273997 0 None -100 2 Human 5.1 pIC50 = 5.1 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 273997 0 None -100 2 Human 5.1 pIC50 = 5.1 Functional
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137642731 314095 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4088103 314095 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
152072967 375273 0 None -6 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 375273 0 None -6 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
152072967 375273 0 None -6 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 375273 0 None -6 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137653550 314678 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4094472 314678 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
156015153 352222 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651018 352222 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
137653550 314678 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4094472 314678 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647679 313636 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4082397 313636 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
137647679 313636 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4082397 313636 0 None None None Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
324 3939 17 None None None Mouse 8.0 pKd = 8.0 Functional
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
6436265 3939 17 None None None Mouse 8.0 pKd = 8.0 Functional
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
CHEMBL277642 3939 17 None None None Mouse 8.0 pKd = 8.0 Functional
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
324 3939 17 None None None Rat 8.3 pKd = 8.3 Functional
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
6436265 3939 17 None None None Rat 8.3 pKd = 8.3 Functional
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
CHEMBL277642 3939 17 None None None Rat 8.3 pKd = 8.3 Functional
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/S0960-894X(00)80534-X
1757 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
23724781 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
71183 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
CHEMBL1354199 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
CHEMBL376897 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
DB00462 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
DB11315 270505 11 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
1979 155056 51 None 1 6 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
4314 155056 51 None 1 6 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 155056 51 None 1 6 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
DB13262 155056 51 None 1 6 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
2684 1823 20 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
584 1823 20 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
9658 1823 20 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
CHEMBL168815 1823 20 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
DB00185 1823 20 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2166 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
305 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
5910 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
91468 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
CHEMBL550 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
CHEMBL91776 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
DB01085 6354 42 None -3 6 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
135398737 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2818 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL253391 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 1973 61 None -18 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2551 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
298 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
488 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
5831 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
CHEMBL965 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
DB00411 1644 11 None -5 9 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
306 7028 17 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
3536 7028 17 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
9577995 7028 17 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
CHEMBL134641 7028 17 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
13626 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
140830653 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
CHEMBL5314557 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
DB18706 3199 32 None 3 3 Human 7.9 pEC50 = 7.9 Functional
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
12301 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
12301 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 26508634
12301 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 37248726
73774630 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
73774630 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 26508634
73774630 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 37248726
CHEMBL3915634 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
CHEMBL3915634 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 26508634
CHEMBL3915634 8771 38 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 37248726
1541501 8725 30 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
3256 8725 30 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
CHEMBL4461667 8725 30 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
3263 8727 47 None -2 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
864492 8727 47 None -2 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
CHEMBL1978713 8727 47 None -2 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
12301 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
73774630 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
CHEMBL3915634 8771 38 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
1273944 518 16 None -7 5 Human 4.8 pEC50 None 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
288 518 16 None -7 5 Human 4.8 pEC50 None 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
6979053 518 16 None -7 5 Human 4.8 pEC50 None 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
CHEMBL612034 518 16 None -7 5 Human 4.8 pEC50 None 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
286 517 6 None -7 5 Human 5.4 pEC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
6954180 517 6 None -7 5 Human 5.4 pEC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
909982 517 6 None -7 5 Human 5.4 pEC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
CHEMBL608828 517 6 None -7 5 Human 5.4 pEC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
11536903 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
11536903 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919
11536903 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 37248726
3262 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
3262 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919
3262 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 37248726
CHEMBL3770346 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
CHEMBL3770346 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919
CHEMBL3770346 4875 52 None None None Human 5.2 pKB = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 37248726


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
5487426 135875 7 None None None Human 9.5 pAC50 = 9.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1038/s41467-023-40064-9
5487427 135875 7 None None None Human 9.5 pAC50 = 9.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1038/s41467-023-40064-9
5487429 135875 7 None None None Human 9.5 pAC50 = 9.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1038/s41467-023-40064-9
CHEMBL1900528 135875 7 None None None Human 9.5 pAC50 = 9.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1038/s41467-023-40064-9
DB01409 135875 7 None None None Human 9.5 pAC50 = 9.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1038/s41467-023-40064-9
3494 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 3732 12 None None None Human 9.0 pAC50 = 9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
1475 116491 8 None None None Human 8.9 pAC50 = 8.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657308 116491 8 None None None Human 8.9 pAC50 = 8.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657309 116491 8 None None None Human 8.9 pAC50 = 8.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1621597 116491 8 None None None Human 8.9 pAC50 = 8.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00332 116491 8 None None None Human 8.9 pAC50 = 8.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
1427 4113 43 None None None Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 4113 43 None None None Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 4113 43 None None None Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 4113 43 None None None Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 4113 43 None None None Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3180 38385 30 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 38385 30 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
DB00645 38385 30 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
2284 6466 25 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 6466 25 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 6466 25 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 6466 25 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 6466 25 None None None Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
135398745 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1982 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
4585 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 5933 69 None None None Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
10660 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
1224 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
441281 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1200406 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB00985 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB13636 2953 69 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2068 370177 47 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
43815 370177 47 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 370177 47 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
DB00715 370177 47 None None None Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
1613 4786 46 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 4786 46 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 4786 46 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 4786 46 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 4786 46 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2784 7898 8 None None None Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
351 7898 8 None None None Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
676 7898 8 None None None Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL620 7898 8 None None None Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
3158 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
667468 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
956 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL101740 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB14750 18465 32 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1971 5840 38 None None None Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 5840 38 None None None Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 5840 38 None None None Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 5840 38 None None None Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 5840 38 None None None Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
191 833 62 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 833 62 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 833 62 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 833 62 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 833 62 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
72713421 202603 0 None None None Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL3040619 202603 0 None None None Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
171351370 386895 0 None None None Human 7.0 pEC50 = 7 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
CHEMBL5288291 386895 0 None None None Human 7.0 pEC50 = 7 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
171351370 386895 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
CHEMBL5288291 386895 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
44176134 202602 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 202602 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
44176134 202602 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 202602 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
132254931 408477 0 None None None Rat 7.0 pEC50 = 7.0 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 285 2 1 6 3.2 Cc1nnc2sc3c(NC4CCC4)ncnc3c2c1C nan
CHEMBL5775811 408477 0 None None None Rat 7.0 pEC50 = 7.0 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 285 2 1 6 3.2 Cc1nnc2sc3c(NC4CCC4)ncnc3c2c1C nan
156016090 351625 0 None None None Rat 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4641848 351625 0 None None None Rat 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
132254489 447268 0 None None None Rat 5.9 pEC50 = 5.9 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 298 1 0 6 2.4 Cc1cnc2sc3c(N4CC5(COC5)C4)ncnc3c2c1 nan
CHEMBL5981563 447268 0 None None None Rat 5.9 pEC50 = 5.9 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 298 1 0 6 2.4 Cc1cnc2sc3c(N4CC5(COC5)C4)ncnc3c2c1 nan
44176127 202589 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 202589 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
3263 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
89777266 294600 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
CHEMBL3933538 294600 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
156013904 351191 0 None None None Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635732 351191 0 None None None Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
2230 961 44 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
296 961 44 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
CHEMBL7303 961 44 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
DB04365 961 44 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
3263 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 8727 47 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
44176127 202589 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 202589 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
44176132 202599 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 202599 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
89777266 294600 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
CHEMBL3933538 294600 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
44176132 202599 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 202599 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
171345098 387096 0 None None None Human 5.9 pEC50 = 5.9 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
171348452 387096 0 None None None Human 5.9 pEC50 = 5.9 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315302 387096 0 None None None Human 5.9 pEC50 = 5.9 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315497 387096 0 None None None Human 5.9 pEC50 = 5.9 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
187 524 25 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
294 524 25 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
65 524 25 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
CHEMBL667 524 25 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
DB03128 524 25 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
72713420 202585 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 202585 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
72713420 202585 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 202585 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
89777094 386111 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269733 386111 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777094 386111 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269733 386111 0 None None None Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
53382542 177191 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 177191 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640201 312873 2 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 312873 2 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
53382542 177191 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 177191 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
2166 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
305 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
91468 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL550 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL91776 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
DB01085 6354 42 None None None Human 4.8 pEC50 = 4.8 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
156015762 351490 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4640254 351490 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
89777266 294600 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3933538 294600 0 None None None Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
2551 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
5831 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 1644 11 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
156020012 352020 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647876 352020 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
3652 8876 57 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 8876 57 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 8876 57 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 8876 57 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 8876 57 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
156013280 351439 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4639387 351439 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156016660 351647 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642156 351647 0 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
137374255 386864 3 None None None Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human muscarinic M4 receptor in presence of EC20 concentration of acetylcholine by FLIPR assayPositive allosteric modulation of human muscarinic M4 receptor in presence of EC20 concentration of acetylcholine by FLIPR assay
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1021/acs.jmedchem.4c00293
CHEMBL5287400 386864 3 None None None Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human muscarinic M4 receptor in presence of EC20 concentration of acetylcholine by FLIPR assayPositive allosteric modulation of human muscarinic M4 receptor in presence of EC20 concentration of acetylcholine by FLIPR assay
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1021/acs.jmedchem.4c00293
53382523 157721 8 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 157721 8 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382523 157721 8 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 157721 8 None None None Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
118719922 234710 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None None None Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
156014219 351199 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4635909 351199 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
132254738 407086 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 348 2 0 7 3.3 Cc1nnc2sc3c(N4CC(c5ccncc5)C4)ncnc3c2c1C nan
CHEMBL5762026 407086 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 348 2 0 7 3.3 Cc1nnc2sc3c(N4CC(c5ccncc5)C4)ncnc3c2c1C nan
3652 8876 57 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 8876 57 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 8876 57 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 8876 57 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 8876 57 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
118719926 234715 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 234715 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
132254815 406027 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 299 1 0 6 3.2 Cc1nnc2sc3c(N4CCCCC4)ncnc3c2c1C nan
CHEMBL5751084 406027 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 299 1 0 6 3.2 Cc1nnc2sc3c(N4CCCCC4)ncnc3c2c1C nan
16757565 39177 0 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 39177 0 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
16757565 39177 0 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 39177 0 None None None Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
2551 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
298 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
488 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
5831 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL965 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
DB00411 1644 11 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
156013839 351127 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4634770 351127 0 None None None Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
2551 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
5831 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 1644 11 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
132254659 412729 2 None None None Rat 7.6 pEC50 = 7.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 379 4 2 7 4.1 Cc1nnc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c1C nan
CHEMBL5822149 412729 2 None None None Rat 7.6 pEC50 = 7.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 379 4 2 7 4.1 Cc1nnc2sc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c2c1C nan
3263 8727 47 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
864492 8727 47 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL1978713 8727 47 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
132255015 429752 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 313 1 0 7 2.1 Cc1nnc2sc3c(N4CC5(COC5)C4)ncnc3c2c1C nan
CHEMBL5900876 429752 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 313 1 0 7 2.1 Cc1nnc2sc3c(N4CC5(COC5)C4)ncnc3c2c1C nan
156018661 351765 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4644004 351765 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156022087 352115 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4649459 352115 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
89777136 386036 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
CHEMBL5267403 386036 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
72713423 202591 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL3040500 202591 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
89777136 386036 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
CHEMBL5267403 386036 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
10442081 202670 5 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 202670 5 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
72713423 202591 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL3040500 202591 0 None None None Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
45142486 105586 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
CHEMBL1589763 105586 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
132254550 407265 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 256 1 0 5 2.8 Cc1cnc2sc3c(N4CCC4)ncnc3c2c1 nan
CHEMBL5763754 407265 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 256 1 0 5 2.8 Cc1cnc2sc3c(N4CCC4)ncnc3c2c1 nan
156016190 351639 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642055 351639 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
45501061 312692 12 None None None Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 312692 12 None None None Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
156010562 351000 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632555 351000 0 None None None Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
89777239 328915 33 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 328915 33 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
171346988 387102 0 None None None Human 5.6 pEC50 = 5.6 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 560 13 1 4 4.5 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[n+]1c[nH]c(CC2COC(=O)C2)c1 10.1021/acs.jnatprod.2c01079
CHEMBL5315392 387102 0 None None None Human 5.6 pEC50 = 5.6 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 560 13 1 4 4.5 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[n+]1c[nH]c(CC2COC(=O)C2)c1 10.1021/acs.jnatprod.2c01079
10236758 234707 4 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
134263768 366500 10 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of rat M4 receptorPositive allosteric modulation of rat M4 receptor
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4795177 366500 10 None None None Rat 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of rat M4 receptorPositive allosteric modulation of rat M4 receptor
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
132254853 409555 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 404 3 1 9 2.7 FC(F)(F)c1cnc(N2CC(Nc3ncnc4c3sc3nccnc34)C2)nc1 nan
CHEMBL5787035 409555 0 None None None Rat 5.6 pEC50 = 5.6 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 404 3 1 9 2.7 FC(F)(F)c1cnc(N2CC(Nc3ncnc4c3sc3nccnc34)C2)nc1 nan
90005322 336446 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 429 4 2 6 3.4 Cc1cncc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4469998 336446 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 429 4 2 6 3.4 Cc1cncc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
156014184 351149 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4635170 351149 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
132254706 428939 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 432 3 1 9 3.4 Cc1nnc2sc3c(NC4CN(c5ncc(C(F)(F)F)cn5)C4)ncnc3c2c1C nan
CHEMBL5892828 428939 0 None None None Rat 7.5 pEC50 = 7.5 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 432 3 1 9 3.4 Cc1nnc2sc3c(NC4CN(c5ncc(C(F)(F)F)cn5)C4)ncnc3c2c1C nan
10261985 468914 0 None None None Human 7.5 pEC50 = 7.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 468914 0 None None None Human 7.5 pEC50 = 7.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
118719921 234709 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
72713214 202588 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL3040488 202588 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
72713214 202588 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL3040488 202588 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
156012754 351263 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636845 351263 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
132254726 427090 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 328 2 0 7 2.4 Cc1nnc2sc3c(N4CCC(N(C)C)C4)ncnc3c2c1C nan
CHEMBL5872052 427090 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 328 2 0 7 2.4 Cc1nnc2sc3c(N4CCC(N(C)C)C4)ncnc3c2c1C nan
302 6062 14 None None None Human 7.5 pEC50 = 7.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 6062 14 None None None Human 7.5 pEC50 = 7.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 6062 14 None None None Human 7.5 pEC50 = 7.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
156014638 351177 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4635575 351177 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
2166 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
305 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
91468 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL550 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL91776 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
DB01085 6354 42 None None None Human 5.5 pEC50 = 5.5 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
156012624 351368 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4638506 351368 0 None None None Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
72713422 202596 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL3040554 202596 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
118719922 234710 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
72713422 202596 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL3040554 202596 0 None None None Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
132254590 448139 0 None None None Rat 7.4 pEC50 = 7.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 297 1 0 6 2.7 Cc1nnc2sc3c(N4CC5CC5C4)ncnc3c2c1C nan
CHEMBL5990773 448139 0 None None None Rat 7.4 pEC50 = 7.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 297 1 0 6 2.7 Cc1nnc2sc3c(N4CC5CC5C4)ncnc3c2c1C nan
171344042 387090 0 None None None Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 574 13 0 5 4.5 Cn1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cc1CC1COC(=O)C1 10.1021/acs.jnatprod.2c01079
CHEMBL5315256 387090 0 None None None Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 574 13 0 5 4.5 Cn1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cc1CC1COC(=O)C1 10.1021/acs.jnatprod.2c01079
156011257 351280 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4637175 351280 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
1541501 8725 30 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
3256 8725 30 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
CHEMBL4461667 8725 30 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
132254477 424760 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 271 1 0 6 2.5 Cc1nnc2sc3c(N4CCC4)ncnc3c2c1C nan
CHEMBL5846615 424760 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 271 1 0 6 2.5 Cc1nnc2sc3c(N4CCC4)ncnc3c2c1C nan
171356531 386390 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5276239 386390 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
171356531 386390 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5276239 386390 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
156011081 351023 0 None None None Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632962 351023 0 None None None Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
132254607 405296 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 417 3 1 8 3.7 Cc1cnc2sc3c(NC4CN(c5ncc(C(F)(F)F)cn5)C4)ncnc3c2c1 nan
CHEMBL5744259 405296 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 417 3 1 8 3.7 Cc1cnc2sc3c(NC4CN(c5ncc(C(F)(F)F)cn5)C4)ncnc3c2c1 nan
171343599 386119 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269998 386119 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
171343599 386119 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269998 386119 0 None None None Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
156014224 351209 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4636061 351209 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
137647620 313494 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 313494 0 None None None Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
2551 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
298 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
488 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
5831 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL965 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
DB00411 1644 11 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
171350960 385968 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5265850 385968 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
171350960 385968 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5265850 385968 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
3263 8727 47 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
864492 8727 47 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
CHEMBL1978713 8727 47 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
132254498 447062 0 None None None Rat 6.3 pEC50 = 6.3 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 315 2 1 7 2.8 Cc1nnc2sc3c(NC4CCOCC4)ncnc3c2c1C nan
CHEMBL5979494 447062 0 None None None Rat 6.3 pEC50 = 6.3 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 315 2 1 7 2.8 Cc1nnc2sc3c(NC4CCOCC4)ncnc3c2c1C nan
171345098 387096 0 None None None Human 6.3 pEC50 = 6.3 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
171348452 387096 0 None None None Human 6.3 pEC50 = 6.3 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315302 387096 0 None None None Human 6.3 pEC50 = 6.3 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315497 387096 0 None None None Human 6.3 pEC50 = 6.3 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
89777239 328915 33 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 328915 33 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
72713209 202601 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL3040603 202601 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
72713209 202601 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL3040603 202601 0 None None None Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
72713419 202595 0 None None None Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL3040531 202595 0 None None None Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
72713419 202595 0 None None None Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL3040531 202595 0 None None None Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
14925759 313920 6 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 313920 6 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
89777307 386662 4 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5282936 386662 4 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
89777307 386662 4 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5282936 386662 4 None None None Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
3652 8876 57 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 8876 57 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 8876 57 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 8876 57 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 8876 57 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
2551 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
5831 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 1644 11 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
101882890 234711 0 None None None Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 234711 0 None None None Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10442337 468913 1 None None None Human 7.2 pEC50 = 7.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 468913 1 None None None Human 7.2 pEC50 = 7.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
132254906 449293 0 None None None Rat 6.2 pEC50 = 6.2 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 340 2 0 7 2.5 Cc1nnc2sc3c(N4CCN(C5CC5)CC4)ncnc3c2c1C nan
CHEMBL6003033 449293 0 None None None Rat 6.2 pEC50 = 6.2 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 340 2 0 7 2.5 Cc1nnc2sc3c(N4CCN(C5CC5)CC4)ncnc3c2c1C nan
118719921 234709 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None None None Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
156011921 351348 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638291 351348 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010821 351018 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
CHEMBL4632855 351018 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
132254989 431762 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 259 1 0 6 2.3 Cc1nnc2sc3c(N(C)C)ncnc3c2c1C nan
CHEMBL5920998 431762 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 259 1 0 6 2.3 Cc1nnc2sc3c(N(C)C)ncnc3c2c1C nan
171347905 386244 0 None None None Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 166 2 1 3 0.5 O=C1C[C@@H](Cc2cnc[nH]2)CO1 10.1021/acs.jnatprod.2c01079
CHEMBL5272950 386244 0 None None None Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 166 2 1 3 0.5 O=C1C[C@@H](Cc2cnc[nH]2)CO1 10.1021/acs.jnatprod.2c01079
132255048 425467 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 285 1 0 6 2.9 Cc1nnc2sc3c(N4CCCC4)ncnc3c2c1C nan
CHEMBL5854191 425467 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 285 1 0 6 2.9 Cc1nnc2sc3c(N4CCCC4)ncnc3c2c1C nan
2551 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
298 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
488 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
5831 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
CHEMBL965 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
DB00411 1644 11 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
89777239 328915 33 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 328915 33 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 328915 33 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
156013272 351432 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4639222 351432 0 None None None Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
132254612 432876 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 313 2 1 6 4.0 Cc1nnc2sc3c(NC4CCCCC4)ncnc3c2c1C nan
CHEMBL5931985 432876 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 313 2 1 6 4.0 Cc1nnc2sc3c(NC4CCCCC4)ncnc3c2c1C nan
89777311 386758 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5285036 386758 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777311 386758 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5285036 386758 0 None None None Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
132254982 451045 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 315 3 0 7 2.3 COCC1CN(c2ncnc3c2sc2nnc(C)c(C)c23)C1 nan
CHEMBL6021481 451045 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 315 3 0 7 2.3 COCC1CN(c2ncnc3c2sc2nnc(C)c(C)c23)C1 nan
89777242 386232 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
CHEMBL5272517 386232 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
45142486 105586 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
CHEMBL1589763 105586 0 None None None Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
89777242 386232 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
CHEMBL5272517 386232 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
132254903 426636 0 None None None Rat 6.0 pEC50 = 6.0 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 303 4 0 7 2.3 COCCN(C)c1ncnc2c1sc1nnc(C)c(C)c12 nan
CHEMBL5866929 426636 0 None None None Rat 6.0 pEC50 = 6.0 Binding
Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).Cell-Based Functional Assay of Muscarinic Acetylcholine Receptor Activity: For high throughput measurement of agonist-evoked increases in intracellular calcium, CHO-K1 cells stably expressing muscarinic receptors were plated in growth medium lacking G418 and hygromycin at 15,000 cells/20 μL/well in Greiner 384-well black-walled, tissue culture (TC)-treated, clear-bottom plates (VWR). Cells were incubated overnight at 37° C. and 5% CO2. The next day, cells were washed using an ELX 405 (BioTek) with assay buffer; the final volume was then aspirated to 20 μL. Next, 20 μL of a 2.3 M stock of Fluo-4/acetoxymethyl ester (Invitrogen, Carlsbad, Calif.), prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) Pluronic F-127 and diluted in assay buffer, was added to the wells and the cell plates were incubated for 50 min at 37° C. and 5% CO2. Dye was removed by washing with the ELX 405 and the final volume was aspirated to 20 μL. Compound master plates were formatted in an 11 point concentration-response curve (CRC) format (1:3 dilutions) in 100% DMSO with a starting concentration of 10 mM using a BRAVO liquid handler (Agilent). Test compound CRCs were then transferred to daughter plates (240 nL) using the Echo acoustic plate reformatter (Labcyte, Sunnyvale, Calif.) and then diluted into assay buffer (40 μL) to a 2× stock using a Thermo Fisher Combi (Thermo Fisher Scientific, Waltham, Mass.).Calcium flux was measured using the Functional Drug Screening System (FDSS) 6000 or 7000 (Hamamatsu Corporation, Tokyo, Japan) as an increase in the fluorescent static ratio. Compounds were applied to cells (20 μL, 2×) using the automated system of the FDSS at 2-4 s into the protocol and the data were collected at 1 Hz. At 144 s, 10 μL of an EC20 concentration of the muscarinic receptor agonist acetylcholine was added (5×), followed by the addition of 12 μL of an EC80 concentration of acetylcholine at the 230 s time point (5×). Agonist activity was analyzed as a concentration-dependent increase in calcium mobilization upon compound addition. Positive allosteric modulator activity was analyzed as a concentration-dependent increase in the EC20 acetylcholine response. Antagonist activity was analyzed as a concentration-dependent decrease in the EC80 acetylcholine response. Concentration-response curves were generated using a four-parameter logistical equation in XLFit curve fitting software (IDBS, Bridgewater, N.J.) for Excel (Microsoft, Redmond, Wash.) or Prism (GraphPad Software, Inc., San Diego, Calif.).
ChEMBL 303 4 0 7 2.3 COCCN(C)c1ncnc2c1sc1nnc(C)c(C)c12 nan
45142486 105586 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human M4 AchRPositive allosteric modulation of human M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
CHEMBL1589763 105586 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human M4 AchRPositive allosteric modulation of human M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
171345277 387134 0 None None None Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
171346325 387134 0 None None None Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315812 387134 0 None None None Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5316061 387134 0 None None None Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
89777215 385972 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5265891 385972 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
89777215 385972 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5265891 385972 0 None None None Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
5487426 135875 7 None None None Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
5487427 135875 7 None None None Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
5487429 135875 7 None None None Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
CHEMBL1900528 135875 7 None None None Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
DB01409 135875 7 None None None Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
3494 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
4302 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
7459 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
9933193 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
CHEMBL1201335 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
DB00986 3732 12 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
11434515 536 9 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
4484 536 9 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
7449 536 9 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
CHEMBL1194325 536 9 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
DB08897 536 9 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
2551 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
298 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
488 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
5831 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
CHEMBL965 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
DB00411 1644 11 None None None Human 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
156493833 368213 5 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
CHEMBL4853244 368213 5 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
1734 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
307 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
CHEMBL168067 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
1734 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
307 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL168067 239 5 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
11968014 18507 4 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
119680147 18507 4 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
CHEMBL1187846 18507 4 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
DB00747 18507 4 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
1734 239 5 None None None Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 239 5 None None None Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 239 5 None None None Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
1757 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
23724781 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
71183 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
CHEMBL1354199 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
CHEMBL376897 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
DB00462 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
DB11315 270505 11 None None None Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
1402 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
154417 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
174174 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL1331216 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00424 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 1082 53 None None None Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
1734 239 5 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
307 239 5 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
CHEMBL168067 239 5 None None None Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
1734 239 5 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 239 5 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 239 5 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
2200 6369 35 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 6369 35 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 6369 35 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 6369 35 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 6369 35 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
3000322 7238 26 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
330 7238 26 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
CHEMBL569713 7238 26 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
DB00747 7238 26 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
1734 239 5 None None None Human 8.7 pIC50 = 8.7 Binding
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
307 239 5 None None None Human 8.7 pIC50 = 8.7 Binding
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
CHEMBL168067 239 5 None None None Human 8.7 pIC50 = 8.7 Binding
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
2028 6066 59 None None None Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 6066 59 None None None Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 6066 59 None None None Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 6066 59 None None None Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 6066 59 None None None Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
44575653 355491 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 327 14 7 4 0.4 N=C(N)NCCCCCCCCC(=O)C(N)CCCNC(=N)N 10.1021/np50120a004
CHEMBL477542 355491 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 327 14 7 4 0.4 N=C(N)NCCCCCCCCC(=O)C(N)CCCNC(=N)N 10.1021/np50120a004
49671356 313325 11 None None None Human 6.0 pIC50 = 6 Binding
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 313325 11 None None None Human 6.0 pIC50 = 6 Binding
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
2551 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
5831 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 1644 11 None None None Human 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
14660293 105872 1 None None None Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
CHEMBL15936 105872 1 None None None Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
3468 350117 13 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
4138 350117 13 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 350117 13 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
DB00406 350117 13 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
1530 4450 49 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 4450 49 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 4450 49 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 4450 49 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 4450 49 None None None Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
1379 116475 17 None None None Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
5282593 116475 17 None None None Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 116475 17 None None None Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
DB11181 116475 17 None None None Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
10777692 25704 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180296 25704 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3013846 371456 2 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 371456 2 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
2200 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
2200 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 6369 35 None None None Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
2683 202943 22 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 202943 22 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
DB11073 202943 22 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
10567192 26367 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1183934 26367 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10678449 46482 0 None None None Human 6.0 pIC50 = 6.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL132698 46482 0 None None None Human 6.0 pIC50 = 6.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
10593954 27336 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190178 27336 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
324 3939 17 None None None Human 6.9 pIC50 = 6.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
6436265 3939 17 None None None Human 6.9 pIC50 = 6.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
CHEMBL277642 3939 17 None None None Human 6.9 pIC50 = 6.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
10784004 27642 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192621 27642 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
10522202 25711 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180312 25711 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
2812 19119 69 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
719 19119 69 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 19119 69 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
DB00257 19119 69 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
107782 38381 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
4667 38381 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 38381 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
DB14669 38381 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
10082470 105932 0 None None None Human 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL15944 105932 0 None None None Human 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
14925759 313920 6 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 313920 6 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
137640201 312873 2 None None None Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 312873 2 None None None Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
118719926 234715 0 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 234715 0 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
1999 473057 30 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
4601 473057 30 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 473057 30 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
DB01173 473057 30 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
10854879 25694 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180239 25694 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
153284501 350107 0 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 480 5 1 5 4.4 CC[C@@]12CCCN3CCc4c([nH]c5ccccc45)[C@]31N(Cc1cn(Cc3ccccc3)nn1)C(=O)C2 10.1021/acs.jmedchem.9b01924
CHEMBL4592258 350107 0 None None None Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 480 5 1 5 4.4 CC[C@@]12CCCN3CCc4c([nH]c5ccccc45)[C@]31N(Cc1cn(Cc3ccccc3)nn1)C(=O)C2 10.1021/acs.jmedchem.9b01924
10538337 26382 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1184062 26382 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
10641009 25703 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180292 25703 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
44190762 350837 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 350837 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
2230 961 44 None None None Human 4.9 pIC50 = 4.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
296 961 44 None None None Human 4.9 pIC50 = 4.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
CHEMBL7303 961 44 None None None Human 4.9 pIC50 = 4.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
DB04365 961 44 None None None Human 4.9 pIC50 = 4.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
2274 6448 36 None None None Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 6448 36 None None None Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 6448 36 None None None Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 6448 36 None None None Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 6448 36 None None None Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10610375 25699 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1180284 25699 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
10610375 25699 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
CHEMBL1180284 25699 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
1688 296777 35 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
6075 296777 35 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 296777 35 None None None Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
2599 116531 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
5404 116531 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1714574 116531 16 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10760249 25700 0 None None None Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
CHEMBL1180285 25700 0 None None None Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
10760249 25700 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180285 25700 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
10636001 25702 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180290 25702 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9905467 25713 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180316 25713 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
118719922 234710 0 None None None Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None None None Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
164606754 368011 17 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 368011 17 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
10688349 26407 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10759393 26407 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184138 26407 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2219563 26407 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10846833 103045 0 None None None Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
CHEMBL15675 103045 0 None None None Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
10663572 27418 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190784 27418 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
44302833 202569 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL304036 202569 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
118719927 234716 0 None None None Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 234716 0 None None None Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
2726 1895 54 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
44302755 466582 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61494 466582 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
9913341 163586 3 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determinedInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 163586 3 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determinedInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
135398745 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1982 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
4585 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 5933 69 None None None Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1482 367203 61 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
60838 367203 61 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 367203 61 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
DB00762 367203 61 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
10522336 39028 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120972 39028 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2337 6622 53 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 6622 53 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 6622 53 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 6622 53 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 6622 53 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
46871844 21141 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083925 21141 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
2090 389838 56 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
4735 389838 56 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 389838 56 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
DB00738 389838 56 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
46871665 20925 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
CHEMBL1083108 20925 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
277 2680 45 None None None Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 2680 45 None None None Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 2680 45 None None None Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 2680 45 None None None Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 2680 45 None None None Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
118719926 234715 0 None None None Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 234715 0 None None None Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
2750 64617 55 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
6604850 64617 55 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL1398683 64617 55 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 64617 55 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
DB09201 64617 55 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
44302775 467876 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL62247 467876 0 None None None Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
1548953 473104 29 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 473104 29 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
DB06735 473104 29 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
10782462 26385 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184068 26385 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
137374255 386864 3 None None None Human 7.8 pIC50 = 7.8 Binding
Positive allosteric modulator activity at human M4 receptorPositive allosteric modulator activity at human M4 receptor
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
CHEMBL5287400 386864 3 None None None Human 7.8 pIC50 = 7.8 Binding
Positive allosteric modulator activity at human M4 receptorPositive allosteric modulator activity at human M4 receptor
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
191 833 62 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 833 62 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 833 62 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 833 62 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 833 62 None None None Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
10664532 26383 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184064 26383 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10569816 25736 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180367 25736 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
10236758 234707 4 None None None Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None None None Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
2247 1042 63 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
118719922 234710 0 None None None Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None None None Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10594386 25695 0 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180249 25695 0 None None None Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
1210 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
5281070 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1200927 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB09555 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 1893 53 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2338 461820 42 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
237 461820 42 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 461820 42 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
DB01103 461820 42 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
1757 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
23724781 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
71183 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
CHEMBL1354199 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
CHEMBL376897 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
DB00462 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
DB11315 270505 11 None None None Human 8.6 pIC50 = 8.6 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/s0960-894x(98)00351-5
1201549 1234 18 None None None Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 1234 18 None None None Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 1234 18 None None None Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 1234 18 None None None Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 1234 18 None None None Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
3042 2911 27 None None None Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 2911 27 None None None Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 2911 27 None None None Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 2911 27 None None None Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 2911 27 None None None Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
26987 1955 32 None None None Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 1955 32 None None None Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 1955 32 None None None Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 1955 32 None None None Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 1955 32 None None None Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10567372 26402 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 26402 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44302900 467878 0 None None None Human 5.7 pIC50 = 5.7 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL62251 467878 0 None None None Human 5.7 pIC50 = 5.7 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
135 5144 38 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 5144 38 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 5144 38 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 5144 38 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 5144 38 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
3198 461850 54 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None None None Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10547222 233784 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333940 233784 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10592484 25712 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180314 25712 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10666533 25709 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180310 25709 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10236758 234707 4 None None None Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None None None Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
10499832 26406 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184134 26406 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
2068 370177 47 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
43815 370177 47 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 370177 47 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
DB00715 370177 47 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
101882890 234711 0 None None None Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 234711 0 None None None Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
2200 6369 35 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
328 6369 35 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
4848 6369 35 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
CHEMBL9967 6369 35 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
DB00670 6369 35 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
2774 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
688595 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1457550 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 8415 68 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
3652 8876 57 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 8876 57 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 8876 57 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 8876 57 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 8876 57 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
2335 26122 15 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
3018 26122 15 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 26122 15 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
DB11125 26122 15 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
10854880 25698 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180282 25698 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
2800 159972 9 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
5648 159972 9 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 159972 9 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
DB13497 159972 9 None None None Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
2436 470362 35 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
68617 470362 35 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 470362 35 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
DB01104 470362 35 None None None Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
44302834 467155 0 None None None Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61700 467155 0 None None None Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
3055 2955 32 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 2955 32 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 2955 32 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 2955 32 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 2955 32 None None None Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
10808719 26403 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184120 26403 0 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
10546275 39100 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL121059 39100 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
137374255 386864 3 None None None Rat 7.5 pIC50 = 7.5 Binding
Positive allosteric modulator activity at rat M4 receptor by FLIPR assayPositive allosteric modulator activity at rat M4 receptor by FLIPR assay
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
CHEMBL5287400 386864 3 None None None Rat 7.5 pIC50 = 7.5 Binding
Positive allosteric modulator activity at rat M4 receptor by FLIPR assayPositive allosteric modulator activity at rat M4 receptor by FLIPR assay
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
2284 6466 25 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 6466 25 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 6466 25 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 6466 25 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 6466 25 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
3000322 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
330 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
CHEMBL569713 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
DB00747 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
3000322 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
330 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
CHEMBL569713 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
DB00747 7238 26 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm501173q
25070582 124212 27 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 124212 27 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
44302728 412789 0 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL58228 412789 0 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10518821 26398 0 None None None Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184108 26398 0 None None None Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
46891179 20747 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082365 20747 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46871666 21395 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084993 21395 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
1800 473856 65 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10611310 26394 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184096 26394 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
124 6070 37 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 6070 37 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 6070 37 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 6070 37 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 6070 37 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
9882189 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic 4 receptor (unknown origin)Binding affinity to muscarinic 4 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
CHEMBL4297224 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic 4 receptor (unknown origin)Binding affinity to muscarinic 4 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
DB05592 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic 4 receptor (unknown origin)Binding affinity to muscarinic 4 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
9882189 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
CHEMBL4297224 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
DB05592 332214 37 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
118719926 234715 0 None None None Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 234715 0 None None None Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
5310989 450338 0 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL60142 450338 0 None None None Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
124087 2860 75 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 2860 75 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 2860 75 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 2860 75 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 2860 75 None None None Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
1212 3415 38 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 3415 38 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 3415 38 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 3415 38 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 3415 38 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
118719921 234709 0 None None None Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None None None Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44302741 466279 0 None None None Human 6.4 pIC50 = 6.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61412 466279 0 None None None Human 6.4 pIC50 = 6.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
2106 461821 25 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
4746 461821 25 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 461821 25 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
DB01074 461821 25 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
176 823 54 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
118719928 234717 0 None None None Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 234717 0 None None None Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
1547484 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
2761 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 1937 56 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10358345 25719 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180331 25719 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
44302813 202036 0 None None None Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL301041 202036 0 None None None Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
10660 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
10516408 25718 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180330 25718 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3168 23567 68 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
966 23567 68 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 23567 68 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 23567 68 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
5318 39468 43 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 39468 43 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB06820 39468 43 None None None Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
46890977 21061 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083723 21061 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
118719922 234710 0 None None None Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None None None Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
1634 163834 36 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
4011 163834 36 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 163834 36 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
DB00934 163834 36 None None None Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
10549581 25726 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180349 25726 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
3158 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
667468 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
956 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
CHEMBL101740 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
CHEMBL1628227 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
DB01142 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
DB14750 18465 32 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
10595006 25722 0 None None None Human 4.4 pIC50 = 4.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180343 25722 0 None None None Human 4.4 pIC50 = 4.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10595006 25722 0 None None None Human 4.4 pIC50 = 4.4 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 25722 0 None None None Human 4.4 pIC50 = 4.4 Binding
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10757736 26198 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10852843 26198 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1182713 26198 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120135 26198 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10851853 26459 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184242 26459 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
118719921 234709 0 None None None Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None None None Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
135398737 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
2818 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL253391 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 1973 61 None None None Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
2536 308773 12 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
5354 308773 12 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
CHEMBL404849 308773 12 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
44302776 202432 0 None None None Human 6.3 pIC50 = 6.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL303758 202432 0 None None None Human 6.3 pIC50 = 6.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10591874 27573 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192001 27573 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
44302793 433128 0 None None None Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
CHEMBL59347 433128 0 None None None Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
2230 961 44 None None None Human 4.3 pIC50 = 4.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
296 961 44 None None None Human 4.3 pIC50 = 4.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
CHEMBL7303 961 44 None None None Human 4.3 pIC50 = 4.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
DB04365 961 44 None None None Human 4.3 pIC50 = 4.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
10236758 234707 4 None None None Human 4.3 pIC50 = 4.3 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None None None Human 4.3 pIC50 = 4.3 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
57396813 143773 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of M4 receptorInhibition of M4 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 143773 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of M4 receptorInhibition of M4 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
1016 8173 46 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
10797864 59828 0 None None None Human 7.3 pIC50 = 7.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
CHEMBL135645 59828 0 None None None Human 7.3 pIC50 = 7.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
10726038 238188 0 None None None Human 6.3 pIC50 = 6.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
CHEMBL344892 238188 0 None None None Human 6.3 pIC50 = 6.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
656392 367132 2 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
CHEMBL480464 367132 2 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
180 829 44 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 829 44 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 829 44 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 829 44 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 829 44 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
11968014 18507 4 None None None Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
119680147 18507 4 None None None Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
CHEMBL1187846 18507 4 None None None Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
DB00747 18507 4 None None None Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/acs.jmedchem.8b00265
2745 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 8402 34 None None None Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
302 6062 14 None None None Human 5.3 pIC50 = 5.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
4630 6062 14 None None None Human 5.3 pIC50 = 5.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
CHEMBL7634 6062 14 None None None Human 5.3 pIC50 = 5.3 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
44302788 448448 0 None None None Human 6.3 pIC50 = 6.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL59939 448448 0 None None None Human 6.3 pIC50 = 6.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
46891488 21495 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1085507 21495 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
10567372 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10684720 26365 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1183926 26365 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10567372 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10567372 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 26402 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
1200 3405 44 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
12488 3405 44 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 3405 44 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 3405 44 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 3405 44 None None None Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
10785471 232751 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL332320 232751 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
156493833 368213 5 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
CHEMBL4853244 368213 5 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
10660 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
10686988 26460 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
CHEMBL1184244 26460 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
118719927 234716 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 234716 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
118719928 234717 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 234717 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
164612139 367984 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4849905 367984 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
2745 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
5572 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
66007 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
7315 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
CHEMBL1490 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
DB00376 8402 34 None None None Human 8.2 pIC50 = 8.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
44302727 202025 0 None None None Human 5.2 pIC50 = 5.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL300987 202025 0 None None None Human 5.2 pIC50 = 5.2 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10806268 26408 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184139 26408 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
4841 139710 2 None None None Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 139710 2 None None None Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
10267601 26400 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184116 26400 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
118719921 234709 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None None None Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10782321 26395 0 None None None Human 4.2 pIC50 = 4.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL1184098 26395 0 None None None Human 4.2 pIC50 = 4.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
1821 410750 60 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
4212 410750 60 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL58 410750 60 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
DB01204 410750 60 None None None Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
10755732 26392 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184092 26392 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
9974222 26195 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1182709 26195 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
2286 6468 43 None None None Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 6468 43 None None None Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 6468 43 None None None Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 6468 43 None None None Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 6468 43 None None None Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
10638050 25692 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180202 25692 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2551 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
298 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
488 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
5831 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
CHEMBL965 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
DB00411 1644 11 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
49853884 181500 0 None None None Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M4 receptor (unknown origin) by radioligand displacement assayBinding affinity to M4 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
CHEMBL2391353 181500 0 None None None Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M4 receptor (unknown origin) by radioligand displacement assayBinding affinity to M4 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
10755733 25705 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180297 25705 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
10761219 25708 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1180309 25708 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
10236758 234707 4 None None None Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None None None Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
10573693 25707 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180305 25707 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
10757736 26198 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10852843 26198 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1182713 26198 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120135 26198 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
118719927 234716 0 None None None Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 234716 0 None None None Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
46891076 21037 0 None None None Human 5.1 pIC50 = 5.1 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083618 21037 0 None None None Human 5.1 pIC50 = 5.1 Binding
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
100 8289 46 None None None Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 8289 46 None None None Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 8289 46 None None None Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 8289 46 None None None Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 8289 46 None None None Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10487582 61890 0 None None None Human 6.1 pIC50 = 6.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL137384 61890 0 None None None Human 6.1 pIC50 = 6.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
44356367 237289 0 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
CHEMBL341447 237289 0 None None None Human 5.1 pIC50 = 5.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
118719928 234717 0 None None None Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 234717 0 None None None Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
10688349 26407 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10759393 26407 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184138 26407 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2219563 26407 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
3191 202914 68 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
977 202914 68 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 202914 68 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 202914 68 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10521205 25706 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180298 25706 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
10829928 26671 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
CHEMBL1185758 26671 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
10614695 26428 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184188 26428 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
137640201 312873 2 None None None Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 312873 2 None None None Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
6726 2642 44 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 2642 44 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 2642 44 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 2642 44 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 2642 44 None None None Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10827157 25714 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180317 25714 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
306 7028 17 None None None Human 7.1 pIC50 = 7.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
3536 7028 17 None None None Human 7.1 pIC50 = 7.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
9577995 7028 17 None None None Human 7.1 pIC50 = 7.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
CHEMBL134641 7028 17 None None None Human 7.1 pIC50 = 7.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
11498 6149 38 None None None Human 7.0 pIC50 = 7.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
4995951 6149 38 None None None Human 7.0 pIC50 = 7.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
CHEMBL59898 6149 38 None None None Human 7.0 pIC50 = 7.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
2398 1965 48 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 1965 48 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 1965 48 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 1965 48 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 1965 48 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
10248541 366275 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 369 15 7 4 0.5 CC(=O)NC(CCCNC(=N)N)C(=O)CCCCCCCCNC(=N)N 10.1021/np50120a004
CHEMBL479224 366275 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 369 15 7 4 0.5 CC(=O)NC(CCCNC(=N)N)C(=O)CCCCCCCCNC(=N)N 10.1021/np50120a004
1971 5840 38 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 5840 38 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 5840 38 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 5840 38 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 5840 38 None None None Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
11793999 26386 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184074 26386 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
101882890 234711 0 None None None Human 4.0 pIC50 = 4.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 234711 0 None None None Human 4.0 pIC50 = 4.0 Binding
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
164612139 367984 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4849905 367984 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
44302901 201193 0 None None None Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL294726 201193 0 None None None Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
10511551 59521 0 None None None Human 6.0 pIC50 = 6.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL135328 59521 0 None None None Human 6.0 pIC50 = 6.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
44302879 467505 0 None None None Human 5.0 pIC50 = 5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61774 467505 0 None None None Human 5.0 pIC50 = 5 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
164612037 368668 0 None 1 14 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 368668 0 None 1 14 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 385513 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 385513 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 385564 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 385564 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 385575 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 385575 0 None -3 20 Human 10.3 pKd = 10.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
10365181 42418 0 None 1 3 Rat 9.5 pKd = 9.5 Binding
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
CHEMBL127587 42418 0 None 1 3 Rat 9.5 pKd = 9.5 Binding
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
137630050 316598 0 None -2 2 Human 9.2 pKd = 9.2 Binding
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4116470 316598 0 None -2 2 Human 9.2 pKd = 9.2 Binding
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
10365181 42418 0 None 1 3 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
CHEMBL127587 42418 0 None 1 3 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
156015807 352214 0 None -6 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding studyBinding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding study
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 352214 0 None -6 3 Human 8.0 pKd = 8.0 Binding
Binding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding studyBinding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding study
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
10274019 469175 0 None 1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71124 469175 0 None 1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
71452756 161024 0 None -2 4 Human 10.1 pKi = 10.1 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2114068 161024 0 None -2 4 Human 10.1 pKi = 10.1 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
1757 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
23724781 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
71183 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
CHEMBL1354199 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
CHEMBL376897 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
DB00462 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
DB11315 270505 11 None -1 5 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 nan
1402 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
154417 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
174174 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL1331216 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00424 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 1082 53 None -1 16 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
16065403 140207 28 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 140207 28 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
DB12408 140207 28 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
1757 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
23724781 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
71183 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
CHEMBL1354199 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
CHEMBL376897 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
DB00462 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
DB11315 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm061374r
1757 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
23724781 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
71183 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
CHEMBL1354199 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
CHEMBL376897 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
DB00462 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
DB11315 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm2013216
1757 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
23724781 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
71183 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
CHEMBL1354199 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
CHEMBL376897 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
DB00462 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
DB11315 270505 11 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm901048j
2028 6066 59 None -1 10 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 6066 59 None -1 10 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 6066 59 None -1 10 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 6066 59 None -1 10 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 6066 59 None -1 10 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
71454563 161131 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2115128 161131 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
9867847 469182 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL71147 469182 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
1201549 1234 18 None -1 20 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 1234 18 None -1 20 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 1234 18 None -1 20 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 1234 18 None -1 20 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 1234 18 None -1 20 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
1402 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
154417 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
174174 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
260 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
320 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL1331216 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL517712 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
DB00424 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
DB00572 1082 53 None -1 16 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
44610056 252041 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 252041 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
1734 239 5 None -1 10 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 239 5 None -1 10 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 239 5 None -1 10 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
325 4217 10 None -2 8 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
3746 4217 10 None -2 8 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
657308 4217 10 None -2 8 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
CHEMBL1615433 4217 10 None -2 8 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
DB00332 4217 10 None -2 8 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
3042 2911 27 None -1 13 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 2911 27 None -1 13 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 2911 27 None -1 13 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 2911 27 None -1 13 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 2911 27 None -1 13 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
162645520 366962 0 None 1 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802414 366962 0 None 1 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
156014450 352166 0 None -2 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650652 352166 0 None -2 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
16116083 26566 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184884 26566 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
137630050 316598 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4116470 316598 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
1734 239 5 None -1 10 Human 9.3 pKi = 9.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
307 239 5 None -1 10 Human 9.3 pKi = 9.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
CHEMBL168067 239 5 None -1 10 Human 9.3 pKi = 9.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
1734 239 5 None -1 10 Rat 9.3 pKi = 9.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
307 239 5 None -1 10 Rat 9.3 pKi = 9.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
CHEMBL168067 239 5 None -1 10 Rat 9.3 pKi = 9.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
1402 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
154417 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
174174 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
260 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
320 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
CHEMBL1331216 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
CHEMBL517712 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
DB00424 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
DB00572 1082 53 None -1 16 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
171351429 386951 0 None 1 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 973 22 2 5 14.1 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5289601 386951 0 None 1 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 973 22 2 5 14.1 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
154417 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
174174 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
637577 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
CHEMBL1379091 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
CHEMBL2449003 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
CHEMBL254656 57629 58 None -2 9 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
5487426 135875 7 None -12 9 Human 9.2 pKi = 9.2 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.6019/CHEMBL5442175
5487427 135875 7 None -12 9 Human 9.2 pKi = 9.2 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.6019/CHEMBL5442175
5487429 135875 7 None -12 9 Human 9.2 pKi = 9.2 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.6019/CHEMBL5442175
CHEMBL1900528 135875 7 None -12 9 Human 9.2 pKi = 9.2 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.6019/CHEMBL5442175
DB01409 135875 7 None -12 9 Human 9.2 pKi = 9.2 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.6019/CHEMBL5442175
1402 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
154417 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
174174 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
260 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
320 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
CHEMBL1331216 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
CHEMBL517712 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
DB00424 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
DB00572 1082 53 None -1 16 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.05.042
1734 239 5 None -1 10 Human 9.2 pKi = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 239 5 None -1 10 Human 9.2 pKi = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 239 5 None -1 10 Human 9.2 pKi = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
164611189 371675 0 None -3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 944 24 11 12 0.6 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028061 371675 0 None -3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 944 24 11 12 0.6 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
46188794 352234 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651099 352234 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
16115947 26123 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182214 26123 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
164625454 371787 0 None -3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 1001 26 12 13 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028885 371787 0 None -3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 1001 26 12 13 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
180 829 44 None -2 32 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 829 44 None -2 32 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 829 44 None -2 32 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 829 44 None -2 32 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 829 44 None -2 32 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
164612662 371686 0 None -2 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 845 20 8 11 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028154 371686 0 None -2 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 845 20 8 11 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2745 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 8402 34 None 1 5 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
9936450 78636 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
CHEMBL143469 78636 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
164622681 371761 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164624669 371761 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028712 371761 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028837 371761 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156014269 351168 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4635500 351168 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
171349546 386954 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 959 21 2 5 13.8 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5289667 386954 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 959 21 2 5 13.8 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
171344666 386187 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
CHEMBL5271406 386187 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
16116085 26120 0 None -8 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182201 26120 0 None -8 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
16115945 26567 0 None -4 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1184886 26567 0 None -4 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
1734 239 5 None -1 10 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
307 239 5 None -1 10 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
CHEMBL168067 239 5 None -1 10 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
118719922 234710 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 234710 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
171356451 386289 0 None 2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 945 20 2 5 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5273907 386289 0 None 2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 945 20 2 5 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
155521894 350393 0 None -11 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596183 350393 0 None -11 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
75167447 352201 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650933 352201 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
162677523 367008 0 None -4 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4802932 367008 0 None -4 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
10160073 220705 0 None 151 5 Human 9.0 pKi = 9 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
CHEMBL326450 220705 0 None 151 5 Human 9.0 pKi = 9 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
16115797 270503 0 None -2 5 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376870 270503 0 None -2 5 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
10160219 19269 0 None 100 5 Human 9.0 pKi = 9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL104693 19269 0 None 100 5 Human 9.0 pKi = 9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
10160073 220705 0 None 151 5 Human 9.0 pKi = 9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL326450 220705 0 None 151 5 Human 9.0 pKi = 9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
2286 6468 43 None -3 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 6468 43 None -3 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 6468 43 None -3 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 6468 43 None -3 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 6468 43 None -3 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
155523648 350556 0 None -7 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597576 350556 0 None -7 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
101882890 234711 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 234711 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
155550436 350467 0 None -14 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596780 350467 0 None -14 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
16115798 270498 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376255 270498 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
155560305 350222 0 None -5 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4594890 350222 0 None -5 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
16115799 164850 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL219825 164850 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
155556290 350423 0 None -7 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596434 350423 0 None -7 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
1402 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
154417 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
174174 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
260 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
320 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
CHEMBL1331216 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
CHEMBL517712 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
DB00424 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
DB00572 1082 53 None -1 16 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
171346725 386786 0 None -2 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
CHEMBL5285607 386786 0 None -2 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
164614083 371695 0 None -7 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028231 371695 0 None -7 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164624066 371777 0 None -6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 787 18 7 10 1.8 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028806 371777 0 None -6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 787 18 7 10 1.8 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
5284632 139685 10 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
CHEMBL1888176 139685 10 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
DB00209 139685 10 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
10628017 45554 0 None -3 4 Rat 8.8 pKi = 8.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL131865 45554 0 None -3 4 Rat 8.8 pKi = 8.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
57326235 158824 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079009 158824 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
24846938 180630 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377267 180630 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
15157137 200078 0 None 1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL286008 200078 0 None 1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
302 6062 14 None -2 7 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
4630 6062 14 None -2 7 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
CHEMBL7634 6062 14 None -2 7 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
1402 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
154417 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
174174 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
260 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
320 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
CHEMBL1331216 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
CHEMBL517712 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
DB00424 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
DB00572 1082 53 None -1 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2017.04.009
155567380 350376 0 None -20 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596064 350376 0 None -20 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
171349519 386938 0 None 1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1002 24 3 6 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCNCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5289083 386938 0 None 1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1002 24 3 6 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCNCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
16115943 26121 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182205 26121 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
164622681 371761 0 None -7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164624669 371761 0 None -7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028712 371761 0 None -7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028837 371761 0 None -7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16115796 274625 0 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375073 274625 0 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
9809330 234933 0 None -18 5 Human 8.7 pKi = 8.7 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
CHEMBL335542 234933 0 None -18 5 Human 8.7 pKi = 8.7 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
372625 201281 5 None -6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL295388 201281 5 None -6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
155566290 350543 0 None -25 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4597498 350543 0 None -25 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
372625 201281 5 None -6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
CHEMBL295388 201281 5 None -6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
10203251 19562 0 None 35 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
CHEMBL106224 19562 0 None 35 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
9911615 199260 0 None 114 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
CHEMBL280220 199260 0 None 114 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
9931930 218201 0 None 35 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL320465 218201 0 None 35 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
129989 933 31 None -2 11 Rat 8.0 pKi = 8 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
8584 933 31 None -2 11 Rat 8.0 pKi = 8 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
CHEMBL43383 933 31 None -2 11 Rat 8.0 pKi = 8 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
119357 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
368 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
CHEMBL279453 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
10125445 157687 0 None -3 5 Human 8.0 pKi = 8 Binding
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 157687 0 None -3 5 Human 8.0 pKi = 8 Binding
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
119357 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
368 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
CHEMBL279453 7874 37 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
137637944 311745 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4059829 311745 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
164610746 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164621305 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164623076 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028038 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028642 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028732 371671 0 None -28 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155559741 350256 0 None -5 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595125 350256 0 None -5 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
324 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
6436265 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
CHEMBL277642 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
324 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 3939 17 None 1 7 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
164619973 371744 0 None -33 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028571 371744 0 None -33 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10114698 19172 0 None 41 5 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104210 19172 0 None 41 5 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
135398737 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2818 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL253391 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 1973 61 None -8 61 Human 7.0 pKi = 7 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
145960827 316924 0 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4126290 316924 0 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
44299589 385094 0 None -1 4 Human 6.0 pKi = 6 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL56275 385094 0 None -1 4 Human 6.0 pKi = 6 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
135398745 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
1982 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
4585 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 5933 69 None -16 45 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
2337 6622 53 None -21 36 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 6622 53 None -21 36 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 6622 53 None -21 36 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 6622 53 None -21 36 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 6622 53 None -21 36 Human 6.0 pKi = 6 Binding
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
11012653 239446 0 None -6 5 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355769 239446 0 None -6 5 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
56593934 137990 0 None -1380 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 137990 0 None -1380 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
44448530 26604 0 None -1 2 Human 4.0 pKi = 4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185259 26604 0 None -1 2 Human 4.0 pKi = 4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44593617 370668 0 None -5 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 370668 0 None -5 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
2684 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
584 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
9658 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
CHEMBL168815 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
DB00185 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
164614364 371699 0 None -2 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 733 15 9 10 -1.0 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028248 371699 0 None -2 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 733 15 9 10 -1.0 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2733619 26185 5 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508725 26185 5 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182634 26185 5 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
44627739 407561 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL576663 407561 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
44593623 371103 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 371103 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
15050948 202873 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL305403 202873 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
164611347 371678 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028070 371678 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2200 6369 35 None -3 11 Human 7.0 pKi = 7.0 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
328 6369 35 None -3 11 Human 7.0 pKi = 7.0 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
4848 6369 35 None -3 11 Human 7.0 pKi = 7.0 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
CHEMBL9967 6369 35 None -3 11 Human 7.0 pKi = 7.0 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
DB00670 6369 35 None -3 11 Human 7.0 pKi = 7.0 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
71575122 177092 0 None -45 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312376 177092 0 None -45 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
154734599 5087 6 None -6 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
327 5087 6 None -6 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
4108 5087 6 None -6 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
CHEMBL27673 5087 6 None -6 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
155559291 350619 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 689 16 5 7 3.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598099 350619 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 689 16 5 7 3.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
109035013 354349 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
CHEMBL4752973 354349 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
11048067 19911 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107679 19911 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
44437227 26152 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 194 3 0 4 0.9 Cc1cc(OCC#CCN(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182447 26152 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 194 3 0 4 0.9 Cc1cc(OCC#CCN(C)C)no1 10.1016/j.bmc.2007.09.003
164611279 371677 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164627387 371677 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028067 371677 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028995 371677 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164623185 371768 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 407 4 3 5 1.5 NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028743 371768 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 407 4 3 5 1.5 NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
66561967 156373 0 None -1 7 Human 6.0 pKi = 6.0 Binding
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
CHEMBL2030626 156373 0 None -1 7 Human 6.0 pKi = 6.0 Binding
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
11061341 160414 0 None -23 5 Human 8.0 pKi = 8.0 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112958 160414 0 None -23 5 Human 8.0 pKi = 8.0 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
100 8289 46 None -4 34 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 8289 46 None -4 34 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 8289 46 None -4 34 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 8289 46 None -4 34 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 8289 46 None -4 34 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
177372528 393723 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 333 3 0 4 4.0 CN1[C@@H]2CC[C@H]1C[C@H](Oc1nc3ccccc3n1-c1ccccc1)C2 10.1016/j.ejmech.2023.115891
CHEMBL5646625 393723 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 333 3 0 4 4.0 CN1[C@@H]2CC[C@H]1C[C@H](Oc1nc3ccccc3n1-c1ccccc1)C2 10.1016/j.ejmech.2023.115891
16086063 162016 0 None -57 5 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214898 162016 0 None -57 5 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
12872437 26329 0 None -4 4 Human 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
CHEMBL1183585 26329 0 None -4 4 Human 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
3652 8876 57 None -3 18 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 8876 57 None -3 18 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 8876 57 None -3 18 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 8876 57 None -3 18 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 8876 57 None -3 18 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
132947 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
361 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
CHEMBL265256 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
145960466 317064 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4128341 317064 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
132947 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
361 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
CHEMBL265256 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
132947 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
361 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
CHEMBL265256 8408 6 None -41 9 Rat 7.9 pKi = 7.9 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
CHEMBL69452 468936 0 None -2 5 Human 5.0 pKi = 5.0 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
44439406 182612 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 8 0 4 5.9 CCCCSC1=CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241283 182612 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 8 0 4 5.9 CCCCSC1=CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
71457690 174785 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 174785 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
118719929 234718 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354076 234718 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
44593627 384960 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 384960 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
162353386 354842 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4758635 354842 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
57326237 158822 0 None -2 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078985 158822 0 None -2 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
44448457 26187 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182638 26187 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44448419 26605 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185266 26605 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
24865895 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL259662 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
44422692 26127 0 None -9 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 26127 0 None -9 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
24865895 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL259662 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
24865895 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL259662 193604 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
3191 202914 68 None -5 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
977 202914 68 None -5 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 202914 68 None -5 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 202914 68 None -5 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
71575027 177102 0 None -24 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL2312389 177102 0 None -24 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
44448385 26184 0 None 2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182633 26184 0 None 2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
44448606 26192 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182652 26192 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44593622 371025 0 None -5 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 371025 0 None -5 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
156013536 352226 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651058 352226 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
145960592 316905 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
145961125 316905 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4126071 316905 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128667 316905 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
162353384 354949 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4760037 354949 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
6726 2642 44 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 2642 44 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 2642 44 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 2642 44 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 2642 44 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
164613559 371690 0 None -38 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028196 371690 0 None -38 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
70685504 156130 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
CHEMBL2027846 156130 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
135398737 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
2818 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL253391 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 1973 61 None -8 61 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
135398745 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
1982 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
4585 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 5933 69 None -16 45 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
25067048 26602 0 None 28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185245 26602 0 None 28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
16094788 279100 0 None -5 5 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 279100 0 None -5 5 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
71449148 161022 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114064 161022 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
70687661 156129 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027845 156129 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
16086067 162753 0 None -75 5 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL215894 162753 0 None -75 5 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
44439400 182026 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 7 0 4 5.2 CCCOC1CCCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL240023 182026 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 7 0 4 5.2 CCCOC1CCCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
44439391 291856 0 None -331 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 3 2 4 3.3 COc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.01.093
CHEMBL391190 291856 0 None -331 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 3 2 4 3.3 COc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.01.093
44274469 162062 1 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21509 162062 1 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
162649767 353984 0 None -5 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 333 4 1 3 4.0 Cn1ccc2c(NC(=O)CCN3CCCc4ccccc43)cccc21 10.1016/j.bmcl.2020.127632
CHEMBL4748337 353984 0 None -5 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 333 4 1 3 4.0 Cn1ccc2c(NC(=O)CCN3CCCc4ccccc43)cccc21 10.1016/j.bmcl.2020.127632
2733638 26188 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508731 26188 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
8030329 26188 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182640 26188 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
9998508 161569 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21321 161569 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
11099206 239416 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355455 239416 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
54816802 355125 1 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4762056 355125 1 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
44448500 26603 0 None 1 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185248 26603 0 None 1 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
44274302 158709 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL20732 158709 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
57326144 158829 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079061 158829 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
71455894 174789 0 None -1 12 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 174789 0 None -1 12 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 174789 0 None -1 12 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2205827 174789 0 None -1 12 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
2337 6622 53 None -21 36 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
50 6622 53 None -21 36 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002 6622 53 None -21 36 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
CHEMBL716 6622 53 None -21 36 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
DB01224 6622 53 None -21 36 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
164614830 371704 0 None -32 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164627253 371704 0 None -32 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028275 371704 0 None -32 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028989 371704 0 None -32 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44274441 199319 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL280684 199319 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
73350931 183342 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432040 183342 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
73350823 202597 0 None -83 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human muscarinic M4 receptor by competitive binding assayBinding affinity to human muscarinic M4 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 202597 0 None -83 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human muscarinic M4 receptor by competitive binding assayBinding affinity to human muscarinic M4 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
11013666 122211 1 None -2 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL171102 122211 1 None -2 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
154059 7390 37 None -5 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
2457 7390 37 None -5 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
7483 7390 37 None -5 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
CHEMBL1734 7390 37 None -5 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
DB01591 7390 37 None -5 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
137642607 314389 0 None -660 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 314389 0 None -660 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
162353388 354841 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
CHEMBL4758633 354841 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
2398 1965 48 None -1 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 1965 48 None -1 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 1965 48 None -1 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 1965 48 None -1 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 1965 48 None -1 22 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
1971 5840 38 None -1 24 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 5840 38 None -1 24 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 5840 38 None -1 24 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 5840 38 None -1 24 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 5840 38 None -1 24 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4134 144899 9 None -8 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL1996652 144899 9 None -8 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
DB13181 144899 9 None -8 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
164610746 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164621305 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164623076 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028038 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028642 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028732 371671 0 None -28 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
129989 933 31 None -2 11 Human 7.9 pKi = 7.9 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
8584 933 31 None -2 11 Human 7.9 pKi = 7.9 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
CHEMBL43383 933 31 None -2 11 Human 7.9 pKi = 7.9 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.6019/CHEMBL5442175
2200 6369 35 None -3 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
328 6369 35 None -3 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
4848 6369 35 None -3 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
CHEMBL9967 6369 35 None -3 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
DB00670 6369 35 None -3 11 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
10092649 385614 38 None -11 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
CHEMBL522460 385614 38 None -11 9 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
611037 468687 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67532 468687 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
71452387 174790 0 None -1 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
CHEMBL2205829 174790 0 None -1 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
71452387 174790 0 None -1 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2205829 174790 0 None -1 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
73347826 183350 0 None 1 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
CHEMBL2432049 183350 0 None 1 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
CHEMBL5092747 479548 0 None -6 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 479 8 2 7 4.0 CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
CHEMBL5092747 479548 0 None -6 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 479 8 2 7 4.0 CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
11001809 121864 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169594 121864 0 None -3 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
11112362 19298 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104804 19298 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
56672197 138852 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 245 2 0 1 3.6 Fc1cccc(CN2C3CC4CC(C3)CC2C4)c1 10.1016/j.bmcl.2011.07.028
CHEMBL1852489 138852 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 245 2 0 1 3.6 Fc1cccc(CN2C3CC4CC(C3)CC2C4)c1 10.1016/j.bmcl.2011.07.028
108993425 355599 0 None -3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4777543 355599 0 None -3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
24894637 371906 0 None -5 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL504733 371906 0 None -5 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
11039424 160411 3 None -45 5 Human 7.9 pKi = 7.9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112955 160411 3 None -45 5 Human 7.9 pKi = 7.9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
1379 116475 17 None 1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
5282593 116475 17 None 1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 116475 17 None 1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
DB11181 116475 17 None 1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
44627740 404411 0 None -11 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL583051 404411 0 None -11 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
10139614 19370 0 None 19 4 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105160 19370 0 None 19 4 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
118719924 234713 0 None 2 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354071 234713 0 None 2 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
9889312 155116 2 None -2 5 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2111540 155116 2 None -2 5 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
3013846 371456 2 None -1 5 Human 6.9 pKi = 6.9 Binding
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 371456 2 None -1 5 Human 6.9 pKi = 6.9 Binding
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
3468 350117 13 None 1 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
4138 350117 13 None 1 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 350117 13 None 1 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
DB00406 350117 13 None 1 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
289 499 13 None -128 14 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 499 13 None -128 14 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 499 13 None -128 14 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
44439396 182610 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 348 3 0 3 4.3 CC(=O)OC1CCCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241281 182610 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 348 3 0 3 4.3 CC(=O)OC1CCCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
44318817 333726 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 333726 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
9308 41623 17 None -10 7 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL12587 41623 17 None -10 7 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
9308 41623 17 None -15 7 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 41623 17 None -15 7 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
1530 4450 49 None -109 24 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 4450 49 None -109 24 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 4450 49 None -109 24 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 4450 49 None -109 24 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 4450 49 None -109 24 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
164619081 371740 0 None -28 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164621814 371740 0 None -28 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028531 371740 0 None -28 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028667 371740 0 None -28 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
145961495 316989 0 None -2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127373 316989 0 None -2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
11120347 239363 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL354841 239363 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
162353391 354689 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
CHEMBL4756873 354689 0 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
36381 27204 1 None -4 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
CHEMBL1189234 27204 1 None -4 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
36381 27204 1 None -4 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
CHEMBL1189234 27204 1 None -4 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
155521383 350394 0 None -13 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596184 350394 0 None -13 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
164608958 371664 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164621861 371664 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027936 371664 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028673 371664 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
639794 199015 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278129 199015 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
11809446 122457 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL172234 122457 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
2683 202943 22 None -2 16 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 202943 22 None -2 16 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
DB11073 202943 22 None -2 16 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
11004046 19789 0 None 33 5 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107444 19789 0 None 33 5 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
11079969 328821 0 None 26 5 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL420662 328821 0 None 26 5 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
71452793 161130 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115127 161130 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
10963509 42356 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL127273 42356 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
44627746 28283 0 None -7 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197392 28283 0 None -7 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
164614388 371701 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 23 12 11 0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028251 371701 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 23 12 11 0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
70681307 156131 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027890 156131 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
44593625 371350 0 None -5 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 371350 0 None -5 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
14939893 23838 0 None -4 4 Rat 7.8 pKi = 7.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL112244 23838 0 None -4 4 Rat 7.8 pKi = 7.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
16086065 161260 0 None -53 4 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL211976 161260 0 None -53 4 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
57326233 158825 0 None -9 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079010 158825 0 None -9 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
164626977 371795 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 532 8 2 6 2.9 NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028969 371795 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 532 8 2 6 2.9 NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44593621 384959 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 384959 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
177372524 393588 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 307 3 0 4 3.5 CN1CCCC(Oc2nc3ccccc3n2-c2ccccc2)C1 10.1016/j.ejmech.2023.115891
CHEMBL5639621 393588 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 307 3 0 4 3.5 CN1CCCC(Oc2nc3ccccc3n2-c2ccccc2)C1 10.1016/j.ejmech.2023.115891
118719928 234717 0 None 1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 234717 0 None 1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
156010212 352152 0 None -4 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650562 352152 0 None -4 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
13990 393603 2 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 296 3 0 3 3.7 CN1CCC(OC(=O)N(c2ccccc2)c2ccccc2)C1 10.1016/j.ejmech.2023.115891
CHEMBL5639857 393603 2 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 296 3 0 3 3.7 CN1CCC(OC(=O)N(c2ccccc2)c2ccccc2)C1 10.1016/j.ejmech.2023.115891
58459 393587 14 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 310 3 0 3 4.1 CN1CCC(OC(=O)N(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2023.115891
CHEMBL5639592 393587 14 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 310 3 0 3 4.1 CN1CCC(OC(=O)N(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2023.115891
46682613 355014 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760823 355014 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
2726 1895 54 None -14 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 1895 54 None -14 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 1895 54 None -14 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 1895 54 None -14 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 1895 54 None -14 48 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
44627741 404464 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL571123 404464 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
101720828 197438 0 None -16 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
16147087 197438 0 None -16 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL267643 197438 0 None -16 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
10606253 313178 0 None -63 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL407678 313178 0 None -63 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
16094793 164733 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 164733 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
16094810 275273 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
CHEMBL376295 275273 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
109013312 354016 0 None -5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4748774 354016 0 None -5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
162353375 353780 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4745885 353780 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
156015141 352182 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650774 352182 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
10865439 44474 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL130835 44474 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
302 6062 14 None -2 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
4630 6062 14 None -2 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
CHEMBL7634 6062 14 None -2 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
177381475 391634 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-epibatidine from M4 receptor (unknown origin)Displacement of [3H]-epibatidine from M4 receptor (unknown origin)
ChEMBL 309 1 1 1 5.1 CC1=CC[C@@H]2C[C@H]1[C@H](c1ccc(C(F)(F)F)cc1)NC2(C)C 10.1021/acs.jmedchem.3c01758
CHEMBL5572105 391634 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-epibatidine from M4 receptor (unknown origin)Displacement of [3H]-epibatidine from M4 receptor (unknown origin)
ChEMBL 309 1 1 1 5.1 CC1=CC[C@@H]2C[C@H]1[C@H](c1ccc(C(F)(F)F)cc1)NC2(C)C 10.1021/acs.jmedchem.3c01758
44439404 182584 0 None -15 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241103 182584 0 None -15 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
1726 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1726 5075 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 5075 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 5075 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 5075 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 5075 9 None -12 5 Human 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2812 19119 69 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
719 19119 69 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 19119 69 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
DB00257 19119 69 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
145960592 316905 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
145961125 316905 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4126071 316905 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128667 316905 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
122387447 275658 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
CHEMBL3770686 275658 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
137661377 315060 0 None -316 8 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 315060 0 None -316 8 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
107782 38381 16 None -1 5 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
4667 38381 16 None -1 5 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 38381 16 None -1 5 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
DB14669 38381 16 None -1 5 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
71449073 160101 0 None -4 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
CHEMBL2112217 160101 0 None -4 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
44437298 26161 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182460 26161 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
197842 202663 1 None -56 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL3041160 202663 1 None -56 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
10043954 163707 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21716 163707 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
10957754 121828 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL169401 121828 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
162353369 354663 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4756442 354663 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
57326239 158821 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078974 158821 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
1999 473057 30 None 1 13 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
4601 473057 30 None 1 13 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 473057 30 None 1 13 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
DB01173 473057 30 None 1 13 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
155560140 350316 0 None -11 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595575 350316 0 None -11 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
5387 193580 24 None -9 4 Rat 7.8 pKi = 7.8 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
CHEMBL253978 193580 24 None -9 4 Rat 7.8 pKi = 7.8 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
71461681 161023 0 None -5 4 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114067 161023 0 None -5 4 Human 7.8 pKi = 7.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
122387447 275658 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
CHEMBL3770686 275658 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
4033 3883 45 None -5011 14 Human 5.8 pKi = 5.8 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.6019/CHEMBL5442175
9826520 3883 45 None -5011 14 Human 5.8 pKi = 5.8 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.6019/CHEMBL5442175
CHEMBL214957 3883 45 None -5011 14 Human 5.8 pKi = 5.8 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.6019/CHEMBL5442175
15157141 183610 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL24369 183610 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10360219 193798 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL301670 193798 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
132712 336328 18 None -5 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4468100 336328 18 None -5 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
10595006 25722 0 None -10 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 25722 0 None -10 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
44299635 200720 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL291562 200720 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
162353390 354812 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
CHEMBL4758316 354812 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
155519621 334943 0 None -54 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting method
ChEMBL 345 2 2 6 2.7 Clc1ccc(C#Cc2nc(N[C@@H]3CCOC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4447908 334943 0 None -54 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting method
ChEMBL 345 2 2 6 2.7 Clc1ccc(C#Cc2nc(N[C@@H]3CCOC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
145960427 316993 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127428 316993 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
10066369 238928 0 None -22 6 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 238928 0 None -22 6 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
162658421 354960 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4760150 354960 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
12739458 138841 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 227 2 0 1 3.5 c1ccc(CN2C3CC4CC(C3)CC2C4)cc1 10.1016/j.bmcl.2011.07.028
CHEMBL1852447 138841 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 227 2 0 1 3.5 c1ccc(CN2C3CC4CC(C3)CC2C4)cc1 10.1016/j.bmcl.2011.07.028
71459971 155170 0 None -1 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 437 6 0 5 4.4 COc1ccc([S@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114066 155170 0 None -1 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 437 6 0 5 4.4 COc1ccc([S@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
214124 334260 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL443780 334260 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10204457 469309 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71971 469309 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
164625419 371786 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 504 8 2 6 3.0 NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028881 371786 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 504 8 2 6 3.0 NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015254 352202 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650938 352202 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
70683405 156146 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027984 156146 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
44415886 161297 0 None -74 4 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212141 161297 0 None -74 4 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
44439390 294496 0 None -398 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 4 2 3 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL393275 294496 0 None -398 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 4 2 3 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
70682037 157546 24 None -29 9 Human 6.7 pKi = 6.7 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.6019/CHEMBL5442175
CHEMBL2048820 157546 24 None -29 9 Human 6.7 pKi = 6.7 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.6019/CHEMBL5442175
10066972 199001 0 None -5 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278074 199001 0 None -5 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
109035056 355175 0 None -29 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 331 4 1 3 4.0 O=C(CCN1CCCc2ccccc21)Nc1cccc2cccnc12 10.1016/j.bmcl.2020.127632
CHEMBL4762755 355175 0 None -29 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 331 4 1 3 4.0 O=C(CCN1CCCc2ccccc21)Nc1cccc2cccnc12 10.1016/j.bmcl.2020.127632
162353378 366286 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
CHEMBL4792360 366286 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
177372529 393582 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 347 3 0 5 3.0 CN1[C@@H]2C[C@@H](Oc3nc4ccccc4n3-c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1016/j.ejmech.2023.115891
CHEMBL5639538 393582 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 347 3 0 5 3.0 CN1[C@@H]2C[C@@H](Oc3nc4ccccc4n3-c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1016/j.ejmech.2023.115891
71575447 177081 0 None -31 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312361 177081 0 None -31 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
1688 296777 35 None -2 16 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
6075 296777 35 None -2 16 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 296777 35 None -2 16 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44593626 371077 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 371077 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44627852 28280 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197387 28280 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
11071537 60170 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL136027 60170 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
164609510 371669 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 817 21 11 10 0.5 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027965 371669 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 817 21 11 10 0.5 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
10651844 234429 0 None 2 4 Rat 7.7 pKi = 7.7 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL335115 234429 0 None 2 4 Rat 7.7 pKi = 7.7 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
2274 6448 36 None -8 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 6448 36 None -8 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 6448 36 None -8 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 6448 36 None -8 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 6448 36 None -8 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10105296 470723 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 470723 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
10982070 19505 0 None 2 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105945 19505 0 None 2 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
177381476 391796 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-epibatidine from M4 receptor (unknown origin)Displacement of [3H]-epibatidine from M4 receptor (unknown origin)
ChEMBL 283 2 1 1 5.2 CC1=CC[C@@H]2C[C@H]1[C@H](c1ccc(C(C)C)cc1)NC2(C)C 10.1021/acs.jmedchem.3c01758
CHEMBL5574911 391796 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-epibatidine from M4 receptor (unknown origin)Displacement of [3H]-epibatidine from M4 receptor (unknown origin)
ChEMBL 283 2 1 1 5.2 CC1=CC[C@@H]2C[C@H]1[C@H](c1ccc(C(C)C)cc1)NC2(C)C 10.1021/acs.jmedchem.3c01758
44439410 293986 0 None -5 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 280 4 1 2 3.5 CN(/C=N/c1ccc2c(c1)C(O)CC2)Cc1ccccc1 10.1016/j.bmcl.2007.01.093
CHEMBL392888 293986 0 None -5 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 280 4 1 2 3.5 CN(/C=N/c1ccc2c(c1)C(O)CC2)Cc1ccccc1 10.1016/j.bmcl.2007.01.093
11759379 239406 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355392 239406 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
2599 116531 16 None -5 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
5404 116531 16 None -5 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1714574 116531 16 None -5 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
57664418 275676 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3770870 275676 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
44299599 327683 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL430587 327683 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
164621085 371751 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 830 17 8 11 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028630 371751 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 830 17 8 11 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10916286 19441 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
CHEMBL105593 19441 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
1692 4398 23 None -239 15 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442175
5311340 4398 23 None -239 15 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442175
CHEMBL140979 4398 23 None -239 15 Human 5.7 pKi = 5.7 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442175
156015895 352196 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650874 352196 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
137655636 314602 0 None -93 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 314602 0 None -93 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
11024241 238969 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352723 238969 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
156011112 352190 0 None -10 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650842 352190 0 None -10 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
156015809 352233 0 None -10 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651096 352233 0 None -10 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
164612852 371687 0 None -15 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028161 371687 0 None -15 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164622945 371764 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 646 14 6 7 3.6 N=C(N)NCCC[C@@H](NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL5028723 371764 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 646 14 6 7 3.6 N=C(N)NCCC[C@@H](NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
155550632 350494 0 None -32 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597071 350494 0 None -32 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
155566290 350543 0 None -25 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597498 350543 0 None -25 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
156015807 352214 0 None -4 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 352214 0 None -4 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
277 2680 45 None -8 34 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 2680 45 None -8 34 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 2680 45 None -8 34 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 2680 45 None -8 34 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 2680 45 None -8 34 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
10180872 203179 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL307810 203179 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
155541812 347163 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
CHEMBL4519301 347163 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
10919522 160413 0 None -9 5 Human 8.6 pKi = 8.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
CHEMBL2112957 160413 0 None -9 5 Human 8.6 pKi = 8.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
16115951 270612 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL385328 270612 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
57326326 158817 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078942 158817 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
57326326 158817 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078942 158817 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
156020548 352098 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4649224 352098 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
155554568 350572 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597724 350572 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
9913341 163586 3 None 3 5 Human 8.6 pKi = 8.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 163586 3 None 3 5 Human 8.6 pKi = 8.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
122203596 311736 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
CHEMBL4059733 311736 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
164627113 371798 0 None -13 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 489 7 2 5 4.2 NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028981 371798 0 None -13 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 489 7 2 5 4.2 NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
9913341 163586 3 None 3 5 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 163586 3 None 3 5 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
155525097 335494 0 None -32 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4455570 335494 0 None -32 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
156015900 352236 0 None -10 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651104 352236 0 None -10 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
171343805 386073 0 None 1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.7 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
CHEMBL5268503 386073 0 None 1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.7 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
42596929 158827 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079021 158827 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
162645430 366961 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802409 366961 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
164615275 371710 0 None -17 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 20 9 11 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028304 371710 0 None -17 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 20 9 11 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155535606 336579 0 None -7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
CHEMBL4471882 336579 0 None -7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
162649253 366979 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4802611 366979 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
26987 1955 32 None -38 21 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 1955 32 None -38 21 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 1955 32 None -38 21 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 1955 32 None -38 21 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 1955 32 None -38 21 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10771937 45532 0 None -5 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL131846 45532 0 None -5 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
164628352 371807 0 None -9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 630 13 5 6 4.0 N=C(N)NCCCCC(=O)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029051 371807 0 None -9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 630 13 5 6 4.0 N=C(N)NCCCCC(=O)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015978 352238 0 None -4 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 352238 0 None -4 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
16086001 276541 0 None -117 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL378772 276541 0 None -117 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
44439398 182025 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 5 0 5 4.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240022 182025 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 5 0 5 4.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCC3)CC2 10.1016/j.bmcl.2007.01.093
44439403 182583 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL241102 182583 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
44439399 294092 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 5 0 5 4.8 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL392970 294092 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 5 0 5 4.8 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
57664418 275676 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3770870 275676 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
44439401 182582 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 395 4 0 5 3.6 COC(=O)N1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241101 182582 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 395 4 0 5 3.6 COC(=O)N1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
156308 333878 4 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 354 2 0 4 3.2 COc1ccc2c(c1OC)C[N+]1(C)CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmcl.2007.01.093
CHEMBL441356 333878 4 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 354 2 0 4 3.2 COc1ccc2c(c1OC)C[N+]1(C)CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmcl.2007.01.093
177372528 393565 0 None -4 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 333 3 0 4 4.0 CN1[C@@H]2CC[C@H]1C[C@@H](Oc1nc3ccccc3n1-c1ccccc1)C2 10.1016/j.ejmech.2023.115891
CHEMBL5639287 393565 0 None -4 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 333 3 0 4 4.0 CN1[C@@H]2CC[C@H]1C[C@@H](Oc1nc3ccccc3n1-c1ccccc1)C2 10.1016/j.ejmech.2023.115891
155551903 350424 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596435 350424 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
10236758 234707 4 None -213 13 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 234707 4 None -213 13 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
44593623 371103 0 None -6 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 371103 0 None -6 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
92218234 239453 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
CHEMBL3558072 239453 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
15157140 200059 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285898 200059 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44568347 374712 0 None 3 15 Human 7.7 pKi = 7.7 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 374712 0 None 3 15 Human 7.7 pKi = 7.7 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
2726 1895 54 None -14 48 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None -14 48 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None -14 48 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None -14 48 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None -14 48 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
15050955 202660 0 None -2 4 Rat 6.7 pKi = 6.7 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL304112 202660 0 None -2 4 Rat 6.7 pKi = 6.7 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
167434636 392325 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M4 receptor assessed as inhibition constantBinding affinity to human M4 receptor assessed as inhibition constant
ChEMBL 397 3 0 7 2.7 Cc1ncc(S(=O)(=O)N2CCC(c3cn4ncnc4cc3Cl)CC2)s1 10.1021/acs.jmedchem.4c01193
CHEMBL5594532 392325 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M4 receptor assessed as inhibition constantBinding affinity to human M4 receptor assessed as inhibition constant
ChEMBL 397 3 0 7 2.7 Cc1ncc(S(=O)(=O)N2CCC(c3cn4ncnc4cc3Cl)CC2)s1 10.1021/acs.jmedchem.4c01193
36014865 366057 1 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
CHEMBL4789054 366057 1 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
164608958 371664 0 None -19 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164621861 371664 0 None -19 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027936 371664 0 None -19 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028673 371664 0 None -19 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
162675053 366606 0 None -3 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
CHEMBL4796491 366606 0 None -3 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
44274400 199173 0 None 1 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279520 199173 0 None 1 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
162667844 356351 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4787283 356351 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
24894625 24081 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL113580 24081 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
1482 367203 61 None 1 2 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
60838 367203 61 None 1 2 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 367203 61 None 1 2 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
DB00762 367203 61 None 1 2 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
135398745 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1982 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
4585 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 5933 69 None -16 45 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
145961161 317146 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129580 317146 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
2090 389838 56 None -6 10 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
4735 389838 56 None -6 10 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 389838 56 None -6 10 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
DB00738 389838 56 None -6 10 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
15050941 468661 0 None 1 4 Rat 6.7 pKi = 6.7 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67381 468661 0 None 1 4 Rat 6.7 pKi = 6.7 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
2337 6622 53 None -21 36 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 6622 53 None -21 36 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 6622 53 None -21 36 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 6622 53 None -21 36 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 6622 53 None -21 36 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
44318766 470567 0 None 3 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 470567 0 None 3 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
10262466 198619 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL275104 198619 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
44274468 162060 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21508 162060 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
44448498 26608 0 None 1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185287 26608 0 None 1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
2750 64617 55 None -1 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
6604850 64617 55 None -1 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL1398683 64617 55 None -1 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 64617 55 None -1 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
DB09201 64617 55 None -1 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(C[C@H]3SC(=O)NC3=O)cc2)CCCCC1 nan
44437308 26596 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
CHEMBL1185188 26596 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
44448496 26186 0 None -3 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182637 26186 0 None -3 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
9308 41623 17 None -10 7 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL12587 41623 17 None -10 7 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
15050953 202421 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL303684 202421 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
155516383 350633 0 None -5 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598230 350633 0 None -5 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
1548953 473104 29 None -1 17 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 473104 29 None -1 17 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
DB06735 473104 29 None -1 17 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
44318929 216521 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 216521 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
71463061 174782 0 None -3 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 174782 0 None -3 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
44627958 28277 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197374 28277 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
10880435 121842 0 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169494 121842 0 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
2551 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
298 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
488 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
5831 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
CHEMBL965 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
DB00411 1644 11 None -38 11 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
16086005 276556 0 None -19 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378859 276556 0 None -19 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
164616974 371721 0 None -9 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 675 15 7 8 2.2 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028407 371721 0 None -9 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 675 15 7 8 2.2 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2230 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
296 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
CHEMBL7303 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
DB04365 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
2230 961 44 None -562 10 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 961 44 None -562 10 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 961 44 None -562 10 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 961 44 None -562 10 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
2230 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 961 44 None -436 10 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
44326733 221123 0 None -2691 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 2 2 3 3.3 c1ccc2c3c([nH]c2c1)C(Cc1ccc2c(c1)OCO2)NCC3 10.1016/j.bmcl.2007.01.093
CHEMBL328476 221123 0 None -2691 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 2 2 3 3.3 c1ccc2c3c([nH]c2c1)C(Cc1ccc2c(c1)OCO2)NCC3 10.1016/j.bmcl.2007.01.093
191 833 62 None -20 26 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 833 62 None -20 26 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 833 62 None -20 26 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 833 62 None -20 26 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 833 62 None -20 26 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
177372530 393580 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 282 3 0 3 3.3 CN1CC(OC(=O)N(c2ccccc2)c2ccccc2)C1 10.1016/j.ejmech.2023.115891
CHEMBL5639510 393580 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 282 3 0 3 3.3 CN1CC(OC(=O)N(c2ccccc2)c2ccccc2)C1 10.1016/j.ejmech.2023.115891
44578707 355972 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2008.06.025
CHEMBL478227 355972 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2008.06.025
9817231 314114 23 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
CHEMBL4088272 314114 23 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
44274433 199709 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL283320 199709 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
24894632 365952 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
CHEMBL513277 365952 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
135413563 241495 20 None -1 8 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.6019/CHEMBL5442175
CHEMBL360648 241495 20 None -1 8 Human 6.6 pKi = 6.6 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.6019/CHEMBL5442175
155562285 349821 0 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4585326 349821 0 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
44418764 163587 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 163587 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
25025581 465490 0 None -3 8 Human 6.6 pKi = 6.6 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
CHEMBL608151 465490 0 None -3 8 Human 6.6 pKi = 6.6 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
164617938 371729 0 None -17 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028470 371729 0 None -17 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015968 352160 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650620 352160 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
6604789 201185 9 None -100 10 Human 4.6 pKi = 4.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL294649 201185 9 None -100 10 Human 4.6 pKi = 4.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
57326140 158818 0 None -3 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2078962 158818 0 None -3 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
155528270 350359 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595943 350359 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
47358375 354630 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756164 354630 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
44593620 371158 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 371158 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
145961981 317072 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128497 317072 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
15050950 469008 0 None -3 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70003 469008 0 None -3 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
164614732 371702 0 None -10 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 519 7 3 7 1.1 NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028266 371702 0 None -10 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 519 7 3 7 1.1 NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162658112 354932 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4759774 354932 0 None -1 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
46227483 38045 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198039 38045 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
49783415 41547 0 None -3467 13 Human 5.6 pKi = 5.6 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 41547 0 None -3467 13 Human 5.6 pKi = 5.6 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
2247 1042 63 None -17 37 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None -17 37 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None -17 37 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None -17 37 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None -17 37 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2230 961 44 None -436 10 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
296 961 44 None -436 10 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
CHEMBL7303 961 44 None -436 10 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
DB04365 961 44 None -436 10 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
154734599 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
327 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
4108 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
CHEMBL27673 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
118719920 234708 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354066 234708 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
154734599 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
327 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
4108 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL27673 5087 6 None -2 9 Rat 7.6 pKi = 7.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL306462 203015 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 211 2 1 4 1.1 CCO/C(O)=C1\CN2CCCC(C2)C1=O 10.1021/jm020572p
2551 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
298 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
488 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
5831 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
CHEMBL965 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
DB00411 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
2551 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
5831 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 1644 11 None -2 11 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
5831 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 1644 11 None -38 11 Human 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
137644962 314364 0 None -131 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 314364 0 None -131 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
132060776 317895 0 None -9 16 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 317895 0 None -9 16 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
44448380 26189 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182644 26189 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
122387444 275573 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3769740 275573 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
10870954 238978 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL352779 238978 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
155560013 350269 0 None -6 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595198 350269 0 None -6 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL69452 468936 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
122387444 275573 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3769740 275573 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
145961126 317093 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128764 317093 0 None -4 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
1210 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
5281070 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1200927 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB09555 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 1893 53 None -9 16 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2338 461820 42 None -1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
237 461820 42 None -1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 461820 42 None -1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
DB01103 461820 42 None -1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
147326216 389070 0 None -2 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to M4 receptor (unknown origin) assessed as inhibition constantBinding affinity to M4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 424 10 2 6 4.3 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
CHEMBL5431371 389070 0 None -2 15 Human 6.6 pKi = 6.6 Binding
Binding affinity to M4 receptor (unknown origin) assessed as inhibition constantBinding affinity to M4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 424 10 2 6 4.3 CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1 10.1021/acs.jmedchem.2c01769
73347827 183352 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432052 183352 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
44439402 333963 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 2 1 2 3.4 OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL442093 333963 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 2 1 2 3.4 OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
9308 41623 17 None -10 7 Human 4.6 pKi = 4.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 41623 17 None -10 7 Human 4.6 pKi = 4.6 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
44593622 371025 0 None -5 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 371025 0 None -5 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
24894635 327814 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL443939 327814 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
611101 468856 2 None -2 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL68771 468856 2 None -2 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
73353378 180631 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
CHEMBL2377268 180631 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
71463022 174688 7 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
CHEMBL2205362 174688 7 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
135 5144 38 None -30 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 5144 38 None -30 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 5144 38 None -30 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 5144 38 None -30 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 5144 38 None -30 42 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
109014373 353689 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4744856 353689 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
44448646 26182 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182612 26182 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
16085999 161748 0 None -60 5 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214029 161748 0 None -60 5 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
155513986 350454 0 None -17 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596667 350454 0 None -17 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
135409468 4159 52 None -5 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 4159 52 None -5 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 4159 52 None -5 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
16086004 276562 0 None -77 3 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL378885 276562 0 None -77 3 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
11751922 145283 22 None -5 2 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 477 4 2 7 4.7 CC(C)Cn1c2ccc(Nc3ncccn3)cc2c2c3c(c4c(c21)CCc1nn(C)cc1-4)C(=O)NC3 10.1021/jm201449n
CHEMBL2010872 145283 22 None -5 2 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 477 4 2 7 4.7 CC(C)Cn1c2ccc(Nc3ncccn3)cc2c2c3c(c4c(c21)CCc1nn(C)cc1-4)C(=O)NC3 10.1021/jm201449n
CHEMBL4520788 478301 14 None -13 26 Human 6.5 pKi = 6.5 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
15050946 202706 0 None -1 4 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL304391 202706 0 None -1 4 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
10104 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
12963076 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
21855 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
6604866 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
903 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL1493369 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL22108 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL564226 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
DB08801 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
155552923 350276 0 None -6 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595245 350276 0 None -6 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
164627658 371803 0 None -72 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029013 371803 0 None -72 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164628906 371810 0 None -56 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029079 371810 0 None -56 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
57326146 158826 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079020 158826 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
7141656 350796 3 None -9 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
CHEMBL461089 350796 3 None -9 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
3198 461850 54 None -8 34 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None -8 34 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None -8 34 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None -8 34 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
71452384 174784 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 174784 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 174784 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 174784 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
1402 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
154417 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
174174 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
260 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
320 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
CHEMBL1331216 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
CHEMBL517712 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
DB00424 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
DB00572 1082 53 None -1 16 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
10949838 19559 0 None 72 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106218 19559 0 None 72 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10225881 217254 0 None 112 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL318995 217254 0 None 112 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
164627445 371801 0 None -14 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028997 371801 0 None -14 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2705 8363 46 None -1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
360 8363 46 None -1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
443879 8363 46 None -1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
CHEMBL1382 8363 46 None -1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
DB01036 8363 46 None -1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
2705 8363 46 None -1 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
360 8363 46 None -1 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
443879 8363 46 None -1 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
CHEMBL1382 8363 46 None -1 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
DB01036 8363 46 None -1 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
164626501 371792 0 None -17 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCNC(=N)N)N[C@@H](CCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028936 371792 0 None -17 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCNC(=N)N)N[C@@H](CCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155539713 350329 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595691 350329 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
171344930 386714 0 None 1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1024 19 1 13 9.4 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
CHEMBL5283759 386714 0 None 1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1024 19 1 13 9.4 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
16115950 273827 0 None 1 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL373515 273827 0 None 1 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
164611865 371680 0 None -41 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028107 371680 0 None -41 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16115801 26565 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184882 26565 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
164618444 371732 0 None -16 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 21 9 11 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028499 371732 0 None -16 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 21 9 11 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2774 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
688595 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1457550 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 8415 68 None 1 5 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
155543944 350303 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595467 350303 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
2028 6066 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
359 6066 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
4634 6066 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
CHEMBL1231 6066 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
DB01062 6066 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
137628879 316534 0 None -5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4115977 316534 0 None -5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
2800 159972 9 None -1 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
5648 159972 9 None -1 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 159972 9 None -1 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
DB13497 159972 9 None -1 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
162677513 367077 0 None -2 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4803695 367077 0 None -2 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
171351069 386047 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.8 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
CHEMBL5267836 386047 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.8 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
164616463 371717 0 None -36 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 860 22 9 12 0.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)NC(=O)[C@@H](N)CCCN 10.1016/j.ejmech.2021.113159
CHEMBL5028381 371717 0 None -36 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 860 22 9 12 0.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)NC(=O)[C@@H](N)CCCN 10.1016/j.ejmech.2021.113159
164628529 371808 0 None -18 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 914 17 9 12 0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL5029058 371808 0 None -18 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 914 17 9 12 0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
164616706 371718 0 None -6 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028391 371718 0 None -6 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015153 352222 0 None -2 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651018 352222 0 None -2 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
44627853 404289 0 None -3 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571121 404289 0 None -3 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
10862395 19365 0 None 22 5 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105148 19365 0 None 22 5 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
11767229 160412 0 None -30 5 Human 7.5 pKi = 7.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112956 160412 0 None -30 5 Human 7.5 pKi = 7.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
156015390 352157 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650585 352157 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
44439408 182027 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 426 4 0 5 4.9 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1C3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240024 182027 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 426 4 0 5 4.9 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1C3)CC2 10.1016/j.bmcl.2007.01.093
9950396 291860 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 352 4 1 4 3.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL391192 291860 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 352 4 1 4 3.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CC3)CC2 10.1016/j.bmcl.2007.01.093
11773414 293982 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 380 4 1 4 4.2 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL392887 293982 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 380 4 1 4 4.2 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
44318930 215852 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 215852 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
11184481 463277 22 None 1 4 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
CHEMBL604798 463277 22 None 1 4 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
156013387 352176 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650725 352176 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
46227485 38043 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198034 38043 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
44593626 371077 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 371077 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL4520788 478301 14 None -13 26 Human 6.5 pKi = 6.5 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
CHEMBL4520788 478301 14 None -13 26 Human 6.5 pKi = 6.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM4
ChEMBL 448 8 2 7 5.6 CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
164622170 371759 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 846 20 9 12 -0.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028687 371759 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 846 20 9 12 -0.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44627856 394574 0 None -2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569953 394574 0 None -2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
46227413 38059 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
CHEMBL1198087 38059 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
11828362 160415 0 None -40 5 Human 7.5 pKi = 7.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112959 160415 0 None -40 5 Human 7.5 pKi = 7.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
16086062 162239 0 None -58 5 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215189 162239 0 None -58 5 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
9909908 27773 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL1193635 27773 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
10373706 120204 0 None -6 4 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL165220 120204 0 None -6 4 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
44593624 371349 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 371349 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44593616 384952 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 384952 0 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
122387449 275625 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770360 275625 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
137636308 312126 0 None -10 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 312126 0 None -10 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
2736067 178396 47 None -371 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335158 178396 47 None -371 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
177372523 393593 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 307 3 0 4 3.5 CN1CCC(Oc2nc3ccccc3n2-c2ccccc2)CC1 10.1016/j.ejmech.2023.115891
CHEMBL5639729 393593 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 307 3 0 4 3.5 CN1CCC(Oc2nc3ccccc3n2-c2ccccc2)CC1 10.1016/j.ejmech.2023.115891
2381 1364 33 None -13 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
374 1364 33 None -13 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
7128 1364 33 None -13 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL1101 1364 33 None -13 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
DB00810 1364 33 None -13 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
118719931 234720 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
CHEMBL3354078 234720 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
154734599 5087 6 None -2 9 Rat 7.5 pKi = 7.5 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
327 5087 6 None -2 9 Rat 7.5 pKi = 7.5 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
4108 5087 6 None -2 9 Rat 7.5 pKi = 7.5 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
CHEMBL27673 5087 6 None -2 9 Rat 7.5 pKi = 7.5 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
122387449 275625 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770360 275625 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
11833737 239002 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352966 239002 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
164615651 371714 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164623530 371714 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028329 371714 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028763 371714 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
9815331 468153 1 None -4 8 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 468153 1 None -4 8 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
9815331 468153 1 None -12 8 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 468153 1 None -12 8 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9815331 468153 1 None -4 8 Human 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 468153 1 None -4 8 Human 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
44627860 28276 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197371 28276 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593619 370697 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 370697 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
2200 6369 35 None -7 11 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
328 6369 35 None -7 11 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
4848 6369 35 None -7 11 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
CHEMBL9967 6369 35 None -7 11 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
DB00670 6369 35 None -7 11 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
11759212 120684 0 None -407 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL167223 120684 0 None -407 6 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
44274317 164782 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21937 164782 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
2068 370177 47 None -26 8 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
43815 370177 47 None -26 8 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 370177 47 None -26 8 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
DB00715 370177 47 None -26 8 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
2200 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
328 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
4848 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
CHEMBL9967 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
DB00670 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
2200 6369 35 None -3 11 Human 7.5 pKi = 7.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
328 6369 35 None -3 11 Human 7.5 pKi = 7.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
4848 6369 35 None -3 11 Human 7.5 pKi = 7.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
CHEMBL9967 6369 35 None -3 11 Human 7.5 pKi = 7.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
DB00670 6369 35 None -3 11 Human 7.5 pKi = 7.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
2200 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
328 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
4848 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
CHEMBL9967 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
DB00670 6369 35 None -7 11 Rat 7.5 pKi = 7.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
156021441 352074 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4648939 352074 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
424430 217262 5 None -1318 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 3 2 2 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL319005 217262 5 None -1318 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 3 2 2 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
9906447 390580 2 None -478 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 390580 2 None -478 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
73355415 183341 0 None -1 13 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 183341 0 None -1 13 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
164623942 371776 0 None -26 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 11 10 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028796 371776 0 None -26 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 11 10 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44593618 370696 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 370696 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
73352415 183346 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432044 183346 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
2335 26122 15 None 1 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
3018 26122 15 None 1 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 26122 15 None 1 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
DB11125 26122 15 None 1 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
10557581 45609 0 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL131913 45609 0 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
3000322 7238 26 None -8 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm301774u
330 7238 26 None -8 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm301774u
CHEMBL569713 7238 26 None -8 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm301774u
DB00747 7238 26 None -8 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1021/jm301774u
164619478 371742 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 533 8 3 7 1.5 NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028552 371742 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 533 8 3 7 1.5 NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
11101362 19464 0 None 7 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
CHEMBL105674 19464 0 None 7 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
2436 470362 35 None -7 14 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
68617 470362 35 None -7 14 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 470362 35 None -7 14 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
DB01104 470362 35 None -7 14 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
9872676 159773 0 None -9332 17 Human 5.4 pKi = 5.4 Binding
Binding affinity to human M4 receptorBinding affinity to human M4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 159773 0 None -9332 17 Human 5.4 pKi = 5.4 Binding
Binding affinity to human M4 receptorBinding affinity to human M4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
155557119 350476 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596899 350476 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
11011757 122004 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
CHEMBL170221 122004 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
44627956 28275 0 None -7 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197362 28275 0 None -7 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
156015465 352239 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651115 352239 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
154734599 5087 6 None -6 9 Human 7.4 pKi = 7.4 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
327 5087 6 None -6 9 Human 7.4 pKi = 7.4 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
4108 5087 6 None -6 9 Human 7.4 pKi = 7.4 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
CHEMBL27673 5087 6 None -6 9 Human 7.4 pKi = 7.4 Binding
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
3055 2955 32 None -1 9 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 2955 32 None -1 9 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 2955 32 None -1 9 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 2955 32 None -1 9 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 2955 32 None -1 9 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
164611187 371674 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 17 8 9 1.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028060 371674 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 17 8 9 1.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44627748 38014 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197705 38014 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
156015051 352243 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651139 352243 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
156009660 352244 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4651150 352244 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
73355419 183357 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 4 0 2 2.7 CN(CCc1ccccn1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432059 183357 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 4 0 2 2.7 CN(CCc1ccccn1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
11536903 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
3262 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
CHEMBL3770346 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
118719927 234716 0 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 234716 0 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
10104 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
12963076 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
21855 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
6604866 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
903 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL1493369 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL22108 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL564226 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
DB08801 7246 46 None -58 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
156011518 352253 0 None -5 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651208 352253 0 None -5 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
16086060 333573 0 None -100 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL438822 333573 0 None -100 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
3652 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
155557119 350476 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596899 350476 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164620907 371750 0 None -47 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028619 371750 0 None -47 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10486393 278903 0 None -43 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL385625 278903 0 None -43 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
3652 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 8876 57 None -3 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
10033774 119345 0 None 1 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL163901 119345 0 None 1 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
73349362 183358 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432060 183358 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
2551 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
5831 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
156012936 352211 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650969 352211 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
2551 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
5831 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 1644 11 None -38 11 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
10474335 387172 20 None -138 10 Human 5.4 pKi = 5.4 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 387172 20 None -138 10 Human 5.4 pKi = 5.4 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
156015719 352173 0 None -7 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650699 352173 0 None -7 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
9815331 468153 1 None -4 8 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 468153 1 None -4 8 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
164619001 371739 0 None -14 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 887 22 9 11 2.3 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028529 371739 0 None -14 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 887 22 9 11 2.3 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164610955 371673 0 None -15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 661 15 6 8 2.3 N=C(N)NCCC[C@@H](NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL5028048 371673 0 None -15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 661 15 6 8 2.3 N=C(N)NCCC[C@@H](NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
44627858 28279 0 None -6 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197382 28279 0 None -6 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
162654942 367005 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802913 367005 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
10316726 26300 0 None -8 4 Human 8.4 pKi = 8.4 Binding
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 26300 0 None -8 4 Human 8.4 pKi = 8.4 Binding
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
164617401 371723 0 None -12 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 900 16 9 12 -0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL5028427 371723 0 None -12 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 900 16 9 12 -0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
156016041 352162 0 None -5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650627 352162 0 None -5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
15157138 199819 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL284137 199819 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10316726 26300 0 None -8 4 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 26300 0 None -8 4 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
56965018 158820 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078967 158820 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
44428745 182968 0 None -6 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
CHEMBL242345 182968 0 None -6 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
164618698 371736 0 None -43 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028512 371736 0 None -43 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
11536903 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
3262 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
CHEMBL3770346 4875 52 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
57339144 183047 56 None -5 7 Human 6.4 pKi = 6.4 Binding
Inhibition of M4 receptor (unknown origin) by radioligand binding assayInhibition of M4 receptor (unknown origin) by radioligand binding assay
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.1038/nchembio.1157
CHEMBL2426364 183047 56 None -5 7 Human 6.4 pKi = 6.4 Binding
Inhibition of M4 receptor (unknown origin) by radioligand binding assayInhibition of M4 receptor (unknown origin) by radioligand binding assay
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.1038/nchembio.1157
57339144 183047 56 None -5 7 Human 6.4 pKi = 6.4 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
CHEMBL2426364 183047 56 None -5 7 Human 6.4 pKi = 6.4 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
73346332 183343 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432041 183343 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
107867 6054 42 None -9 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
309 6054 42 None -9 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
CHEMBL17045 6054 42 None -9 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
10104 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
12963076 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
21855 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
6604866 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
903 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL1493369 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL22108 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL564226 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
DB08801 7246 46 None -58 6 Human 6.4 pKi = 6.4 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1016/s0960-894x(01)00186-x
44593617 370668 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 370668 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
162353382 355576 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
CHEMBL4777127 355576 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
16086000 161811 0 None -79 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL214342 161811 0 None -79 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
11766733 311684 0 None -95 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL405739 311684 0 None -95 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
10421982 470831 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 470831 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
56963799 156563 0 None -1047 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 156563 0 None -1047 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
155565286 350235 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 18 6 8 2.7 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595003 350235 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 18 6 8 2.7 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
11012712 120622 2 None -3 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL167027 120622 2 None -3 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
10969696 259986 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL369575 259986 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
16086059 162223 0 None -134 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
CHEMBL215180 162223 0 None -134 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
2284 6466 25 None -9 23 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 6466 25 None -9 23 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 6466 25 None -9 23 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 6466 25 None -9 23 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 6466 25 None -9 23 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44318929 216521 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 216521 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
16086059 162223 0 None -134 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 162223 0 None -134 5 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
44593618 370696 0 None -5 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 370696 0 None -5 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44439387 182516 0 None -52 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 276 2 1 2 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL240888 182516 0 None -52 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 276 2 1 2 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
164622017 371757 0 None -47 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028681 371757 0 None -47 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
122387448 275684 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770968 275684 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
11006792 160417 0 None -19 5 Human 7.4 pKi = 7.4 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112961 160417 0 None -19 5 Human 7.4 pKi = 7.4 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
137408738 374297 3 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assayDisplacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 374297 3 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assayDisplacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
44517677 390257 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 326 4 1 2 3.3 O=C(c1ccccc1C(F)(F)F)N(CC1CCC1)[C@H]1CCNC1 10.1016/j.bmcl.2009.06.096
CHEMBL552338 390257 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 326 4 1 2 3.3 O=C(c1ccccc1C(F)(F)F)N(CC1CCC1)[C@H]1CCNC1 10.1016/j.bmcl.2009.06.096
122387448 275684 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770968 275684 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
10969390 122455 0 None -60 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL172233 122455 0 None -60 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
145963288 317155 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129723 317155 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
109018479 355657 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
CHEMBL4778178 355657 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
24894630 372135 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL508347 372135 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
9901086 370865 25 None -147 15 Human 6.4 pKi = 6.4 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442175
CHEMBL494947 370865 25 None -147 15 Human 6.4 pKi = 6.4 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442175
24882532 195491 0 None -35 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 195491 0 None -35 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
1800 473856 65 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
118719926 234715 0 None -102 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 234715 0 None -102 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
44593619 370697 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 370697 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
46227457 38054 0 None -2 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1198075 38054 0 None -2 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
71454562 161129 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115126 161129 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44318736 216674 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 216674 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
44439409 182028 0 None -44 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL240025 182028 0 None -44 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
44439407 332197 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 424 8 0 4 5.9 CCCCSC1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL429644 332197 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 424 8 0 4 5.9 CCCCSC1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
124 6070 37 None -54 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 6070 37 None -54 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 6070 37 None -54 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 6070 37 None -54 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 6070 37 None -54 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
11834199 121558 0 None -10 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL168704 121558 0 None -10 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
164614830 371704 0 None -32 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164627253 371704 0 None -32 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028275 371704 0 None -32 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028989 371704 0 None -32 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44422697 26126 0 None -8 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182277 26126 0 None -8 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
11498 6149 38 None 19 13 Human 7.3 pKi = 7.3 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.6019/CHEMBL5442175
4995951 6149 38 None 19 13 Human 7.3 pKi = 7.3 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.6019/CHEMBL5442175
CHEMBL59898 6149 38 None 19 13 Human 7.3 pKi = 7.3 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.6019/CHEMBL5442175
44593624 371349 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 371349 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
164615651 371714 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164623530 371714 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028329 371714 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028763 371714 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44274417 199132 0 None -5 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279225 199132 0 None -5 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
11523051 193610 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
CHEMBL261194 193610 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
11759058 239474 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355851 239474 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
124087 2860 75 None -10 15 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 2860 75 None -10 15 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 2860 75 None -10 15 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 2860 75 None -10 15 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 2860 75 None -10 15 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
71452382 174781 0 None -14 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 174781 0 None -14 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44448538 26687 0 None -1 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185855 26687 0 None -1 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
24894516 346843 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL450463 346843 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
44318736 216674 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 216674 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
16086064 161421 0 None -93 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212645 161421 0 None -93 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
16086003 161885 0 None -114 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL214642 161885 0 None -114 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
1212 3415 38 None -30 41 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 3415 38 None -30 41 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 3415 38 None -30 41 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 3415 38 None -30 41 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 3415 38 None -30 41 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
171357345 386435 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 930 19 2 5 13.0 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5277670 386435 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 930 19 2 5 13.0 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
3158 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
667468 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
956 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
CHEMBL101740 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
CHEMBL1628227 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
DB01142 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
DB14750 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 nan
177372531 393650 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 336 3 0 3 4.6 CN1[C@@H]2CC[C@H]1C[C@H](OC(=O)N(c1ccccc1)c1ccccc1)C2 10.1016/j.ejmech.2023.115891
CHEMBL5641756 393650 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 336 3 0 3 4.6 CN1[C@@H]2CC[C@H]1C[C@H](OC(=O)N(c1ccccc1)c1ccccc1)C2 10.1016/j.ejmech.2023.115891
10030021 334444 16 None -6 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4440484 334444 16 None -6 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
10105296 470723 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 470723 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
2106 461821 25 None 1 4 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
4746 461821 25 None 1 4 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 461821 25 None 1 4 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
DB01074 461821 25 None 1 4 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
154156695 451676 3 None -1 2 Human 5.3 pKi = 5.3 Binding
New CNS Specificity Data for AK3-238 (FA44) and AK3-99B (FA26): Two exemplary compounds, FA44 and FA26, were screened against a panel of CNS receptors, transporters, and ion channels to examine specificity for CLC-2 in the brain. A comprehensive primary binding assay screen was performed through the NIH Psychoactive Drug Screening Program (PDSP) at UNC-Chapel Hill. Secondary or functional assays were performed for compounds showing >50% activity in the primary assay.New CNS Specificity Data for AK3-238 (FA44) and AK3-99B (FA26): Two exemplary compounds, FA44 and FA26, were screened against a panel of CNS receptors, transporters, and ion channels to examine specificity for CLC-2 in the brain. A comprehensive primary binding assay screen was performed through the NIH Psychoactive Drug Screening Program (PDSP) at UNC-Chapel Hill. Secondary or functional assays were performed for compounds showing >50% activity in the primary assay.
ChEMBL 387 6 2 3 6.0 O=C(O)c1ccccc1Nc1c(Cl)ccc(OCc2ccccc2)c1Cl nan
CHEMBL6028327 451676 3 None -1 2 Human 5.3 pKi = 5.3 Binding
New CNS Specificity Data for AK3-238 (FA44) and AK3-99B (FA26): Two exemplary compounds, FA44 and FA26, were screened against a panel of CNS receptors, transporters, and ion channels to examine specificity for CLC-2 in the brain. A comprehensive primary binding assay screen was performed through the NIH Psychoactive Drug Screening Program (PDSP) at UNC-Chapel Hill. Secondary or functional assays were performed for compounds showing >50% activity in the primary assay.New CNS Specificity Data for AK3-238 (FA44) and AK3-99B (FA26): Two exemplary compounds, FA44 and FA26, were screened against a panel of CNS receptors, transporters, and ion channels to examine specificity for CLC-2 in the brain. A comprehensive primary binding assay screen was performed through the NIH Psychoactive Drug Screening Program (PDSP) at UNC-Chapel Hill. Secondary or functional assays were performed for compounds showing >50% activity in the primary assay.
ChEMBL 387 6 2 3 6.0 O=C(O)c1ccccc1Nc1c(Cl)ccc(OCc2ccccc2)c1Cl nan
44439397 182024 0 None -22 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 437 4 0 5 4.7 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)N(C(=O)OC(C)(C)C)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240021 182024 0 None -22 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 437 4 0 5 4.7 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)N(C(=O)OC(C)(C)C)CC3)CC2 10.1016/j.bmcl.2007.01.093
44593621 384959 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 384959 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
162353376 354304 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 3 1 3 1.4 O=C(CCN1CCCc2ccccc21)N1CCC(O)C1 10.1016/j.bmcl.2020.127632
CHEMBL4752380 354304 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 3 1 3 1.4 O=C(CCN1CCCc2ccccc21)N1CCC(O)C1 10.1016/j.bmcl.2020.127632
176 823 54 None -1 31 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None -1 31 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None -1 31 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None -1 31 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None -1 31 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
1547484 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
2761 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 1937 56 None -9 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
46224516 40316 54 None -1 6 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (US National Institute of Mental Health's Psychoactive Drug Screen Program Selectivity Panel) EUB0001125a CHRM4Selectivity interaction (US National Institute of Mental Health's Psychoactive Drug Screen Program Selectivity Panel) EUB0001125a CHRM4
ChEMBL 509 10 1 7 5.8 COc1cc2c(NC3CCN(C(C)C)CC3)nc(C3CCCCC3)nc2cc1OCCCN1CCCC1 10.6019/CHEMBL5715260
CHEMBL1231795 40316 54 None -1 6 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (US National Institute of Mental Health's Psychoactive Drug Screen Program Selectivity Panel) EUB0001125a CHRM4Selectivity interaction (US National Institute of Mental Health's Psychoactive Drug Screen Program Selectivity Panel) EUB0001125a CHRM4
ChEMBL 509 10 1 7 5.8 COc1cc2c(NC3CCN(C(C)C)CC3)nc(C3CCCCC3)nc2cc1OCCCN1CCCC1 10.6019/CHEMBL5715260
44593616 384952 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 384952 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
145961152 317131 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
145962050 317131 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4129382 317131 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4130037 317131 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
164625211 371784 0 None -15 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028864 371784 0 None -15 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
137635734 312036 0 None -177 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 312036 0 None -177 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
24894109 372187 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL509202 372187 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
4715419 365919 30 None -12 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
CHEMBL505086 365919 30 None -12 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
71457691 174786 0 None -1 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205823 174786 0 None -1 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
10660 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None -1 13 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
122387446 275652 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
CHEMBL3770667 275652 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
122387446 275652 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
CHEMBL3770667 275652 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
162353374 353925 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4747590 353925 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
16086066 276560 0 None -134 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378872 276560 0 None -134 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
26987 1955 32 None -38 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
6063 1955 32 None -38 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
671 1955 32 None -38 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
CHEMBL1626 1955 32 None -38 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
DB00283 1955 32 None -38 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
3168 23567 68 None -89 19 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
966 23567 68 None -89 19 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 23567 68 None -89 19 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 23567 68 None -89 19 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
10418420 142518 0 None -40 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
CHEMBL194216 142518 0 None -40 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
46227487 38047 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198047 38047 0 None -1 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
24841480 367228 0 None -26 20 Human 7.3 pKi = 7.3 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 367228 0 None -26 20 Human 7.3 pKi = 7.3 Binding
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
178313861 466361 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 1235 28 5 15 8.7 O=C(CCOCCOCCNC(=O)c1ccc(-c2c3cc(F)c(=O)cc-3oc3cc(O)c(F)cc23)c(C(=O)O)c1)NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
CHEMBL6143437 466361 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 1235 28 5 15 8.7 O=C(CCOCCOCCNC(=O)c1ccc(-c2c3cc(F)c(=O)cc-3oc3cc(O)c(F)cc23)c(C(=O)O)c1)NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
44627854 404290 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571341 404290 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44437256 26665 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
CHEMBL1185707 26665 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
44627855 394458 0 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569212 394458 0 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
1395 99516 64 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
3652 99516 64 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
CHEMBL1535 99516 64 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
DB01611 99516 64 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
10066369 238928 0 None -22 6 Human 5.3 pKi = 5.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 238928 0 None -22 6 Human 5.3 pKi = 5.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44274432 161586 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21328 161586 0 None -3 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
161811679 405053 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5741939 405053 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153682079 405085 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.2 O=C(NCCC1CCN(Cc2ccccc2)CC1O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5742211 405085 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.2 O=C(NCCC1CCN(Cc2ccccc2)CC1O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370248 405099 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 482 6 1 6 3.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2csnn2)CC1 nan
CHEMBL5742363 405099 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 482 6 1 6 3.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2csnn2)CC1 nan
153682141 405105 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5742399 405105 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
161295032 405313 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 473 6 1 2 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL5744370 405313 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 473 6 1 2 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2cccc(C(F)(F)F)c2)CC1 nan
129105337 405370 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 547 9 1 6 4.9 COC(=O)C(c1ccccc1)N1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
CHEMBL5744923 405370 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 547 9 1 6 4.9 COC(=O)C(c1ccccc1)N1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
162370400 405435 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 7 1 5 4.1 C[C@@H]1CN(c2ccc(C#N)c(N(C)C)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5745572 405435 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 7 1 5 4.1 C[C@@H]1CN(c2ccc(C#N)c(N(C)C)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682063 405936 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 540 8 1 4 5.2 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2OC(F)F)CC1 nan
CHEMBL5750230 405936 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 540 8 1 4 5.2 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2OC(F)F)CC1 nan
162370249 405980 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 532 6 1 5 4.4 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc3c(c2)OCCO3)CC1 nan
CHEMBL5750653 405980 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 532 6 1 5 4.4 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc3c(c2)OCCO3)CC1 nan
162370252 406335 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(C#N)c2)CC1 nan
CHEMBL5754104 406335 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(C#N)c2)CC1 nan
129105254 406504 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 1 4 4.6 C[C@@H]1CN(c2ccc(C(F)(F)F)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5755923 406504 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 1 4 4.6 C[C@@H]1CN(c2ccc(C(F)(F)F)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682062 406588 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 3 4.8 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(F)c2)CC1 nan
CHEMBL5756869 406588 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 3 4.8 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(F)c2)CC1 nan
162370204 406830 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 6 1 3 4.3 C[C@@H]1CN(c2ccc(F)cc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5759553 406830 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 6 1 3 4.3 C[C@@H]1CN(c2ccc(F)cc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370312 406884 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 8 2 5 3.7 N#Cc1cc(N2CCC(C(=O)NCCC3(CO)CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5760109 406884 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 8 2 5 3.7 N#Cc1cc(N2CCC(C(=O)NCCC3(CO)CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
129105366 406888 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 433 8 1 4 5.0 O=C(NCCC1CCN(Cc2cccnc2F)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL5760150 406888 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 433 8 1 4 5.0 O=C(NCCC1CCN(Cc2cccnc2F)CC1)c1ccc(Oc2ccccc2)cc1 nan
153682081 407163 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 5.3 N#Cc1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)cc2)cc1 nan
CHEMBL5762836 407163 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 5.3 N#Cc1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)cc2)cc1 nan
153682108 407183 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.2 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1OC(F)(F)F nan
CHEMBL5763029 407183 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.2 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1OC(F)(F)F nan
153682107 407372 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2cc(C(F)(F)F)ccn2)CC1 nan
CHEMBL5764871 407372 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2cc(C(F)(F)F)ccn2)CC1 nan
161958285 407428 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 476 6 1 5 3.4 C[C@@H]1CN(c2nc(F)c(F)c(F)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5765470 407428 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 476 6 1 5 3.4 C[C@@H]1CN(c2nc(F)c(F)c(F)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105270 407461 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 3 4.8 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
CHEMBL5765734 407461 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 3 4.8 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
162370278 407589 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 6 2 6 4.1 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(O)cc2)CC1 nan
CHEMBL5766922 407589 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 6 2 6 4.1 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(O)cc2)CC1 nan
162370402 408344 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccc1C#N nan
CHEMBL5774449 408344 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccc1C#N nan
158665731 408421 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2ccc(C#N)nn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5775173 408421 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2ccc(C#N)nn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370377 408443 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 5 1 6 3.2 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(C2Cc3ccccc3C2)CC1 nan
CHEMBL5775425 408443 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 5 1 6 3.2 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(C2Cc3ccccc3C2)CC1 nan
162370212 408578 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 6 1 5 4.1 C[C@@H]1CN(c2ccc(C#N)s2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5776920 408578 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 6 1 5 4.1 C[C@@H]1CN(c2ccc(C#N)s2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105394 408933 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 484 8 1 7 4.1 COc1ncccc1-c1cc2ncc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(C)n2n1 nan
CHEMBL5780469 408933 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 484 8 1 7 4.1 COc1ncccc1-c1cc2ncc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(C)n2n1 nan
162370313 409027 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 8 1 5 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
CHEMBL5781591 409027 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 8 1 5 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
129105353 409125 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.6 C[C@@H]1CN(c2cc(F)c(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5782429 409125 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.6 C[C@@H]1CN(c2cc(F)c(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370355 409172 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 1 5 5.6 O=C(NC1CCN(c2ccc(OC(F)(F)F)cc2)CC1)OCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5782973 409172 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 1 5 5.6 O=C(NC1CCN(c2ccc(OC(F)(F)F)cc2)CC1)OCCC1CCN(Cc2ccccc2)CC1 nan
135374958 409215 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.9 O=C(NCCC1CCN(Cc2ccc(O)cc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5783485 409215 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.9 O=C(NCCC1CCN(Cc2ccc(O)cc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370228 409279 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 6 1 5 4.0 C[C@@H]1CN(c2ncc(C#N)cc2F)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5784173 409279 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 6 1 5 4.0 C[C@@H]1CN(c2ncc(C#N)cc2F)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370209 409486 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 6 1 7 2.7 C[C@@H]1CN(c2nc(C#N)cc(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5786419 409486 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 6 1 7 2.7 C[C@@H]1CN(c2nc(C#N)cc(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682077 409631 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2cccc(OC(F)(F)F)c2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5787738 409631 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2cccc(OC(F)(F)F)c2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
129105284 409701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 9 1 4 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)F)cc2)CC1 nan
CHEMBL5788458 409701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 9 1 4 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)F)cc2)CC1 nan
162370283 409825 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1cccc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)c1 nan
CHEMBL5789901 409825 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1cccc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)c1 nan
129105404 410065 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 444 9 2 4 5.0 O=C(NCCC1CCN(Cc2ccccc2O)CC1)c1ccc(OCc2ccccc2)cc1 nan
CHEMBL5792354 410065 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 444 9 2 4 5.0 O=C(NCCC1CCN(Cc2ccccc2O)CC1)c1ccc(OCc2ccccc2)cc1 nan
129105402 410149 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 7 1 6 4.6 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(C#N)c3)nn12 nan
CHEMBL5793098 410149 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 7 1 6 4.6 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(C#N)c3)nn12 nan
162370277 410286 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 547 7 1 6 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(N(C)C)cc2)CC1 nan
CHEMBL5794700 410286 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 547 7 1 6 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(N(C)C)cc2)CC1 nan
162370208 410377 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2cccc(F)c2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5795855 410377 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2cccc(F)c2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370297 410398 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 4 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2nc3ccccc3s2)CC1 nan
CHEMBL5796098 410398 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 4 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2nc3ccccc3s2)CC1 nan
162370189 410591 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 1 5 3.8 CO[C@H](CNC(=O)N1CCN(c2ccc(F)c(C#N)c2)C[C@H]1C)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5798238 410591 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 1 5 3.8 CO[C@H](CNC(=O)N1CCN(c2ccc(F)c(C#N)c2)C[C@H]1C)C1CCN(Cc2ccccc2)CC1 nan
162370301 410878 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 2 3 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL5801368 410878 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 2 3 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2cccc(C(F)(F)F)c2)CC1 nan
129105333 410959 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 6 1 3 5.2 CC(c1ccccc1)N1CCC(CCNC(=O)N2CCN(c3cc(F)c(F)c(F)c3)C[C@H]2C)CC1 nan
CHEMBL5802210 410959 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 6 1 3 5.2 CC(c1ccccc1)N1CCC(CCNC(=O)N2CCN(c3cc(F)c(F)c(F)c3)C[C@H]2C)CC1 nan
162370275 410971 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccc(F)c2)CC1 nan
CHEMBL5802375 410971 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccc(F)c2)CC1 nan
129105390 411023 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 5 5.0 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(F)c3F)nn12 nan
CHEMBL5803045 411023 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 5 5.0 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(F)c3F)nn12 nan
129105330 411106 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 6 1 4 4.8 C[C@@H]1CN(c2cnc3ccccc3c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5803998 411106 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 6 1 4 4.8 C[C@@H]1CN(c2cnc3ccccc3c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370334 411699 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5810777 411699 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370206 411701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2ccc(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5810781 411701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2ccc(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682075 411735 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 1 2 6.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(Cl)cc2)cc1F nan
CHEMBL5811121 411735 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 1 2 6.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(Cl)cc2)cc1F nan
153682109 411755 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 530 8 2 6 4.2 N#Cc1cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1OC(F)(F)F nan
CHEMBL5811329 411755 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 530 8 2 6 4.2 N#Cc1cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1OC(F)(F)F nan
129105208 411824 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 523 7 1 4 5.3 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL5812099 411824 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 523 7 1 4 5.3 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(C(F)(F)F)cc2Cl)C1 nan
129105386 412055 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 8 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
CHEMBL5814698 412055 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 8 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
162370244 412358 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 6 2 6 2.8 Nc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ncc1Cl nan
CHEMBL5817727 412358 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 6 2 6 2.8 Nc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ncc1Cl nan
162370298 412531 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 509 6 1 4 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1 nan
CHEMBL5819828 412531 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 509 6 1 4 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1 nan
129105179 412708 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.6 O=C(NCCC1(CO)CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5821885 412708 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.6 O=C(NCCC1(CO)CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370202 412784 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 1 6 3.1 COc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ncc1F nan
CHEMBL5822758 412784 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 1 6 3.1 COc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ncc1F nan
153682113 413363 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 530 8 2 6 4.2 N#Cc1cc(OC(F)(F)F)cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5828979 413363 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 530 8 2 6 4.2 N#Cc1cc(OC(F)(F)F)cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
153683042 413541 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 7 2.9 C[C@@H]1CN(c2ncc(C#N)c(N(C)C)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5830929 413541 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 7 2.9 C[C@@H]1CN(c2ncc(C#N)c(N(C)C)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370368 413896 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 7 1 5 5.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccc3C(F)(F)F)nn12 nan
CHEMBL5834508 413896 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 7 1 5 5.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccc3C(F)(F)F)nn12 nan
153682064 414030 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 7 2 4 3.7 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C(N)=O)cc2)CC1 nan
CHEMBL5836155 414030 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 7 2 4 3.7 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C(N)=O)cc2)CC1 nan
153682082 423788 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2cccc(OC(F)(F)F)c2)CC1)[C@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5901488 423788 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2cccc(OC(F)(F)F)c2)CC1)[C@H]1CCN(Cc2ccccc2)C1 nan
160487528 424267 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 3 6.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2csc3ccccc23)CC1 nan
CHEMBL5840878 424267 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 3 6.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2csc3ccccc23)CC1 nan
153683044 424346 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 9 2 5 3.9 O=C(NCCN[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1 nan
CHEMBL5841665 424346 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 9 2 5 3.9 O=C(NCCN[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1 nan
158593517 424370 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 2 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccc(Cl)cc2)CC1 nan
CHEMBL5841868 424370 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 2 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccc(Cl)cc2)CC1 nan
153682111 424481 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 2 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL5843256 424481 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 2 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cc(F)c(F)c(F)c2)CC1 nan
162370280 424851 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 518 7 1 5 4.4 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(CCc2ccccc2)CC1 nan
CHEMBL5847610 424851 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 518 7 1 5 4.4 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(CCc2ccccc2)CC1 nan
129105443 425054 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 1 4 4.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
CHEMBL5849805 425054 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 1 4 4.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
129105326 425520 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2nccc(C(F)(F)F)n2)CC1 nan
CHEMBL5854770 425520 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2nccc(C(F)(F)F)n2)CC1 nan
129105188 426023 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 549 5 0 5 4.8 O=C(C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1)N1CCN(C2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5859977 426023 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 549 5 0 5 4.8 O=C(C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1)N1CCN(C2CCN(Cc3ccccc3)CC2)CC1 nan
162370210 426196 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1cc(C#N)cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)c1 nan
CHEMBL5862001 426196 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1cc(C#N)cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)c1 nan
153682142 426224 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1F nan
CHEMBL5862256 426224 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1F nan
162370300 426259 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 N#Cc1cc(F)cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5862548 426259 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 N#Cc1cc(F)cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370284 426469 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 501 6 1 7 4.0 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc3occc3c2)CC1 nan
CHEMBL5865059 426469 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 501 6 1 7 4.0 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc3occc3c2)CC1 nan
162370214 426662 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5867140 426662 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370362 427022 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 7 1 5 5.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C(F)(F)F)cc3)nn12 nan
CHEMBL5871231 427022 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 7 1 5 5.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C(F)(F)F)cc3)nn12 nan
158500097 427201 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 479 6 2 5 3.2 C[C@@H]1CN(c2cc(F)cc(C#N)c2)CCN1C(=O)NC[C@H](O)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5873109 427201 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 479 6 2 5 3.2 C[C@@H]1CN(c2cc(F)cc(C#N)c2)CCN1C(=O)NC[C@H](O)C1CCN(Cc2ccccc2)CC1 nan
162370385 427286 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 6 1 6 2.4 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC23C4C5C6C4C2C6C53)CC1 nan
CHEMBL5874106 427286 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 6 1 6 2.4 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC23C4C5C6C4C2C6C53)CC1 nan
162370414 427410 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 9 2 6 3.7 Cc1cc(C(=O)NCC(C)C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5875471 427410 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 9 2 6 3.7 Cc1cc(C(=O)NCC(C)C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
159606134 427469 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)cc2F)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5876302 427469 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)cc2F)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682087 427518 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.3 O=C(NCCC1(O)CCN(Cc2ccccc2)CC1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5876920 427518 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.3 O=C(NCCC1(O)CCN(Cc2ccccc2)CC1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
153682103 427604 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)cn2)CC1 nan
CHEMBL5877979 427604 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)cn2)CC1 nan
162370263 427609 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 6 1 5 4.2 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
CHEMBL5878049 427609 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 6 1 5 4.2 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
162370279 427845 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(F)cc2)CC1 nan
CHEMBL5880695 427845 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(F)cc2)CC1 nan
162370291 427890 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 2 5 3.6 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)NCCC1(CO)CCN(Cc2ccccc2)CC1 nan
CHEMBL5881237 427890 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 2 5 3.6 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)NCCC1(CO)CCN(Cc2ccccc2)CC1 nan
129105305 428022 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1ccccc1-c1cc2ncc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(C)n2n1 nan
CHEMBL5882823 428022 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1ccccc1-c1cc2ncc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(C)n2n1 nan
153682065 428234 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(F)c2F)CC1 nan
CHEMBL5885223 428234 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(F)c2F)CC1 nan
162370186 428357 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 2 5 3.9 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)NC[C@@H](CC(=O)O)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5886734 428357 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 2 5 3.9 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)NC[C@@H](CC(=O)O)C1CCN(Cc2ccccc2)CC1 nan
162370352 428751 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 0 5 5.1 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5891145 428751 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 0 5 5.1 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
162370314 428925 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 7 0 5 5.0 CN(C1CCN(C(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5892721 428925 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 7 0 5 5.0 CN(C1CCN(C(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
162370311 428980 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 7 0 5 5.0 CN(C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)C1CCN(C2CCN(Cc3ccccc3)CC2)C1 nan
CHEMBL5893220 428980 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 7 0 5 5.0 CN(C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)C1CCN(C2CCN(Cc3ccccc3)CC2)C1 nan
162370257 429077 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2cccnc2)CC1 nan
CHEMBL5894194 429077 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2cccnc2)CC1 nan
160791390 429195 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 9 2 6 3.4 CC(C)CNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
CHEMBL5895354 429195 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 9 2 6 3.4 CC(C)CNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
162370292 429504 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 516 6 1 6 3.5 C[C@@H]1CN(c2ccc(OC(F)(F)F)c(C#N)c2)CCN1C(=O)NCCN1CCN(c2ccccc2)CC1 nan
CHEMBL5898368 429504 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 516 6 1 6 3.5 C[C@@H]1CN(c2ccc(OC(F)(F)F)c(C#N)c2)CCN1C(=O)NCCN1CCN(c2ccccc2)CC1 nan
129105348 429569 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 6 1 3 4.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL5898978 429569 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 6 1 3 4.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cc(F)c(F)c(F)c2)CC1 nan
162370288 429613 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1ccc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)cc1 nan
CHEMBL5899419 429613 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1ccc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)cc1 nan
159088337 429686 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 655 7 1 5 5.6 C[C@@H]1CN(c2ccc(OC(F)(F)F)c(C#N)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(I)cc2)CC1 nan
CHEMBL5900105 429686 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 655 7 1 5 5.6 C[C@@H]1CN(c2ccc(OC(F)(F)F)c(C#N)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(I)cc2)CC1 nan
162370213 429701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2cc(F)ccc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5900260 429701 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 6 1 3 4.5 C[C@@H]1CN(c2cc(F)ccc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129124749 429707 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.3 C[C@@H]1CN(c2ncc(C(=O)NC3CC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5900308 429707 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.3 C[C@@H]1CN(c2ncc(C(=O)NC3CC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105484 429813 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 9 1 3 5.4 O=C(NCCC1CCN(Cc2ccc(F)cc2)CC1)c1ccc(OCc2ccccc2)cc1 nan
CHEMBL5901417 429813 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 9 1 3 5.4 O=C(NCCC1CCN(Cc2ccc(F)cc2)CC1)c1ccc(OCc2ccccc2)cc1 nan
162370407 429966 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2cnc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5903136 429966 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2cnc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370203 429969 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cc1C#N nan
CHEMBL5903161 429969 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 5 4.1 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cc1C#N nan
129105336 430305 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 485 7 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2cccc3c2OC(F)(F)O3)CC1 nan
CHEMBL5906173 430305 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 485 7 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2cccc3c2OC(F)(F)O3)CC1 nan
153682080 430752 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
CHEMBL5910584 430752 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
162370391 430771 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 1 4 4.3 C[C@@H]1CN(c2ccc(Cl)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5910842 430771 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 1 4 4.3 C[C@@H]1CN(c2ccc(Cl)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105295 431015 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 8 1 4 4.5 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1F nan
CHEMBL5913329 431015 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 8 1 4 4.5 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1F nan
129105432 431501 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2F)CC1 nan
CHEMBL5918352 431501 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2F)CC1 nan
162370231 431800 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 8 2 7 3.8 C[C@@H]1CN(c2ncc(C#N)c(NCC(F)(F)F)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5921388 431800 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 544 8 2 7 3.8 C[C@@H]1CN(c2ncc(C#N)c(NCC(F)(F)F)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
159738505 432059 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(Cl)c2)CC1 nan
CHEMBL5924079 432059 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(Cl)c2)CC1 nan
162370215 432409 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 6 1 4 3.9 C[C@@H]1CN(c2ncc(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5927366 432409 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 6 1 4 3.9 C[C@@H]1CN(c2ncc(F)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
157933450 432427 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 6 1 4 4.2 C[C@@H]1CN(c2ccc(C#N)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5927612 432427 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 6 1 4 4.2 C[C@@H]1CN(c2ccc(C#N)cc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
161408977 432872 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5931951 432872 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
162370299 432911 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL5932297 432911 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
129105357 433043 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 8 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)nc2)CC1 nan
CHEMBL5933785 433043 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 8 1 5 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)nc2)CC1 nan
162370207 433119 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccc(F)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5934608 433119 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccc(F)nc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105415 433312 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 7 2 4 4.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1(CO)CCN(Cc2ccccc2)CC1 nan
CHEMBL5936650 433312 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 7 2 4 4.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1(CO)CCN(Cc2ccccc2)CC1 nan
162002529 442626 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.6 C[C@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5967614 442626 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 3 4.6 C[C@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105261 442964 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 6 1 5 4.4 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6007090 442964 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 6 1 5 4.4 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370307 443234 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 8 1 4 5.2 COC(=O)c1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)cc2)cc1 nan
CHEMBL5938223 443234 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 456 8 1 4 5.2 COC(=O)c1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)cc2)cc1 nan
162370276 443324 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
CHEMBL5939043 443324 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 6 1 5 4.5 C[C@@H]1CN(c2cnc(C(F)(F)F)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2F)CC1 nan
153682086 443329 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.4 N#Cc1cc(N2CCC(C(=O)NCCC3(O)CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5939146 443329 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.4 N#Cc1cc(N2CCC(C(=O)NCCC3(O)CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
135375122 443391 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 7 1 6 3.2 C[C@H]1CN(c2ncc(C#N)cn2)CCC1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5939776 443391 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 7 1 6 3.2 C[C@H]1CN(c2ncc(C#N)cn2)CCC1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105422 443486 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 7 1 4 4.4 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(Br)cn2)C1 nan
CHEMBL5940751 443486 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 7 1 4 4.4 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(Br)cn2)C1 nan
158922000 443855 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 8 2 7 4.2 C[C@@H]1CN(c2ncc(C#N)c(NCC(F)(F)F)n2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5944519 443855 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 8 2 7 4.2 C[C@@H]1CN(c2ncc(C#N)c(NCC(F)(F)F)n2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158607213 443896 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 5 3.0 C[C@@H]1CN(c2cncnc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5944904 443896 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 5 3.0 C[C@@H]1CN(c2cncnc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153683047 444221 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5948273 444221 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
162370200 444254 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 445 6 1 4 4.1 C[C@@H]1CN(c2ccc(C#N)cc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5948596 444254 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 445 6 1 4 4.1 C[C@@H]1CN(c2ccc(C#N)cc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682110 444307 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.0 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5949062 444307 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.0 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153682076 444404 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.3 N#Cc1cc(N2CCC(C(=O)NC[C@H](O)C3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5950026 444404 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.3 N#Cc1cc(N2CCC(C(=O)NC[C@H](O)C3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
162370296 444738 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.7 N#Cc1cc(C(F)(F)F)ccc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5953844 444738 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.7 N#Cc1cc(C(F)(F)F)ccc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
153682114 444834 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 8 1 5 4.5 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2cc(C(F)(F)F)ccn2)CC1 nan
CHEMBL5954761 444834 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 8 1 5 4.5 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2cc(C(F)(F)F)ccn2)CC1 nan
129105341 445376 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccnc(F)c3)nn12 nan
CHEMBL5960658 445376 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccnc(F)c3)nn12 nan
162370251 445404 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 495 6 1 5 4.4 Cc1nc(CN2CCC(CCNC(=O)N3CCN(c4cc(F)c(F)c(F)c4)C[C@H]3C)CC2)cs1 nan
CHEMBL5960917 445404 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 495 6 1 5 4.4 Cc1nc(CN2CCC(CCNC(=O)N3CCN(c4cc(F)c(F)c(F)c4)C[C@H]3C)CC2)cs1 nan
129105187 445667 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.6 O=C(NCCC1(CO)CCN(Cc2ccccc2)CC1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5963763 445667 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.6 O=C(NCCC1(CO)CCN(Cc2ccccc2)CC1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
159877436 446061 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 7 1 7 3.3 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(N(C)C)cc2)CC1 nan
CHEMBL5967925 446061 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 7 1 7 3.3 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(N(C)C)cc2)CC1 nan
162370358 446115 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 7 1 5 5.4 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(Cl)cc3)nn12 nan
CHEMBL5968586 446115 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 7 1 5 5.4 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(Cl)cc3)nn12 nan
153682121 446518 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(F)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5972801 446518 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(F)CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153682084 446874 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 2 5.8 Cc1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(F)c2)cc1 nan
CHEMBL5977253 446874 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 2 5.8 Cc1ccc(-c2ccc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c(F)c2)cc1 nan
162370401 446878 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2cnc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5977274 446878 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2cnc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682106 447347 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.2 COc1cc(OC(F)(F)F)cc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5982319 447347 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.2 COc1cc(OC(F)(F)F)cc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
157055452 447429 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(Cl)cc2)CC1 nan
CHEMBL5983167 447429 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(Cl)cc2)CC1 nan
162370394 447835 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccn1 nan
CHEMBL5987643 447835 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccn1 nan
162370309 447857 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)[C@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5987876 447857 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)[C@H]1CCN(Cc2ccccc2)C1 nan
129105424 447962 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 497 9 1 4 5.2 CN(CCNC(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5988959 447962 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 497 9 1 4 5.2 CN(CCNC(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@@H]1CCN(Cc2ccccc2)C1 nan
162370396 448232 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccnc(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5991725 448232 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2ccnc(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370308 448235 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 466 7 1 2 6.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 nan
CHEMBL5991741 448235 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 466 7 1 2 6.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 nan
129105375 448536 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 7 1 7 4.5 Cc1c(C(=O)NCCC2CCN(Cc3cccc4c3OCCO4)CC2)cnc2cc(-c3ccccc3)nn12 nan
CHEMBL5994727 448536 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 7 1 7 4.5 Cc1c(C(=O)NCCC2CCN(Cc3cccc4c3OCCO4)CC2)cnc2cc(-c3ccccc3)nn12 nan
160919441 449408 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 454 6 1 5 3.5 C[C@@H]1CN(c2ncc(F)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6004279 449408 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 454 6 1 5 3.5 C[C@@H]1CN(c2ncc(F)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370205 449470 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 3.5 C[C@@H]1CN(c2ccc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6004949 449470 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 3.5 C[C@@H]1CN(c2ccc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370201 449830 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 477 7 1 7 2.9 COc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ncc1C#N nan
CHEMBL6008489 449830 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 477 7 1 7 2.9 COc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ncc1C#N nan
162370223 450093 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 468 7 1 4 4.4 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cc1F nan
CHEMBL6011585 450093 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 468 7 1 4 4.4 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cc1F nan
162370290 450095 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1ccccc1CN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
CHEMBL6011627 450095 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1ccccc1CN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
162370337 450267 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 486 9 1 5 5.1 O=C(NCCC1CCN(Cc2cccc3c2OCCO3)CC1)c1ccc(OCc2ccccc2)cc1 nan
CHEMBL6013413 450267 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 486 9 1 5 5.1 O=C(NCCC1CCN(Cc2cccc3c2OCCO3)CC1)c1ccc(OCc2ccccc2)cc1 nan
129105302 450602 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6016845 450602 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105395 450990 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 480 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(CC2CCCCC2)CC1 nan
CHEMBL6020963 450990 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 480 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(CC2CCCCC2)CC1 nan
129105257 451130 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 496 7 1 6 4.7 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C#N)c(F)c3)nn12 nan
CHEMBL6022488 451130 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 496 7 1 6 4.7 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C#N)c(F)c3)nn12 nan
162370211 451432 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 5 3.1 C[C@@H]1CN(c2ncc(F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6025660 451432 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 6 1 5 3.1 C[C@@H]1CN(c2ncc(F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105344 451624 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 556 11 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2n(CCC)c1=O nan
CHEMBL6027803 451624 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 556 11 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2n(CCC)c1=O nan
135374959 451725 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 0 5 5.1 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL6028753 451725 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 0 5 5.1 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370367 451838 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 7 1 5 4.9 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(F)c3)nn12 nan
CHEMBL6030219 451838 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 471 7 1 5 4.9 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccc(F)c3)nn12 nan
162370191 452003 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2nccc(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6031843 452003 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 6 1 6 2.9 C[C@@H]1CN(c2nccc(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370266 452013 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 515 6 1 6 3.9 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
CHEMBL6031950 452013 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 515 6 1 6 3.9 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
153682078 461468 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL6064496 461468 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 9 1 5 4.1 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)[C@@H]1CCN(Cc2ccccc2)C1 nan
129105298 461907 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 5 5.0 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cc(F)ccc3F)nn12 nan
CHEMBL6034348 461907 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 5 5.0 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cc(F)ccc3F)nn12 nan
129105314 461924 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 523 8 2 5 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1 nan
CHEMBL6034504 461924 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 523 8 2 5 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1 nan
129124839 462212 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 467 6 1 6 3.6 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCCC2)CC1 nan
CHEMBL6037384 462212 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 467 6 1 6 3.6 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCCC2)CC1 nan
162370250 462293 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 2 5 4.1 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccc5[nH]ccc5c4)CC3)CC2)nc1 nan
CHEMBL6038384 462293 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 2 5 4.1 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccc5[nH]ccc5c4)CC3)CC2)nc1 nan
153682085 462410 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 416 7 1 2 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(F)cc2)cc1 nan
CHEMBL6039546 462410 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 416 7 1 2 5.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(F)cc2)cc1 nan
129105320 462846 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 7 1 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6043997 462846 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 487 7 1 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370222 463295 0 None 10 4 Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1nc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)ncc1C#N nan
CHEMBL6048174 463295 0 None 10 4 Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 7 1 7 3.3 COc1nc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)ncc1C#N nan
160106121 463483 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 0 4 4.7 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL6050233 463483 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 0 4 4.7 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cc(F)c(F)c(F)c2)CC1 nan
162370281 463485 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 2 7 3.3 Cc1cc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)ccc1O nan
CHEMBL6050271 463485 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 2 7 3.3 Cc1cc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4ncc(C#N)cn4)C[C@@H]3C)CC2)ccc1O nan
129105483 463769 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(F)cc2)CC1 nan
CHEMBL6052979 463769 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(F)cc2)CC1 nan
129105293 464154 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 420 6 1 3 4.2 C[C@@H]1CN(c2ccccc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6057012 464154 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 420 6 1 3 4.2 C[C@@H]1CN(c2ccccc2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370403 464190 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 1 4 4.6 C[C@@H]1CN(c2ccnc(C(F)(F)F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6057373 464190 0 None None None Human 7.3 pKi = 7.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 6 1 4 4.6 C[C@@H]1CN(c2ccnc(C(F)(F)F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682136 404822 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1 nan
153682137 404822 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1 nan
CHEMBL5739601 404822 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1 nan
CHEMBL5746574 404822 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1 nan
129105204 404997 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 2 3 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2ccc(Cl)cc2)CC1 nan
CHEMBL5741287 404997 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 2 3 4.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2ccc(Cl)cc2)CC1 nan
153683046 405043 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 2 3 5.7 Cc1[nH]c(-c2ccc(Cl)cc2Cl)nc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5741850 405043 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 470 7 2 3 5.7 Cc1[nH]c(-c2ccc(Cl)cc2Cl)nc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
157188498 405112 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 6 1 4 3.9 Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cn1 nan
CHEMBL5742452 405112 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 6 1 4 3.9 Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)cn1 nan
162020813 405470 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 9 2 6 3.9 CCC(C)NC(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
CHEMBL5745911 405470 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 9 2 6 3.9 CCC(C)NC(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
129105176 405506 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccc(F)cc2)CC1 nan
CHEMBL5746211 405506 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccc(F)cc2)CC1 nan
162370258 405680 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
CHEMBL5747978 405680 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
129105250 405686 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 7 2 3 4.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2ccc(F)cc2)CC1 nan
CHEMBL5748055 405686 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 7 2 3 4.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2ccc(F)cc2)CC1 nan
157411756 405768 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 6 3.1 CCN(C)C(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
CHEMBL5748757 405768 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 6 3.1 CCN(C)C(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
162370282 406014 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 6 1 8 2.0 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ncccn2)CC1 nan
CHEMBL5750969 406014 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 6 1 8 2.0 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ncccn2)CC1 nan
153682116 406380 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1 nan
153682119 406380 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL5754463 406380 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL6030630 406380 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCCC1CCN(Cc2ccccc2)CC1)[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1 nan
162370321 406415 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCC[C@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5754815 406415 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCC[C@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
159649060 406635 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 1 6 3.4 CCN(C)C(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5757388 406635 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 1 6 3.4 CCN(C)C(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
160664823 407144 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 6 0 5 4.3 N#Cc1cc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5762631 407144 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 6 0 5 4.3 N#Cc1cc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
159532422 407357 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 5 3.0 C[C@@H]1CN(c2ncccn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5764727 407357 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 5 3.0 C[C@@H]1CN(c2ncccn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370354 407410 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 7 1 4 4.8 O=C(NC1CCN(c2ccc(F)cc2)CC1)OCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5765339 407410 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 7 1 4 4.8 O=C(NC1CCN(c2ccc(F)cc2)CC1)OCCC1CCN(Cc2ccccc2)CC1 nan
160455882 407586 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 6 2 6 2.3 Nc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ncc1F nan
CHEMBL5766917 407586 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 6 2 6 2.3 Nc1nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ncc1F nan
159384857 407961 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 405 7 1 3 4.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2)CC1 nan
CHEMBL5770442 407961 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 405 7 1 3 4.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2)CC1 nan
162370269 407962 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 486 6 1 7 3.1 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
CHEMBL5770448 407962 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 486 6 1 7 3.1 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
129105449 408600 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 6 2 4 3.4 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN1CCC(O)(Cc2ccccc2)CC1 nan
CHEMBL5777149 408600 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 6 2 4 3.4 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN1CCC(O)(Cc2ccccc2)CC1 nan
153682135 408651 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1cc(F)ccc1N1CCC(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5777628 408651 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1cc(F)ccc1N1CCC(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
158003662 408693 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 428 7 1 6 3.5 Cc1nc(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cn1-c1ccc(C#N)cn1 nan
CHEMBL5778021 408693 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 428 7 1 6 3.5 Cc1nc(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cn1-c1ccc(C#N)cn1 nan
162370340 409458 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.8 O=C(NCCC1CCN(C(CO)c2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5786055 409458 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 5 4.8 O=C(NCCC1CCN(C(CO)c2ccccc2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162146805 409719 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 7 1 6 3.1 CC(C)CCN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
CHEMBL5788622 409719 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 7 1 6 3.1 CC(C)CCN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
162370413 409952 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 8 2 6 3.1 C[C@@H]1CN(c2ncc(C(=O)NCCF)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
CHEMBL5791189 409952 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 8 2 6 3.1 C[C@@H]1CN(c2ncc(C(=O)NCCF)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
153682072 409954 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1ccc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
CHEMBL5791200 409954 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1ccc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
162370371 409996 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 2 6 4.4 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3O)CC2)cnc2cc(-c3ccccc3)nn12 nan
CHEMBL5791720 409996 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 2 6 4.4 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3O)CC2)cnc2cc(-c3ccccc3)nn12 nan
157200193 410182 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 432 6 0 5 4.1 N#Cc1cccc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5793496 410182 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 432 6 0 5 4.1 N#Cc1cccc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370304 410416 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 4.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(n2nnc3ccccc32)CC1 nan
CHEMBL5796318 410416 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 4.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(n2nnc3ccccc32)CC1 nan
162370259 410459 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 515 6 1 6 3.9 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2C#N)CC1 nan
CHEMBL5796738 410459 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 515 6 1 6 3.9 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2C#N)CC1 nan
162370256 410499 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccncc2)CC1 nan
CHEMBL5797184 410499 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 491 6 1 6 3.4 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2ccncc2)CC1 nan
129105427 410500 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 7 0 5 6.2 O=C(c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5797187 410500 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 7 0 5 6.2 O=C(c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
161089968 410638 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 8 1 6 3.9 CC(C)N(C)C(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
CHEMBL5798652 410638 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 535 8 1 6 3.9 CC(C)N(C)C(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
157534224 410761 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 420 7 1 4 4.0 Cc1ccnc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5800093 410761 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 420 7 1 4 4.0 Cc1ccnc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370378 410826 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCC2)CC1 nan
CHEMBL5800761 410826 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCC2)CC1 nan
162370293 410835 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 C[C@@H]1CN(c2cc(F)cc(C#N)c2)CCN1C(=O)NCC[C@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL5800868 410835 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 C[C@@H]1CN(c2cc(F)cc(C#N)c2)CCN1C(=O)NCC[C@H]1CCN(Cc2ccccc2)C1 nan
153682131 411167 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 5 3.7 CS(=O)(=O)c1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5804651 411167 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 5 3.7 CS(=O)(=O)c1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370234 411248 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 514 7 1 7 3.4 COC(=O)c1cc(Cl)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5805481 411248 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 514 7 1 7 3.4 COC(=O)c1cc(Cl)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
162370324 411581 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 548 8 0 4 6.3 O=C(C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1)N(CCC1CCN(Cc2ccccc2)CC1)C1CC1 nan
CHEMBL5809342 411581 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 548 8 0 4 6.3 O=C(C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1)N(CCC1CCN(Cc2ccccc2)CC1)C1CC1 nan
162370333 411628 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.2 O=C(CC1CCN(Cc2ccccc2)CC1)NCC1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5809979 411628 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.2 O=C(CC1CCN(Cc2ccccc2)CC1)NCC1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
162370336 411798 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 8 1 6 5.0 Cc1nc(CN2CCC(CCNC(=O)C3CCN(c4ccc(OC(F)(F)F)cc4)CC3)CC2)cs1 nan
CHEMBL5811741 411798 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 8 1 6 5.0 Cc1nc(CN2CCC(CCNC(=O)C3CCN(c4ccc(OC(F)(F)F)cc4)CC3)CC2)cs1 nan
162370287 411940 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 480 6 1 7 2.8 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccnc2F)CC1 nan
CHEMBL5813514 411940 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 480 6 1 7 2.8 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccnc2F)CC1 nan
162370351 412024 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 531 8 1 5 5.2 O=C(NCCC1CCN(Cc2cccc3c2OCC3)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5814346 412024 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 531 8 1 5 5.2 O=C(NCCC1CCN(Cc2cccc3c2OCC3)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370339 412130 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 497 8 1 7 4.1 O=C(NCCC1CCN(Cc2csnn2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5815535 412130 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 497 8 1 7 4.1 O=C(NCCC1CCN(Cc2csnn2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153682133 412245 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1ccccc1N1CCC(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5816473 412245 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 7 1 4 4.2 N#Cc1ccccc1N1CCC(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
161052566 412301 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1cccc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5817086 412301 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1cccc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370286 412385 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccncc2)CC1 nan
CHEMBL5818040 412385 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccncc2)CC1 nan
153682140 412502 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.0 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccccc2OC(F)(F)F)CC1 nan
CHEMBL5819492 412502 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 1 5 5.0 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccccc2OC(F)(F)F)CC1 nan
162370347 413316 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 8 2 5 4.6 O=C(NCC(O)C1CCN(CC2CCCCC2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5828597 413316 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 511 8 2 5 4.6 O=C(NCC(O)C1CCN(CC2CCCCC2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370342 413391 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 7 3.4 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4cccc5c4OCCO5)CC3)CC2)nc1 nan
CHEMBL5829278 413391 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 1 7 3.4 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4cccc5c4OCCO5)CC3)CC2)nc1 nan
129105487 413660 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2OC(F)(F)F)CC1 nan
CHEMBL5832134 413660 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.2 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2OC(F)(F)F)CC1 nan
162370318 413944 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 518 8 0 3 5.7 CN(CCC1CC[N+](C)(Cc2ccccc2)CC1)C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5835032 413944 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 518 8 0 3 5.7 CN(CCC1CC[N+](C)(Cc2ccccc2)CC1)C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
129105434 414023 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 3.5 C[C@@H]1CN(c2cncc(C#N)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5836106 414023 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 6 1 5 3.5 C[C@@H]1CN(c2cncc(C#N)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370344 414025 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 8 1 5 5.3 O=C(NCCC1CCN(Cc2cccc3c2OCCO3)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL5836123 414025 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 8 1 5 5.3 O=C(NCCC1CCN(Cc2cccc3c2OCCO3)CC1)c1ccc(Oc2ccccc2)cc1 nan
162370295 414054 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 465 6 1 4 4.3 N#Cc1cc(Cl)ccc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5836322 414054 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 465 6 1 4 4.3 N#Cc1cc(Cl)ccc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
129105414 414167 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 405 6 1 2 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2)CC1 nan
CHEMBL5837298 414167 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 405 6 1 2 4.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2)CC1 nan
153682091 423825 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCC[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5907878 423825 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 8 1 4 4.8 O=C(NCC[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370315 424123 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 0 4 5.6 CN(CCC1CCN(c2ccccc2)CC1)C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5839458 424123 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 7 0 4 5.6 CN(CCC1CCN(c2ccccc2)CC1)C(=O)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153682073 424255 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 2 4 4.0 COc1ccccc1C1(O)CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5840760 424255 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 2 4 4.0 COc1ccccc1C1(O)CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
162370194 424532 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 459 6 1 4 4.4 Cc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccc1C#N nan
CHEMBL5843826 424532 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 459 6 1 4 4.4 Cc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)ccc1C#N nan
129105248 424597 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 4 0 4 5.9 CN(C(=O)c1ccc(Cl)c(-c2nc3ccccc3cc2C#N)c1)[C@@H]1CCN(C2CCCCC2)C1 nan
CHEMBL5844616 424597 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 4 0 4 5.9 CN(C(=O)c1ccc(Cl)c(-c2nc3ccccc3cc2C#N)c1)[C@@H]1CCN(C2CCCCC2)C1 nan
129105479 424852 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 498 8 1 7 4.4 COc1cc(C)c(-c2cc3ncc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)c(C)n3n2)cn1 nan
CHEMBL5847612 424852 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 498 8 1 7 4.4 COc1cc(C)c(-c2cc3ncc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)c(C)n3n2)cn1 nan
162370193 424869 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 452 7 1 6 3.0 COc1ccnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5847800 424869 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 452 7 1 6 3.0 COc1ccnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
157467685 424928 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 8 1 5 4.2 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1C#N nan
CHEMBL5848437 424928 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 8 1 5 4.2 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1C#N nan
153682128 425115 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5850534 425115 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 8 2 5 4.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
162370238 425137 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 7 2 7 1.8 N#Cc1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](CO)C2)nc1 nan
CHEMBL5850757 425137 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 7 2 7 1.8 N#Cc1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](CO)C2)nc1 nan
153682125 425625 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2F)CC1 nan
CHEMBL5855984 425625 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 7 1 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccccc2F)CC1 nan
162370219 425666 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 1 4 4.2 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2C)cc1 nan
CHEMBL5856482 425666 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 1 4 4.2 COc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2C)cc1 nan
129105286 425767 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 7 1 5 4.4 CC(C)c1noc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)n1 nan
CHEMBL5857476 425767 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 7 1 5 4.4 CC(C)c1noc(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)n1 nan
153682099 425776 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(F)CCN(c2ccccc2OC(F)(F)F)CC1 nan
CHEMBL5857560 425776 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 1 4 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(F)CCN(c2ccccc2OC(F)(F)F)CC1 nan
153682083 425823 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 485 7 1 5 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(Br)cn2)CC1 nan
CHEMBL5857996 425823 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 485 7 1 5 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(Br)cn2)CC1 nan
129105210 425882 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 408 6 1 5 2.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncccn2)CC1 nan
CHEMBL5858629 425882 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 408 6 1 5 2.6 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncccn2)CC1 nan
162370326 425944 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 8 1 5 5.6 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
CHEMBL5859213 425944 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 8 1 5 5.6 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
162370254 425952 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 528 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(F)c(F)c2F)CC1 nan
CHEMBL5859250 425952 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 528 6 1 3 5.0 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(F)c(F)c2F)CC1 nan
157461412 425973 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 479 7 2 6 2.4 CNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
CHEMBL5859475 425973 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 479 7 2 6 2.4 CNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
153682132 425986 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1ccnc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5859640 425986 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1ccnc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
153682138 426083 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 7 1 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(F)cn2)CC1 nan
CHEMBL5860634 426083 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 7 1 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(F)cn2)CC1 nan
162370373 426574 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3ccccn3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
CHEMBL5866305 426574 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3ccccn3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
162370338 426638 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 437 7 1 5 4.0 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(CC4CCCCC4)CC3)CC2)nc1 nan
CHEMBL5866943 426638 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 437 7 1 5 4.0 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(CC4CCCCC4)CC3)CC2)nc1 nan
153682126 426735 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 8 1 4 4.3 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
CHEMBL5867887 426735 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 8 1 4 4.3 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
158327284 426838 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 2 6 3.1 CCNC(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5868964 426838 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 2 6 3.1 CCNC(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
162370289 427137 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 516 6 1 9 2.5 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc3c(c2)nnn3C)CC1 nan
CHEMBL5872598 427137 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 516 6 1 9 2.5 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc3c(c2)nnn3C)CC1 nan
129105292 427244 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 6 1 4 3.7 N#Cc1cccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5873475 427244 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 6 1 4 3.7 N#Cc1cccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
153682090 427316 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 494 6 1 4 5.0 O=C(NCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1 nan
CHEMBL5874428 427316 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 494 6 1 4 5.0 O=C(NCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ncc(C(F)(F)F)cc2Cl)CC1 nan
129105184 427472 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 467 7 1 3 6.0 Cc1cc(Cl)c(-c2cc(C(=O)NCC[C@@H]3CCN(Cc4ccccc4)C3)ccc2Cl)cn1 nan
CHEMBL5876319 427472 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 467 7 1 3 6.0 Cc1cc(Cl)c(-c2cc(C(=O)NCC[C@@H]3CCN(Cc4ccccc4)C3)ccc2Cl)cn1 nan
162370330 427505 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1cncc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5876755 427505 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1cncc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
160537419 427582 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 1 6 2.7 C[C@@H]1CN(c2ncc(C(=O)N(C)C)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5877742 427582 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 7 1 6 2.7 C[C@@H]1CN(c2ncc(C(=O)N(C)C)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129124761 427659 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2cnc(C#N)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5878736 427659 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@@H]1CN(c2cnc(C#N)nc2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158381507 427776 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 7 3 8 0.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(B(O)O)cc2)CC1 nan
CHEMBL5879999 427776 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 505 7 3 8 0.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccc(B(O)O)cc2)CC1 nan
129105356 427838 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(F)nc3)nn12 nan
CHEMBL5880643 427838 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(F)nc3)nn12 nan
129105385 428105 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 7 1 4 6.5 N#Cc1cc2ccccc2nc1-c1cc(C(=O)NCCC2CCN(Cc3ccccc3)CC2)ccc1Cl nan
CHEMBL5883727 428105 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 508 7 1 4 6.5 N#Cc1cc2ccccc2nc1-c1cc(C(=O)NCCC2CCN(Cc3ccccc3)CC2)ccc1Cl nan
159930151 428135 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1ccccc1C1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5884112 428135 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 3 4.9 COc1ccccc1C1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
129105211 428154 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 9 1 6 4.6 COc1cccc(CN2CCC(CCNC(=O)C3CCN(c4ccc(OC(F)(F)F)cc4)CC3)CC2)n1 nan
CHEMBL5884304 428154 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 9 1 6 4.6 COc1cccc(CN2CCC(CCNC(=O)C3CCN(c4ccc(OC(F)(F)F)cc4)CC3)CC2)n1 nan
162370343 428158 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 7 2 6 3.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccc(O)cc4)CC3)CC2)nc1 nan
CHEMBL5884338 428158 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 7 2 6 3.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccc(O)cc4)CC3)CC2)nc1 nan
129105459 428267 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 5 2.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN(C)[C@@H]1C[C@H](CO)N(Cc2ccccc2)C1 nan
CHEMBL5885607 428267 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 5 2.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN(C)[C@@H]1C[C@H](CO)N(Cc2ccccc2)C1 nan
162370220 428595 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2cncc(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5889513 428595 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 439 6 1 4 3.7 C[C@@H]1CN(c2cncc(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105174 428951 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2cccc(O)c2)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL5892932 428951 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2cccc(O)c2)CC1)c1ccc(Oc2ccccc2)cc1 nan
153682120 429285 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 8 1 4 4.3 COc1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5896227 429285 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 8 1 4 4.3 COc1cccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370409 429694 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 6 1 6 3.6 C[C@@H]1CN(c2ncc(C(=O)N3CCCC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
CHEMBL5900171 429694 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 6 1 6 3.6 C[C@@H]1CN(c2ncc(C(=O)N3CCCC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
162370346 429731 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 495 8 1 4 5.6 O=C(NCCC1CCN(CC2CCCCC2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5900644 429731 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 495 8 1 4 5.6 O=C(NCCC1CCN(CC2CCCCC2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
162370376 429852 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
CHEMBL5901760 429852 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccn2)CC1 nan
129105377 430009 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 7 1 4 3.1 CCN1CCN(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)CC1 nan
CHEMBL5903526 430009 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 7 1 4 3.1 CCN1CCN(C2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)CC1 nan
129105290 430219 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 6 1 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncccc2Cl)CC1 nan
CHEMBL5905504 430219 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 441 6 1 4 3.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ncccc2Cl)CC1 nan
162370325 430390 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 537 8 1 6 5.5 COc1ccc(-c2cc(C(F)(F)F)n3nc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)cc3n2)cc1 nan
CHEMBL5906949 430390 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 537 8 1 6 5.5 COc1ccc(-c2cc(C(F)(F)F)n3nc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)cc3n2)cc1 nan
135374995 430496 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 406 6 0 3 5.3 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2)CC1 nan
CHEMBL5907850 430496 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 406 6 0 3 5.3 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2)CC1 nan
162370379 430526 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 427 6 1 6 2.7 CC(C)CN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
CHEMBL5908125 430526 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 427 6 1 6 2.7 CC(C)CN1CCC(CCNC(=O)N2[C@H](C)CN(c3ncc(C#N)cn3)C[C@@H]2C)CC1 nan
129105319 430557 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 2 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 nan
CHEMBL5908461 430557 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 2 3 4.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 nan
162370381 431039 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 6 1 7 2.6 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCCO2)CC1 nan
CHEMBL5913533 431039 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 6 1 7 2.6 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCCO2)CC1 nan
162370216 431054 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 6 1 3 4.3 C[C@@H]1CN(c2ccccc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5913728 431054 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 6 1 3 4.3 C[C@@H]1CN(c2ccccc2F)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105431 431103 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 416 6 0 3 5.7 O=C(c1ccc(-c2cccs2)cc1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5914219 431103 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 416 6 0 3 5.7 O=C(c1ccc(-c2cccs2)cc1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
129105400 431195 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 444 6 2 2 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 nan
CHEMBL5915212 431195 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 444 6 2 2 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 nan
162370349 431201 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 1 4 5.1 CC(C)(C)CN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
CHEMBL5915275 431201 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 1 4 5.1 CC(C)(C)CN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
162370264 431203 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 7 2.8 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2cncnc2)CC1 nan
CHEMBL5915305 431203 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 6 1 7 2.8 C[C@@H]1CN(c2ncc(C(F)(F)F)cn2)CCN1C(=O)NCCC1CCN(Cc2cncnc2)CC1 nan
161857098 431235 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5915578 431235 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 nan
159168877 431465 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5917986 431465 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 nan
157579557 431493 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 4 4.4 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2ccccc2)CC1 nan
CHEMBL5918277 431493 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 1 4 4.4 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCC(O)(c2ccccc2)CC1 nan
157474507 431508 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.2 Cc1cc(C(=O)NC2CC2)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5918401 431508 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.2 Cc1cc(C(=O)NC2CC2)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
153682070 431769 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 6 1 4 4.6 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2F)CC1 nan
CHEMBL5921067 431769 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 6 1 4 4.6 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2F)CC1 nan
162370370 431919 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 527 7 1 5 6.1 Cc1c(C(=O)NCCC2CCN(CC3CCCCC3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
CHEMBL5922638 431919 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 527 7 1 5 6.1 Cc1c(C(=O)NCCC2CCN(CC3CCCCC3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
153682118 432007 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.4 N#Cc1cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5923730 432007 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 464 7 2 5 3.4 N#Cc1cc(N2CCC(O)(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
153682069 432126 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2c(F)cccc2F)CC1 nan
CHEMBL5924745 432126 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2c(F)cccc2F)CC1 nan
129105316 432205 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2F)CC1 nan
CHEMBL5925431 432205 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2ccccc2F)CC1 nan
153682104 432218 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 7 1 4 4.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(Cl)nc2)CC1 nan
CHEMBL5925583 432218 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 440 7 1 4 4.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(Cl)nc2)CC1 nan
162370327 432229 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccccc2OC(F)(F)F)CC1 nan
CHEMBL5925680 432229 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.6 CC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccccc2OC(F)(F)F)CC1 nan
153682127 432512 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 506 8 2 6 3.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
CHEMBL5928535 432512 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 506 8 2 6 3.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
162370363 432678 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 454 7 1 6 4.1 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccn3)nn12 nan
CHEMBL5930129 432678 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 454 7 1 6 4.1 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccn3)nn12 nan
160817536 432875 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5931963 432875 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 461 6 1 6 3.3 C[C@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105369 432904 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 432 6 1 5 3.1 N#Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
CHEMBL5932204 432904 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 432 6 1 5 3.1 N#Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
153682117 433050 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c(F)c1 nan
CHEMBL5933882 433050 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c(F)c1 nan
162370310 433089 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 538 8 2 6 4.7 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
CHEMBL5934292 433089 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 538 8 2 6 4.7 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)c1ccn2cc(-c3ccc(OC(F)(F)F)cc3)nc2c1 nan
129105274 433271 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 2 4 3.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(O)c2)CC1 nan
CHEMBL5936213 433271 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 6 2 4 3.5 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2cccc(O)c2)CC1 nan
129105453 443406 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2ccccc2O)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL5939938 443406 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2ccccc2O)CC1)c1ccc(Oc2ccccc2)cc1 nan
153682066 443457 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cc(F)cc(F)c2)CC1 nan
CHEMBL5940468 443457 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cc(F)cc(F)c2)CC1 nan
153682134 443532 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)nc2)CC1 nan
CHEMBL5941225 443532 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 7 1 4 4.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)nc2)CC1 nan
161843807 443554 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 7 2 7 1.8 N#Cc1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)C[C@H]2CO)nc1 nan
CHEMBL5941489 443554 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 463 7 2 7 1.8 N#Cc1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)C[C@H]2CO)nc1 nan
129105318 443702 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.0 CC(=O)c1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
CHEMBL5942975 443702 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 448 7 1 4 4.0 CC(=O)c1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
162370285 443742 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccnc2)CC1 nan
CHEMBL5943400 443742 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 462 6 1 7 2.7 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2cccnc2)CC1 nan
153682088 443802 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
CHEMBL5944037 443802 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 7 1 5 3.6 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
159841217 443829 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 477 6 0 4 4.6 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)N(C)CCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5944278 443829 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 477 6 0 4 4.6 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)N(C)CCC1CCN(Cc2ccccc2)CC1 nan
153682105 443923 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 436 8 1 5 3.7 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
CHEMBL5945140 443923 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 436 8 1 5 3.7 COc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)nc1 nan
162370255 443930 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2C#N)CC1 nan
CHEMBL5945230 443930 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2C#N)CC1 nan
129105239 443936 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2cccc(F)c2)CC1 nan
CHEMBL5945288 443936 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 423 6 1 2 5.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCC(c2cccc(F)c2)CC1 nan
160986230 443950 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 2 6 3.1 CC(C)NC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
CHEMBL5945371 443950 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 507 8 2 6 3.1 CC(C)NC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
162370305 444263 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 7 1 4 5.8 Cc1nc(-c2ccc(Cl)cc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5948699 444263 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 7 1 4 5.8 Cc1nc(-c2ccc(Cl)cc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
160203487 444274 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 421 6 1 4 3.6 C[C@@H]1CN(c2ccccn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5948760 444274 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 421 6 1 4 3.6 C[C@@H]1CN(c2ccccn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158639946 444328 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 425 6 0 4 4.4 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(F)cc2)CC1 nan
CHEMBL5949261 444328 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 425 6 0 4 4.4 O=C(OCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(F)cc2)CC1 nan
162370316 444342 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 538 9 2 6 3.5 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1)C1CN(c2ccccc2)CC1CO nan
CHEMBL5949403 444342 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 538 9 2 6 3.5 CN(CCNC(=O)C1CCN(c2ccc(OC(F)(F)F)c(F)c2)CC1)C1CN(c2ccccc2)CC1CO nan
162370375 444349 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 2 6 4.4 Cc1c(C(=O)NCCC2CCN(Cc3ccc(O)cc3)CC2)cnc2cc(-c3ccccc3)nn12 nan
CHEMBL5949463 444349 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 7 2 6 4.4 Cc1c(C(=O)NCCC2CCN(Cc3ccc(O)cc3)CC2)cnc2cc(-c3ccccc3)nn12 nan
157095996 444646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 465 6 1 6 3.0 C[C@@H]1CN(c2ncc(F)c(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5952694 444646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 465 6 1 6 3.0 C[C@@H]1CN(c2ncc(F)c(C#N)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105282 444701 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 7 1 5 4.7 Cc1nc(-c2ccc(F)nc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5953291 444701 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 438 7 1 5 4.7 Cc1nc(-c2ccc(F)nc2)sc1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158250287 444747 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 6 1 5 4.3 C[C@@H]1CN(c2ncc(Cl)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5953923 444747 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 6 1 5 4.3 C[C@@H]1CN(c2ncc(Cl)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158550607 445080 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 6 1 4 3.9 Cc1cncc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)c1 nan
CHEMBL5957539 445080 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 6 1 4 3.9 Cc1cncc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)c1 nan
162370187 445484 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 6 1 5 3.5 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)N(C)C[C@@H](O)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5961861 445484 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 6 1 5 3.5 C[C@@H]1CN(c2ccc(F)c(C#N)c2)CCN1C(=O)N(C)C[C@@H](O)C1CCN(Cc2ccccc2)CC1 nan
129105389 445735 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 N#Cc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
CHEMBL5964590 445735 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 449 6 1 4 3.8 N#Cc1cc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)ccc1F nan
162370353 445784 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 7 1 5 4.6 N#Cc1cccc(N2CCC(NC(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5965121 445784 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 7 1 5 4.6 N#Cc1cccc(N2CCC(NC(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
129105213 445911 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 6 1 3 4.6 N#CC1(c2ccccc2)CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL5966421 445911 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 6 1 3 4.6 N#CC1(c2ccccc2)CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CC1 nan
162370319 446111 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 10 1 3 5.2 O=C(Cc1ccc(OCc2ccccc2)cc1)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL5968567 446111 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 10 1 3 5.2 O=C(Cc1ccc(OCc2ccccc2)cc1)NCCC1CCN(Cc2ccccc2)CC1 nan
162370345 446183 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 9 1 4 5.1 CC(C)CCN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
CHEMBL5969304 446183 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 469 9 1 4 5.1 CC(C)CCN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
162370322 446317 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.4 O=C(CCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL5970768 446317 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.4 O=C(CCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
129105205 446376 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 429 9 1 4 4.7 O=C(NCCC1CCN(Cc2cccnc2)CC1)c1ccc(OCc2ccccc2)cc1 nan
CHEMBL5971380 446376 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 429 9 1 4 4.7 O=C(NCCC1CCN(Cc2cccnc2)CC1)c1ccc(OCc2ccccc2)cc1 nan
129105372 446397 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 481 7 1 3 6.4 Cc1cc(Cl)c(-c2cc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)ccc2Cl)cn1 nan
CHEMBL5971600 446397 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 481 7 1 3 6.4 Cc1cc(Cl)c(-c2cc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)ccc2Cl)cn1 nan
159864748 446614 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 6 0 5 4.3 N#Cc1cc(F)cc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL5974047 446614 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 6 0 5 4.3 N#Cc1cc(F)cc(N2CCN(C(=O)OCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370411 446770 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.5 C[C@@H]1CN(c2ncc(C(=O)NCC3CC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
CHEMBL5975894 446770 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 8 2 6 3.5 C[C@@H]1CN(c2ncc(C(=O)NCC3CC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(c2ccccc2)CC1 nan
162370384 447006 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC23CC(C2)C3)CC1 nan
CHEMBL5978853 447006 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 6 1 6 2.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC23CC(C2)C3)CC1 nan
162370372 447143 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3ccncc3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
CHEMBL5980322 447143 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3ccncc3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
129105418 447324 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 6 1 4 3.7 N#Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
CHEMBL5982129 447324 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 431 6 1 4 3.7 N#Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)cc1 nan
162370350 447340 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 10 1 3 5.9 O=C(NCCC1CCN(CCCc2ccccc2)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL5982272 447340 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 10 1 3 5.9 O=C(NCCC1CCN(CCCc2ccccc2)CC1)c1ccc(Oc2ccccc2)cc1 nan
153682092 447396 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 414 7 2 3 5.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(O)cc2)cc1 nan
CHEMBL5982861 447396 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 414 7 2 3 5.1 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2ccc(O)cc2)cc1 nan
162370341 447471 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 9 1 3 5.9 CC(c1ccccc1)N1CCC(CCNC(=O)c2ccc(OCc3ccccc3)cc2)CC1 nan
CHEMBL5983572 447471 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 442 9 1 3 5.9 CC(c1ccccc1)N1CCC(CCNC(=O)c2ccc(OCc3ccccc3)cc2)CC1 nan
153682089 447543 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 7 1 3 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(SC(F)(F)F)cc1 nan
CHEMBL5984424 447543 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 422 7 1 3 5.3 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(SC(F)(F)F)cc1 nan
129105265 447660 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 8 1 5 4.6 Cn1cccc1CN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
CHEMBL5985837 447660 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 492 8 1 5 4.6 Cn1cccc1CN1CCC(CCNC(=O)C2CCN(c3ccc(OC(F)(F)F)cc3)CC2)CC1 nan
129105368 447736 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 528 8 2 4 5.7 O=C(NCCC1CCN(Cc2ccc3[nH]ccc3c2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL5986616 447736 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 528 8 2 4 5.7 O=C(NCCC1CCN(Cc2ccc3[nH]ccc3c2)CC1)C1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
129105412 447867 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 494 7 1 7 3.1 COC(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL5988015 447867 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 494 7 1 7 3.1 COC(=O)c1cc(C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
162370364 448042 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 7 1 6 4.6 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C#N)cc3)nn12 nan
CHEMBL5989864 448042 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 478 7 1 6 4.6 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccc(C#N)cc3)nn12 nan
135375151 448315 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3cccnc3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
CHEMBL5992462 448315 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 522 7 1 6 5.2 Cc1c(C(=O)NCCC2CCN(Cc3cccnc3)CC2)cnc2cc(-c3cccc(C(F)(F)F)c3)nn12 nan
162370410 448320 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 6 3.3 C=CCNC(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
CHEMBL5992519 448320 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 519 9 2 6 3.3 C=CCNC(=O)c1cnc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)nc1 nan
153682067 448420 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cc(F)ccc2F)CC1 nan
CHEMBL5993563 448420 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 510 6 1 3 4.9 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2cc(F)ccc2F)CC1 nan
162370302 448493 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 7 1 3 5.2 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)cc2)C1 nan
CHEMBL5994342 448493 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 488 7 1 3 5.2 CN(C(=O)NCCC1CCN(Cc2ccccc2)CC1)C1CCN(c2ccc(C(F)(F)F)cc2)C1 nan
153682139 448586 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 5 3.7 Cc1cc(C)nc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)n1 nan
CHEMBL5995191 448586 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 435 7 1 5 3.7 Cc1cc(C)nc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)n1 nan
135375149 448607 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 410 6 0 2 5.6 O=C(c1ccc(-c2ccccc2)cc1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
CHEMBL5995432 448607 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 410 6 0 2 5.6 O=C(c1ccc(-c2ccccc2)cc1)N(C1CC1)C1CCN(Cc2ccccc2)CC1 nan
162370235 448637 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 2 7 3.3 CNc1nc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)ncc1C#N nan
CHEMBL5995731 448637 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 7 2 7 3.3 CNc1nc(N2C[C@@H](C)N(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@@H](C)C2)ncc1C#N nan
129105477 448782 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 6 1 3 4.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(F)cc2)CC1 nan
CHEMBL5997458 448782 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 6 1 3 4.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccc(F)cc2)CC1 nan
153682129 448947 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 9 1 6 4.4 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
CHEMBL5999145 448947 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 520 9 1 6 4.4 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(OC(F)(F)F)cn2)CC1 nan
159915214 449020 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 6 1 3 4.2 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCC[C@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL6000076 449020 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 460 6 1 3 4.2 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCC[C@H]1CCN(Cc2ccccc2)C1 nan
129105198 449047 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2ccc(O)cc2)CC1)c1ccc(Oc2ccccc2)cc1 nan
CHEMBL6000299 449047 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 430 8 2 4 5.2 O=C(NCCC1CCN(Cc2ccc(O)cc2)CC1)c1ccc(Oc2ccccc2)cc1 nan
162370268 449120 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 6 3.3 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CCc2ccccc2)CC1 nan
CHEMBL6001109 449120 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 7 1 6 3.3 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CCc2ccccc2)CC1 nan
129105299 449228 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 404 7 1 3 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2cccs2)cc1 nan
CHEMBL6002474 449228 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 404 7 1 3 5.4 O=C(NCCC1CCN(Cc2ccccc2)CC1)c1ccc(-c2cccs2)cc1 nan
129105425 449324 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 6 1 3 4.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccccc2F)CC1 nan
CHEMBL6003491 449324 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 424 6 1 3 4.0 O=C(NCCC1CCN(Cc2ccccc2)CC1)N1CCN(c2ccccc2F)CC1 nan
129105363 449526 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 445 7 2 4 4.1 N#Cc1cccc(N2CCC(NC(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
CHEMBL6005342 449526 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 445 7 2 4 4.1 N#Cc1cccc(N2CCC(NC(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c1 nan
162370382 449719 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 1 7 2.1 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2(C)COC2)CC1 nan
CHEMBL6007290 449719 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 455 6 1 7 2.1 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2(C)COC2)CC1 nan
162370273 449879 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 6 2 6 4.4 Cc1cc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4cnc(C(F)(F)F)nc4)C[C@@H]3C)CC2)ccc1O nan
CHEMBL6008973 449879 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 6 2 6 4.4 Cc1cc(CN2CCC(CCNC(=O)N3[C@H](C)CN(c4cnc(C(F)(F)F)nc4)C[C@@H]3C)CC2)ccc1O nan
162370233 450012 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 6 1 5 4.4 C[C@@H]1CN(c2ncc(Br)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6010358 450012 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 534 6 1 5 4.4 C[C@@H]1CN(c2ncc(Br)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370317 450063 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.4 O=C(CCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL6011046 450063 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 489 8 1 4 5.4 O=C(CCC1CCN(Cc2ccccc2)CC1)NC1CCN(c2ccc(OC(F)(F)F)cc2)CC1 nan
153683045 450355 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 9 2 5 3.8 O=C(NCCN[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
CHEMBL6014365 450355 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 490 9 2 5 3.8 O=C(NCCN[C@@H]1CCN(Cc2ccccc2)C1)C1CCN(c2cccc(OC(F)(F)F)c2)CC1 nan
129105233 450394 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 429 8 2 3 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)Nc1ccc(Oc2ccccc2)cc1 nan
CHEMBL6014683 450394 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 429 8 2 3 5.9 O=C(NCCC1CCN(Cc2ccccc2)CC1)Nc1ccc(Oc2ccccc2)cc1 nan
162370361 451030 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 459 7 1 6 4.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccs3)nn12 nan
CHEMBL6021316 451030 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 459 7 1 6 4.8 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccs3)nn12 nan
162370303 451064 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 2 4 3.6 Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c(CO)c1 nan
CHEMBL6021705 451064 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 450 7 2 4 3.6 Cc1ccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)CC2)c(CO)c1 nan
158365193 451280 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 533 10 1 5 4.9 O=C(C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)N(CCO)CCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6024044 451280 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 533 10 1 5 4.9 O=C(C1CCN(c2ccc(OC(F)(F)F)cc2)CC1)N(CCO)CCC1CCN(Cc2ccccc2)CC1 nan
162370197 451286 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cccnc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)[C@H](C)C1 nan
CHEMBL6024130 451286 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cccnc1N1CCN(C(=O)NCCC2CCN(Cc3ccccc3)CC2)[C@H](C)C1 nan
162370348 451417 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 7 2 6 3.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4O)CC3)CC2)nc1 nan
CHEMBL6025478 451417 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 447 7 2 6 3.3 N#Cc1ccc(N2CCC(C(=O)NCCC3CCN(Cc4ccccc4O)CC3)CC2)nc1 nan
162370356 451827 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 7 1 5 4.7 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccc3)nn12 nan
CHEMBL6030077 451827 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 453 7 1 5 4.7 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3ccccc3)nn12 nan
153682097 452196 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.5 CC1CN(c2ccccc2OC(F)(F)F)CCC1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6033735 452196 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 503 8 1 4 5.5 CC1CN(c2ccccc2OC(F)(F)F)CCC1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
129105346 462488 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 9 1 3 5.4 O=C(NCCC1CCN(Cc2cccc(F)c2)CC1)c1ccc(OCc2ccccc2)cc1 nan
CHEMBL6040289 462488 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 446 9 1 3 5.4 O=C(NCCC1CCN(Cc2cccc(F)c2)CC1)c1ccc(OCc2ccccc2)cc1 nan
162370374 462676 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1cccc(CN2CCC(CCNC(=O)c3cnc4cc(-c5ccccc5)nn4c3C)CC2)c1 nan
CHEMBL6042258 462676 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1cccc(CN2CCC(CCNC(=O)c3cnc4cc(-c5ccccc5)nn4c3C)CC2)c1 nan
162370217 462816 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL6043660 462816 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 451 7 1 5 3.6 COc1cccc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
129105379 462853 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 413 8 1 3 4.3 CN(CCNC(=O)c1ccc(-c2ccccc2)cc1)[C@@H]1CCN(Cc2ccccc2)C1 nan
CHEMBL6044036 462853 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 413 8 1 3 4.3 CN(CCNC(=O)c1ccc(-c2ccccc2)cc1)[C@@H]1CCN(Cc2ccccc2)C1 nan
162370323 462869 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1ccc(-c2cc3ncc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)c(C)n3n2)cc1 nan
CHEMBL6044171 462869 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 483 8 1 6 4.7 COc1ccc(-c2cc3ncc(C(=O)NCCC4CCN(Cc5ccccc5)CC4)c(C)n3n2)cc1 nan
160310139 463003 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 466 7 2 6 2.7 C[C@@H]1CN(c2ncc(C(=O)O)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6045340 463003 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 466 7 2 6 2.7 C[C@@H]1CN(c2ncc(C(=O)O)cn2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
162370412 463246 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 533 8 2 6 3.7 C[C@@H]1CN(c2ncc(C(=O)NC3CCC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6047699 463246 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 533 8 2 6 3.7 C[C@@H]1CN(c2ncc(C(=O)NC3CCC3)cn2)C[C@H](C)N1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
153682130 463263 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 7 2 4 3.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cc(F)ccc2F)CC1 nan
CHEMBL6047873 463263 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 457 7 2 4 3.7 O=C(NCCC1CCN(Cc2ccccc2)CC1)C1(O)CCN(c2cc(F)ccc2F)CC1 nan
162370383 463289 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 6 1 8 1.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCS(=O)(=O)C2)CC1 nan
CHEMBL6048120 463289 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 517 6 1 8 1.9 C[C@@H]1CN(c2ncc(C#N)cn2)C[C@H](C)N1C(=O)NCCC1CCN(CC2CCCS(=O)(=O)C2)CC1 nan
129105227 463646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 10 2 5 5.0 COc1cccc(CN2CCC(CCNC(=O)c3ccc(OCc4ccccc4)cc3)CC2)c1O nan
CHEMBL6051662 463646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 10 2 5 5.0 COc1cccc(CN2CCC(CCNC(=O)c3ccc(OCc4ccccc4)cc3)CC2)c1O nan
129105340 463690 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 2 6 3.4 Cc1cc(C(=O)NC(C)C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
CHEMBL6052099 463690 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 521 8 2 6 3.4 Cc1cc(C(=O)NC(C)C)nc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)n1 nan
162370245 463700 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
CHEMBL6052276 463700 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 499 6 1 4 4.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccc(C#N)cc2)CC1 nan
160094233 463846 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2OC(F)(F)F)CC1 nan
CHEMBL6053795 463846 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 558 7 1 4 5.5 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCC1CCN(Cc2ccccc2OC(F)(F)F)CC1 nan
153682115 463943 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 8 1 5 4.5 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(C(F)(F)F)cn2)CC1 nan
CHEMBL6054801 463943 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 504 8 1 5 4.5 COC1(C(=O)NCCC2CCN(Cc3ccccc3)CC2)CCN(c2ccc(C(F)(F)F)cn2)CC1 nan
162370253 464071 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 556 7 1 6 4.9 Cc1nnc(C(c2ccccc2)N2CCC(CCNC(=O)N3CCN(c4cc(F)c(F)c(F)c4)C[C@H]3C)CC2)o1 nan
CHEMBL6056118 464071 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 556 7 1 6 4.9 Cc1nnc(C(c2ccccc2)N2CCC(CCNC(=O)N3CCN(c4cc(F)c(F)c(F)c4)C[C@H]3C)CC2)o1 nan
129105411 464085 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 1 4 3.1 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN1CCN(Cc2ccccc2)CC1 nan
CHEMBL6056272 464085 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 475 6 1 4 3.1 C[C@@H]1CN(c2cc(F)c(F)c(F)c2)CCN1C(=O)NCCN1CCN(Cc2ccccc2)CC1 nan
129105384 464384 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccnc3F)nn12 nan
CHEMBL6059338 464384 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 472 7 1 6 4.3 Cc1c(C(=O)NCCC2CCN(Cc3ccccc3)CC2)cnc2cc(-c3cccnc3F)nn12 nan
157812398 464558 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 5 3.8 C[C@@H]1CN(c2ncc(F)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
CHEMBL6061461 464558 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 474 6 1 5 3.8 C[C@@H]1CN(c2ncc(F)c(Cl)n2)CCN1C(=O)NCCC1CCN(Cc2ccccc2)CC1 nan
158074086 464646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 414 7 1 6 3.2 N#Cc1ccc(-n2cnc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c2)nc1 nan
CHEMBL6062275 464646 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 414 7 1 6 3.2 N#Cc1ccc(-n2cnc(C(=O)NCCC3CCN(Cc4ccccc4)CC3)c2)nc1 nan
157951939 464878 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 8 2 6 2.7 CCNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
CHEMBL6064835 464878 0 None None None Human 6.3 pKi = 6.3 Binding
Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.Binding Assay: Binding affinity (Ki) of compounds was measured by inhibition of radioligand binding to membranes from CHO cells expressing human M1, M2, M3, M4 and M5 receptors. Membranes were prepared by nitrogen cavitation and differential centrifugation as previously described (Hoare et al., Mol. Pharmacol. 2003 March; 63(3): 751-65). The radioligand employed was tritiated N-methylscopolamine, used at a concentration of 1.5 nM. A dose-response of twelve concentrations of compound was used, ranging from 10 μM to 32 μM. The assay buffer was 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 1 mM ethylenediaminetetraacetic acid, pH-adjusted to pH 7.4.
ChEMBL 493 8 2 6 2.7 CCNC(=O)c1cnc(N2CCN(C(=O)NCCC3CCN(Cc4ccccc4)CC3)[C@H](C)C2)nc1 nan
103 8980 49 None -31 31 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 8980 49 None -31 31 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 8980 49 None -31 31 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 8980 49 None -31 31 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 8980 49 None -31 31 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5318 39468 43 None 1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 39468 43 None 1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB06820 39468 43 None 1 13 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
155548586 350560 0 None -10 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597611 350560 0 None -10 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
156016047 352175 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650722 352175 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
24894514 346867 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL450729 346867 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
14537188 273980 0 None -3388 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
CHEMBL37372 273980 0 None -3388 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
155543345 350646 0 None -6 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598362 350646 0 None -6 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
71575652 177077 0 None -10 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312352 177077 0 None -10 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
137645938 313479 0 None -416 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 313479 0 None -416 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
2719 1891 63 None -1 8 Human 5.2 pKi = 5.2 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
5535 1891 63 None -1 8 Human 5.2 pKi = 5.2 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
607 1891 63 None -1 8 Human 5.2 pKi = 5.2 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
CHEMBL76 1891 63 None -1 8 Human 5.2 pKi = 5.2 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
DB00608 1891 63 None -1 8 Human 5.2 pKi = 5.2 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
162353379 354825 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
CHEMBL4758449 354825 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
46227461 38056 0 None -1 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198077 38056 0 None -1 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
1634 163834 36 None -8 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
4011 163834 36 None -8 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 163834 36 None -8 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
DB00934 163834 36 None -8 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
164620270 371745 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028587 371745 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44593625 371350 0 None -5 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 371350 0 None -5 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
156015971 352197 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650880 352197 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
164627575 371802 0 None -33 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 21 8 11 1.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029004 371802 0 None -33 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 21 8 11 1.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
118719925 234714 0 None -7 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
CHEMBL3354072 234714 0 None -7 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
162353381 353911 0 None -52 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 287 4 1 4 2.9 O=C(CCN1CCCc2ccccc21)Nc1nccs1 10.1016/j.bmcl.2020.127632
CHEMBL4747438 353911 0 None -52 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 287 4 1 4 2.9 O=C(CCN1CCCc2ccccc21)Nc1nccs1 10.1016/j.bmcl.2020.127632
162353380 356313 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4786868 356313 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
24894633 350857 0 None -3 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL461709 350857 0 None -3 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
9843967 311417 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding ability of compound to m4 muscarinic receptorBinding ability of compound to m4 muscarinic receptor
ChEMBL 400 7 1 5 3.4 Nc1cccc(-c2ccc(CCN3CCN(CC(=O)c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(99)00432-1
CHEMBL40391 311417 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding ability of compound to m4 muscarinic receptorBinding ability of compound to m4 muscarinic receptor
ChEMBL 400 7 1 5 3.4 Nc1cccc(-c2ccc(CCN3CCN(CC(=O)c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(99)00432-1
137645406 313787 0 None -74 13 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 313787 0 None -74 13 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
73355420 183359 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432061 183359 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44437249 26146 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182436 26146 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
44437259 26153 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182448 26153 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
13567081 25514 0 None -5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1178839 25514 0 None -5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
178315524 467824 0 None -5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 841 24 3 11 4.7 NCCOCCOCCC(=O)NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
CHEMBL6199292 467824 0 None -5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 841 24 3 11 4.7 NCCOCCOCCC(=O)NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
44455198 197960 0 None -1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
CHEMBL271108 197960 0 None -1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
44455198 197960 0 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
CHEMBL271108 197960 0 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
135398737 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
2818 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL253391 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 1973 61 None -8 61 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
132947 8408 6 None -34 9 Human 8.2 pKi = 8.2 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
361 8408 6 None -34 9 Human 8.2 pKi = 8.2 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL265256 8408 6 None -34 9 Human 8.2 pKi = 8.2 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
155519740 334960 0 None -23 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
CHEMBL4448108 334960 0 None -23 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
129989 933 31 None -2 11 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 933 31 None -2 11 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 933 31 None -2 11 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
11498 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
4995951 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
CHEMBL59898 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
152278786 366136 1 None -7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 366136 1 None -7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
118719923 234712 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354070 234712 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44386115 259321 0 None -28 5 Human 7.2 pKi = 7.2 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL369062 259321 0 None -28 5 Human 7.2 pKi = 7.2 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
2230 961 44 None -436 10 Human 4.2 pKi = 4.2 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
296 961 44 None -436 10 Human 4.2 pKi = 4.2 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
CHEMBL7303 961 44 None -436 10 Human 4.2 pKi = 4.2 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
DB04365 961 44 None -436 10 Human 4.2 pKi = 4.2 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
11808947 122232 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL171216 122232 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44593627 384960 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 384960 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44437295 26167 0 None -6 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182472 26167 0 None -6 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
9894173 39048 6 None -69 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
CHEMBL12098 39048 6 None -69 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
155522355 350377 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596065 350377 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
135430667 19297 0 None 35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
CHEMBL104803 19297 0 None 35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
9968046 404314 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL57485 404314 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
11045444 121970 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL170088 121970 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44448417 26183 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182629 26183 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
172472598 389522 0 None -8 6 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 772 11 1 10 5.7 O=C1CCC(N2Cc3cc(C4CCN(C(=O)CCCCCN5CCC(c6ccc(Oc7nn8cnnc8c8c7CCCC8)cc6)CC5)CC4)ccc3C2=O)C(=O)N1 10.6019/CHEMBL5463725
CHEMBL5465171 389522 0 None -8 6 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 772 11 1 10 5.7 O=C1CCC(N2Cc3cc(C4CCN(C(=O)CCCCCN5CCC(c6ccc(Oc7nn8cnnc8c8c7CCCC8)cc6)CC5)CC4)ccc3C2=O)C(=O)N1 10.6019/CHEMBL5463725
66561966 156372 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 193 2 0 1 3.2 C1CCC(CN2C3CCC2CC3)CC1 10.1016/j.bmcl.2012.04.077
CHEMBL2030625 156372 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 193 2 0 1 3.2 C1CCC(CN2C3CCC2CC3)CC1 10.1016/j.bmcl.2012.04.077
73346336 183353 0 None -1 6 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432054 183353 0 None -1 6 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
71128 197136 21 None -39 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL26505 197136 21 None -39 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
155522355 350377 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596065 350377 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
10770914 58753 0 None -11 4 Rat 7.2 pKi = 7.2 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL134692 58753 0 None -11 4 Rat 7.2 pKi = 7.2 Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
16094783 273997 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 273997 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
164621443 371755 0 None -37 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028653 371755 0 None -37 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2551 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
298 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
488 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
5831 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
CHEMBL965 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
DB00411 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
164622564 371760 0 None -25 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028706 371760 0 None -25 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162353371 355497 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 CC1CCc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4775999 355497 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 CC1CCc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
2551 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
298 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
488 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
5831 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL965 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB00411 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
2551 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
298 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
488 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
5831 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
CHEMBL965 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
DB00411 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
300 5101 11 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
4141 5101 11 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
CHEMBL92387 5101 11 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
2551 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
298 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
488 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
5831 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
CHEMBL965 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
DB00411 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
2551 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
298 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
488 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
5831 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
CHEMBL965 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
DB00411 1644 11 None -38 11 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
156010398 352151 0 None -31 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650561 352151 0 None -31 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
172472598 389522 0 None -8 6 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 772 11 1 10 5.7 O=C1CCC(N2Cc3cc(C4CCN(C(=O)CCCCCN5CCC(c6ccc(Oc7nn8cnnc8c8c7CCCC8)cc6)CC5)CC4)ccc3C2=O)C(=O)N1 10.6019/CHEMBL5463725
CHEMBL5465171 389522 0 None -8 6 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 772 11 1 10 5.7 O=C1CCC(N2Cc3cc(C4CCN(C(=O)CCCCCN5CCC(c6ccc(Oc7nn8cnnc8c8c7CCCC8)cc6)CC5)CC4)ccc3C2=O)C(=O)N1 10.6019/CHEMBL5463725
2536 308773 12 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
5354 308773 12 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
CHEMBL404849 308773 12 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 nan
44627744 28281 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197389 28281 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
11034265 239030 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL353290 239030 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
162353393 353330 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
CHEMBL4740422 353330 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
24894628 346776 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
CHEMBL471942 346776 0 None -2 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
177372525 393573 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 293 3 0 4 3.1 CN1CCC(Oc2nc3ccccc3n2-c2ccccc2)C1 10.1016/j.ejmech.2023.115891
CHEMBL5639365 393573 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 293 3 0 4 3.1 CN1CCC(Oc2nc3ccccc3n2-c2ccccc2)C1 10.1016/j.ejmech.2023.115891
15157139 199999 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285440 199999 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
73353884 183131 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 183131 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
71463063 174788 0 None -1 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 174788 0 None -1 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44318851 214439 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 214439 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
11808946 239272 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354678 239272 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
25147647 355970 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@H]21 10.1016/j.bmc.2008.06.025
CHEMBL478226 355970 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@H]21 10.1016/j.bmc.2008.06.025
156009698 352251 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651200 352251 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
11015312 19611 0 None 15 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106505 19611 0 None 15 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
1016 8173 46 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
422063 392615 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL560649 392615 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
44439394 291859 0 None -398 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccc(CC2NCCc3c2[nH]c2ccccc32)cc1 10.1016/j.bmcl.2007.01.093
CHEMBL391191 291859 0 None -398 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccc(CC2NCCc3c2[nH]c2ccccc32)cc1 10.1016/j.bmcl.2007.01.093
73355418 183354 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432056 183354 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
24809738 26163 0 None -13 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182466 26163 0 None -13 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
71450550 174794 0 None -1 16 Human 6.2 pKi = 6.2 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 174794 0 None -1 16 Human 6.2 pKi = 6.2 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
164609302 371667 0 None -36 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027951 371667 0 None -36 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44207909 40583 6 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1242923 40583 6 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
44422699 26125 0 None -10 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182272 26125 0 None -10 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
24894631 350724 1 None -2 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
CHEMBL460470 350724 1 None -2 5 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
73355416 183345 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 0 3 1.8 CN(Cc1cccnc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432043 183345 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 0 3 1.8 CN(Cc1cccnc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
11498 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
4995951 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
CHEMBL59898 6149 38 None 19 13 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
11143997 19361 0 None 32 5 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL105122 19361 0 None 32 5 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
315401 180641 1 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377387 180641 1 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
71128 197136 21 None -39 5 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
CHEMBL26505 197136 21 None -39 5 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
178308480 467814 0 None -4 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 682 15 2 8 5.1 NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
CHEMBL6198855 467814 0 None -4 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 682 15 2 8 5.1 NCCOCCOCCNc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
164610746 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164621305 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164623076 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028038 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028642 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028732 371671 0 None -28 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164617895 371728 0 None -41 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028466 371728 0 None -41 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
137638270 312793 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 312793 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
129989 933 31 None -2 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 933 31 None -2 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 933 31 None -2 11 Human 8.1 pKi = 8.1 Binding
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
118719921 234709 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 234709 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
57326325 158823 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078987 158823 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
156014205 352207 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650957 352207 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
57326325 158823 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078987 158823 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44439405 182611 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 440 4 0 5 5.3 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL241282 182611 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 440 4 0 5 5.3 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1CC3)CC2 10.1016/j.bmcl.2007.01.093
44318930 215852 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 215852 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
44439389 182579 0 None -8 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 324 3 1 5 2.8 COc1ccc2[nH]c3c(c2c1)CCN=C3c1cc([N+](=O)[O-])cn1C 10.1016/j.bmcl.2007.01.093
CHEMBL241099 182579 0 None -8 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 324 3 1 5 2.8 COc1ccc2[nH]c3c(c2c1)CCN=C3c1cc([N+](=O)[O-])cn1C 10.1016/j.bmcl.2007.01.093
53324553 119653 0 None 1 10 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 119653 0 None 1 10 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 119653 0 None 1 10 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 119653 0 None 1 10 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
73352414 183340 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
CHEMBL2432038 183340 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
164613685 371693 0 None -24 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164620290 371693 0 None -24 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028207 371693 0 None -24 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028589 371693 0 None -24 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164617650 371724 0 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 676 13 8 9 -0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028445 371724 0 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 676 13 8 9 -0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
3652 8876 57 None -3 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 8876 57 None -3 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 8876 57 None -3 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 8876 57 None -3 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 8876 57 None -3 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
11092603 19200 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104332 19200 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10874119 19246 0 None 15 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104574 19246 0 None 15 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
164613685 371693 0 None -24 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164620290 371693 0 None -24 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028207 371693 0 None -24 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028589 371693 0 None -24 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
137640201 312873 2 None -575 13 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 312873 2 None -575 13 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
162353372 355238 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4763422 355238 0 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
156014875 352156 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650577 352156 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
73350932 183344 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 339 5 0 4 2.5 COc1ccc(CN(C)[C@H]2C3C4CC5C3C(=O)C3C5C4C32)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432042 183344 0 None None None Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 339 5 0 4 2.5 COc1ccc(CN(C)[C@H]2C3C4CC5C3C(=O)C3C5C4C32)cc1OC 10.1016/j.bmc.2013.07.045
44385809 124224 0 None -22 5 Human 7.1 pKi = 7.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL177040 124224 0 None -22 5 Human 7.1 pKi = 7.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44448421 26606 0 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185269 26606 0 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
10925451 121559 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL168707 121559 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
10066369 238928 0 None -22 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 238928 0 None -22 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
11011332 239431 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355560 239431 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
108993439 353745 0 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4745429 353745 0 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
49783209 41478 0 None -1318 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 41478 0 None -1318 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
2551 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
298 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
488 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
5831 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
CHEMBL965 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
DB00411 1644 11 None -38 11 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
44627742 407602 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL576707 407602 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
109032820 366253 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4791819 366253 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
11154555 1656 51 None -2754 24 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
5037 1656 51 None -2754 24 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
7671 1656 51 None -2754 24 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
CHEMBL2028019 1656 51 None -2754 24 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
DB06016 1656 51 None -2754 24 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
44439388 182572 0 None -22 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 3 1 3 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL241082 182572 0 None -22 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 3 1 3 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
1200 3405 44 None -12 23 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
12488 3405 44 None -12 23 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 3405 44 None -12 23 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 3405 44 None -12 23 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 3405 44 None -12 23 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
10226457 27237 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL1189471 27237 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
155525065 350519 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597243 350519 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
16094791 164669 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 164669 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44304818 468335 0 None -30 7 Rat 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 468335 0 None -30 7 Rat 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44304818 468335 0 None -30 7 Human 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 468335 0 None -30 7 Human 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44437270 26597 0 None -19 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1185211 26597 0 None -19 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
44299564 423685 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL58824 423685 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
10109893 163593 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 163593 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
156012563 352163 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650635 352163 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
24894515 350827 1 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL461502 350827 1 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
4841 139710 2 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 139710 2 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
319 7908 34 None -9 9 Human 8.1 pKi = 8.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
444031 7908 34 None -9 9 Human 8.1 pKi = 8.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
784 7908 34 None -9 9 Human 8.1 pKi = 8.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
CHEMBL1346 7908 34 None -9 9 Human 8.1 pKi = 8.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
324 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
10660 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
441281 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL1200406 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB00985 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB13636 2953 69 None -1 13 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
11748799 330292 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL423831 330292 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
71455896 174792 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205832 174792 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccn1 10.1016/j.bmcl.2012.08.046
10035281 201121 0 None -1 8 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 201121 0 None -1 8 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
10035281 201121 0 None -3 8 Rat 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 201121 0 None -3 8 Rat 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10035281 201121 0 None -1 8 Human 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 201121 0 None -1 8 Human 5.1 pKi = 5.1 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10871551 239153 0 None -7 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354523 239153 0 None -7 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
11000399 121876 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169680 121876 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
44318766 470567 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 470567 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
44318851 214439 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 214439 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL4755229 478371 38 None None None Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 557 8 2 10 2.2 CNC(=O)COc1cc2cc(Nc3nc(N4CCC(C(=O)N(C)C)CC4)ncc3Cl)cc(OC)c2n(C)c1=O 10.6019/CHEMBL5303764
11131099 238931 0 None -8 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352404 238931 0 None -8 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
187 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
294 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
65 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL667 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB03128 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
145961152 317131 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
145962050 317131 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4129382 317131 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4130037 317131 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44634573 5612 1 None -8 12 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442175
9168 5612 1 None -8 12 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442175
CHEMBL1474387 5612 1 None -8 12 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442175
CHEMBL1622930 5612 1 None -8 12 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442175
68764898 1384 3 None -2 3 Human 6.1 pKi = 6.1 Binding
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 1384 3 None -2 3 Human 6.1 pKi = 6.1 Binding
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 1384 3 None -2 3 Human 6.1 pKi = 6.1 Binding
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
162353383 356394 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
CHEMBL4787944 356394 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
11110049 121030 0 None -2 4 Human 4.1 pKi = 4.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL168223 121030 0 None -2 4 Human 4.1 pKi = 4.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
162353387 355085 0 None -2 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 2 1 3 2.2 O=C(CN1CCCc2ccc(O)cc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4761549 355085 0 None -2 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 2 1 3 2.2 O=C(CN1CCCc2ccc(O)cc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
44422692 26127 0 None -9 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 26127 0 None -9 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
3675988 350794 38 None -7 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
CHEMBL461087 350794 38 None -7 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
44446841 26607 0 None -5 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1185281 26607 0 None -5 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
46227481 38058 0 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198081 38058 0 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL4755229 478371 38 None None None Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 557 8 2 10 2.2 CNC(=O)COc1cc2cc(Nc3nc(N4CCC(C(=O)N(C)C)CC4)ncc3Cl)cc(OC)c2n(C)c1=O 10.6019/CHEMBL5303764
155523889 350489 0 None -11 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597014 350489 0 None -11 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
73345823 180644 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377392 180644 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
1821 410750 60 None -1 4 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
4212 410750 60 None -1 4 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL58 410750 60 None -1 4 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
DB01204 410750 60 None -1 4 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
10315426 201186 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL294663 201186 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
44299616 385073 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL55698 385073 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
133640439 355224 1 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4763304 355224 1 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
172472599 389523 0 None -12 6 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 758 11 1 9 6.2 O=C1NCCCC1N1Cc2cc(C3CCN(C(=O)CCCCCN4CCC(c5ccc(Oc6nn7cnnc7c7c6CCCC7)cc5)CC4)CC3)ccc2C1=O 10.6019/CHEMBL5463725
CHEMBL5465172 389523 0 None -12 6 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 758 11 1 9 6.2 O=C1NCCCC1N1Cc2cc(C3CCN(C(=O)CCCCCN4CCC(c5ccc(Oc6nn7cnnc7c7c6CCCC7)cc5)CC4)CC3)ccc2C1=O 10.6019/CHEMBL5463725
162353377 355023 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760904 355023 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
657347 19415 0 None -75 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL105457 19415 0 None -75 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
44274477 330444 0 None -3 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
CHEMBL424214 330444 0 None -3 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
7047822 350795 15 None -3 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
CHEMBL461088 350795 15 None -3 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
73346334 183349 0 None 1 7 Human 6.1 pKi = 6.1 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432048 183349 0 None 1 7 Human 6.1 pKi = 6.1 Binding
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
172472599 389523 0 None -12 6 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 758 11 1 9 6.2 O=C1NCCCC1N1Cc2cc(C3CCN(C(=O)CCCCCN4CCC(c5ccc(Oc6nn7cnnc7c7c6CCCC7)cc5)CC4)CC3)ccc2C1=O 10.6019/CHEMBL5463725
CHEMBL5465172 389523 0 None -12 6 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL 758 11 1 9 6.2 O=C1NCCCC1N1Cc2cc(C3CCN(C(=O)CCCCCN4CCC(c5ccc(Oc6nn7cnnc7c7c6CCCC7)cc5)CC4)CC3)ccc2C1=O 10.6019/CHEMBL5463725
5048 6373 55 None -724 10 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
8924 6373 55 None -724 10 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
9948102 6373 55 None -724 10 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
CHEMBL462605 6373 55 None -724 10 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
DB11642 6373 55 None -724 10 Human 6.1 pKi = 6.1 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
10225340 469251 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71531 469251 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
9937474 335021 0 None -61 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
CHEMBL4448933 335021 0 None -61 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counterDisplacement of [3H]-Scopolamine from human M4 receptor expressed in CHO cells assessed as inhibition constant measured for 120 mins by microplate beta scintillation counter
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1021/acsmedchemlett.4c00592
177372527 393613 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 319 3 0 4 3.5 c1ccc(-n2c(O[C@H]3CN4CCC3CC4)nc3ccccc32)cc1 10.1016/j.ejmech.2023.115891
CHEMBL5639994 393613 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cell membrane assessed as inhibition constant incubated for 90 mins by competitive radioligand binding assay
ChEMBL 319 3 0 4 3.5 c1ccc(-n2c(O[C@H]3CN4CCC3CC4)nc3ccccc32)cc1 10.1016/j.ejmech.2023.115891
410345 180632 2 None -1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377269 180632 2 None -1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
156014820 352220 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650998 352220 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
156014820 352220 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4650998 352220 0 None -3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
10035281 201121 0 None -1 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 201121 0 None -1 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
9937474 335021 0 None -61 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4448933 335021 0 None -61 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
10421982 470831 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 470831 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
3055 2955 32 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
313 2955 32 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
7163 2955 32 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL936 2955 32 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
DB01231 2955 32 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
171578 26574 2 None -4 5 Human 5.0 pKi = 5.0 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
CHEMBL1184962 26574 2 None -4 5 Human 5.0 pKi = 5.0 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
290 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
4022 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
5926 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL40554 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL74300 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
290 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
4022 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
5926 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL40554 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL74300 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
290 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
4022 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
5926 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL40554 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL74300 5025 4 None -1 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
162657652 354847 0 None -2 4 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
CHEMBL4758742 354847 0 None -2 4 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
1530 4450 49 None -109 24 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
3827 4450 49 None -109 24 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
7206 4450 49 None -109 24 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
CHEMBL534 4450 49 None -109 24 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
DB00920 4450 49 None -109 24 Human 6.0 pKi = 6.0 Binding
PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.6019/CHEMBL5442175
16086061 161675 0 None -99 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL213709 161675 0 None -99 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
155554262 350520 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597244 350520 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44593620 371158 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 371158 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
164614994 371706 0 None -77 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028287 371706 0 None -77 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164611279 371677 0 None -5 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164627387 371677 0 None -5 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028067 371677 0 None -5 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028995 371677 0 None -5 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
137640511 312976 0 None -36 8 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 312976 0 None -36 8 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
14925759 313920 6 None -3235 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 313920 6 None -3235 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
46227555 38051 1 None -8 4 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198062 38051 1 None -8 4 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
44439392 182581 0 None -4677 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 5 2 2 5.1 CCCSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
CHEMBL241100 182581 0 None -4677 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 5 2 2 5.1 CCCSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
118719930 234719 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354077 234719 0 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
44576913 385831 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524186 385831 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44439393 182608 0 None -2754 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
CHEMBL241279 182608 0 None -2754 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
164624458 371780 0 None -29 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 19 9 12 -0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028823 371780 0 None -29 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 19 9 12 -0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44318817 333726 0 None -5 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 333726 0 None -5 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
11808040 333092 0 None -7 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL434684 333092 0 None -7 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
156017826 351788 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4644285 351788 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
10951142 19560 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106219 19560 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
71459604 174780 0 None -1 14 Human 6.0 pKi = 6.0 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 174780 0 None -1 14 Human 6.0 pKi = 6.0 Binding
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
2229 959 17 None -2 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
295 959 17 None -2 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
CHEMBL128365 959 17 None -2 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
44448575 26191 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182650 26191 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
24865895 193604 0 None -3 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL259662 193604 0 None -3 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
11729182 19569 0 None -2 5 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106259 19569 0 None -2 5 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
2745 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 8402 34 None None None Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
11434515 536 9 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
4484 536 9 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
7449 536 9 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
CHEMBL1194325 536 9 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
DB08897 536 9 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
15376 8661 0 None -4 4 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
349 8661 0 None -4 4 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
3643 8661 0 None -4 4 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
CHEMBL1165342 8661 0 None -4 4 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
DB13374 8661 0 None -4 4 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
2824 8659 0 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
345 8659 0 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
71203 8659 0 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
CHEMBL1892145 8659 0 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
DB13793 8659 0 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
3170 37981 15 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
92112 37981 15 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
CHEMBL1318553 37981 15 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
2484 7502 30 None -1 5 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
347 7502 30 None -1 5 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
441071 7502 30 None -1 5 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
CHEMBL227934 7502 30 None -1 5 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
DB15954 7502 30 None -1 5 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
2381 1364 33 None -2 5 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 1364 33 None -2 5 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 1364 33 None -2 5 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 1364 33 None -2 5 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 1364 33 None -2 5 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
317 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
71183 8007 0 None 1 8 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
23056 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
23056 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
318 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
318 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
CHEMBL12980 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
CHEMBL12980 8033 20 None -3 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
12486 7952 0 None -1 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 1 3 -1.1 [3H][N+](C)(C)CC#CCOC1=NOCC1 24863257
167993643 7952 0 None -1 5 Human 10.1 pKd = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 1 3 -1.1 [3H][N+](C)(C)CC#CCOC1=NOCC1 24863257
348 8285 0 None -2 4 Human 4.0 pKd = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
66706 8285 0 None -2 4 Human 4.0 pKd = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
57664406 4877 44 None -1 2 Human 5.5 pKd = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
6938 4877 44 None -1 2 Human 5.5 pKd = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
CHEMBL4089376 4877 44 None -1 2 Human 5.5 pKd = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
107867 6054 42 None 6 2 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
309 6054 42 None 6 2 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
CHEMBL17045 6054 42 None 6 2 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
187 7873 0 None -3 2 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
65 7873 0 None -3 2 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
8593 7873 0 None -3 2 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
2381 1364 33 None -2 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
374 1364 33 None -2 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
7128 1364 33 None -2 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
CHEMBL1101 1364 33 None -2 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
DB00810 1364 33 None -2 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
119357 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
119357 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
119357 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
368 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
368 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
368 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
CHEMBL279453 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
CHEMBL279453 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
CHEMBL279453 7874 37 None -1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
21123938 1510 0 None 1 5 Human 3.6 pKd None 3.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
343 1510 0 None 1 5 Human 3.6 pKd None 3.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
15376 8661 0 None -4 4 Human 4.2 pKd None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
349 8661 0 None -4 4 Human 4.2 pKd None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
3643 8661 0 None -4 4 Human 4.2 pKd None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
CHEMBL1165342 8661 0 None -4 4 Human 4.2 pKd None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
DB13374 8661 0 None -4 4 Human 4.2 pKd None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
344 5614 0 None -1 5 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
44358908 5614 0 None -1 5 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
CHEMBL139677 5614 0 None -1 5 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
332 4157 0 None -1 5 Human 4.5 pKd None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
44358893 4157 0 None -1 5 Human 4.5 pKd None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
CHEMBL343796 4157 0 None -1 5 Human 4.5 pKd None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
2824 8659 0 None -1 4 Human 4.6 pKd None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
345 8659 0 None -1 4 Human 4.6 pKd None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
71203 8659 0 None -1 4 Human 4.6 pKd None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
CHEMBL1892145 8659 0 None -1 4 Human 4.6 pKd None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
DB13793 8659 0 None -1 4 Human 4.6 pKd None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
2484 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
2484 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
347 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
347 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
441071 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
441071 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
CHEMBL227934 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
CHEMBL227934 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
DB15954 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
DB15954 7502 30 None -1 5 Human 4.9 pKd None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
346 7494 0 None -3 3 Human 5.3 pKd None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
44259 7494 0 None -3 3 Human 5.3 pKd None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
CHEMBL388978 7494 0 None -3 3 Human 5.3 pKd None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
DB02010 7494 0 None -3 3 Human 5.3 pKd None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
342 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
342 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
442021 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
442021 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
CHEMBL501756 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
CHEMBL501756 1508 34 None 3 5 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
341 698 0 None -7 4 Human 5.6 pKd None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
5311001 698 0 None -7 4 Human 5.6 pKd None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
335 3751 0 None -1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
3500 3751 0 None -1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
CHEMBL157822 3751 0 None -1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
15118529 8849 0 None 2 4 Human 5.9 pKd None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
340 8849 0 None 2 4 Human 5.9 pKd None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
CHEMBL1256845 8849 0 None 2 4 Human 5.9 pKd None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
339 8846 0 None 1 4 Human 6.2 pKd None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
9803245 8846 0 None 1 4 Human 6.2 pKd None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
CHEMBL2206331 8846 0 None 1 4 Human 6.2 pKd None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
16219545 4486 0 None -1 2 Human 6.4 pKd None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 6 2 7 5.6 CCCCCCOC(=O)[C@@]1(O)C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
337 4486 0 None -1 2 Human 6.4 pKd None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 6 2 7 5.6 CCCCCCOC(=O)[C@@]1(O)C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
42519285 5242 26 None -60 5 Human 4.5 pKi < 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
8591 5242 26 None -60 5 Human 4.5 pKi < 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
CHEMBL3185781 5242 26 None -60 5 Human 4.5 pKi < 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
1757 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
23724781 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
71183 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
CHEMBL1354199 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
CHEMBL376897 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
DB00462 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
DB11315 270505 11 None -1 5 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 None
2293 6474 18 None 1 4 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
329 6474 18 None 1 4 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
4934 6474 18 None 1 4 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
CHEMBL1180725 6474 18 None 1 4 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
DB00782 6474 18 None 1 4 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
11519070 8553 4 None -2 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
4816 8553 4 None -2 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
7354 8553 4 None -2 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
CHEMBL1187833 8553 4 None -2 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
DB09076 8553 4 None -2 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
2677 346761 7 None -9 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 None
5487427 346761 7 None -9 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 None
CHEMBL4650755 346761 7 None -9 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 None
11548 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
2370 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
297 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
358 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
CHEMBL1482 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
DB01019 1286 20 None -1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
10938 3497 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
299 3497 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
3256 3497 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
CHEMBL2110739 3497 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
3294 4099 60 None -1 24 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 4099 60 None -1 24 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 4099 60 None -1 24 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 4099 60 None -1 24 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 4099 60 None -1 24 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
66265 194428 9 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
832 194428 9 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 194428 9 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
DB01191 194428 9 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
2719 1891 63 None -1 8 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 1891 63 None -1 8 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 1891 63 None -1 8 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 1891 63 None -1 8 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 1891 63 None -1 8 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
1395 99516 64 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
3652 99516 64 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 99516 64 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
DB01611 99516 64 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
1214 506896 0 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)C(F)(F)F None
3372 506896 0 None -1 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)C(F)(F)F None
15387 99098 49 None 1 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1677 99098 49 None 1 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 99098 49 None 1 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
DB09224 99098 49 None 1 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1209 3407 55 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 3407 55 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 3407 55 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 3407 55 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 3407 55 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2389 6775 83 None -15 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 6775 83 None -15 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 6775 83 None -15 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 6775 83 None -15 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 6775 83 None -15 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2551 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
298 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
488 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
5831 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
CHEMBL965 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
DB00411 1644 11 None -2 11 Rat 8.3 pKi = 8.3 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C None
187 524 25 None -3 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 524 25 None -3 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 524 25 None -3 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 524 25 None -3 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 524 25 None -3 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
109 509441 0 None None None Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 666 6 2 4 5.5 OC\C=C1\C[N@+]2(CC=C)CC[C@@]34[C@@H]2C[C@@H]1C1=CN2[C@H]5C(=CN([C@H]31)C1=CC=CC=C41)[C@H]1C[C@H]3[C@@]5(CC[N@@+]3(CC=C)C\C1=C\CO)C1=CC=CC=C21 None
2599 116531 16 None -5 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
5404 116531 16 None -5 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1714574 116531 16 None -5 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OCC3COC(Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
2448 199534 52 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
407 199534 52 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 199534 52 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
DB12401 199534 52 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
107782 38381 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
4667 38381 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
CHEMBL1201207 38381 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
DB14669 38381 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
2812 19119 69 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
719 19119 69 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 19119 69 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
DB00257 19119 69 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1726 5075 9 None -32 5 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 5075 9 None -32 5 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 5075 9 None -32 5 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 5075 9 None -32 5 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 5075 9 None -32 5 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1726 5075 9 None -12 5 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 5075 9 None -12 5 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 5075 9 None -12 5 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 5075 9 None -12 5 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 5075 9 None -12 5 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
212 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 8291 39 None -1 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
242 971 74 None -3 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 971 74 None -3 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 971 74 None -3 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 971 74 None -3 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 971 74 None -3 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2436 470362 35 None -7 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
68617 470362 35 None -7 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 470362 35 None -7 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
DB01104 470362 35 None -7 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
1613 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 4786 46 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1200 3405 44 None -12 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
12488 3405 44 None -12 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 3405 44 None -12 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 3405 44 None -12 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 3405 44 None -12 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
1016 8173 46 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 8173 46 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 8173 46 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 8173 46 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 8173 46 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
4191 38422 36 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
6918558 38422 36 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
CHEMBL1201764 38422 36 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
DB06702 38422 36 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
2536 308773 12 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 None
5354 308773 12 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 None
CHEMBL404849 308773 12 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 None
103 8980 49 None -31 31 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 8980 49 None -31 31 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 8980 49 None -31 31 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 8980 49 None -31 31 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 8980 49 None -31 31 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2495 509455 0 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 ClC1=CC=C(CS[C@@H](CN2C=CN=C2)C2=CC=C(Cl)C=C2Cl)C=C1 None
3168 23567 68 None -89 19 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
966 23567 68 None -89 19 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 23567 68 None -89 19 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
DB00450 23567 68 None -89 19 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
2337 6622 53 None -21 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 6622 53 None -21 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 6622 53 None -21 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 6622 53 None -21 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 6622 53 None -21 36 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1547484 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
2761 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 1937 56 None -9 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
176 823 54 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 823 54 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 823 54 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 823 54 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 823 54 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2106 461821 25 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
4746 461821 25 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL75880 461821 25 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
DB01074 461821 25 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
1212 3415 38 None -30 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 3415 38 None -30 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 3415 38 None -30 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 3415 38 None -30 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 3415 38 None -30 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
124 6070 37 None -54 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 6070 37 None -54 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 6070 37 None -54 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 6070 37 None -54 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 6070 37 None -54 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
1800 473856 65 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4189 473856 65 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 473856 65 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
DB01110 473856 65 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
10104 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
12963076 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
21855 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
6604866 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
903 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
CHEMBL1493369 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
CHEMBL22108 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
CHEMBL564226 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
DB08801 7246 46 None -58 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C None
1592 473362 45 None -1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
3947 473362 45 None -1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 473362 45 None -1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
DB13411 473362 45 None -1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
2200 6369 35 None -7 11 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 6369 35 None -7 11 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 6369 35 None -7 11 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 6369 35 None -7 11 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 6369 35 None -7 11 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3198 461850 54 None -8 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
983 461850 54 None -8 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 461850 54 None -8 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
DB01127 461850 54 None -8 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
135 5144 38 None -30 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 5144 38 None -30 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 5144 38 None -30 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 5144 38 None -30 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 5144 38 None -30 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1210 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
5281070 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
90475904 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1200927 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB09555 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 1893 53 None -9 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2338 461820 42 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
237 461820 42 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 461820 42 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
DB01103 461820 42 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
2247 1042 63 None -17 37 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 1042 63 None -17 37 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 1042 63 None -17 37 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 1042 63 None -17 37 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 1042 63 None -17 37 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
191 833 62 None -20 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 833 62 None -20 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 833 62 None -20 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 833 62 None -20 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 833 62 None -20 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2800 179440 13 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
700 179440 13 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 179440 13 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
DB00882 179440 13 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
1482 367203 61 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
60838 367203 61 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
CHEMBL481 367203 61 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
DB00762 367203 61 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
2090 389838 56 None -6 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
4735 389838 56 None -6 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL55 389838 56 None -6 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
DB00738 389838 56 None -6 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
2274 6448 36 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 6448 36 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 6448 36 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 6448 36 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 6448 36 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
154059 7390 37 None -5 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 7390 37 None -5 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 7390 37 None -5 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 7390 37 None -5 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 7390 37 None -5 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2995 469311 34 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
812 469311 34 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 469311 34 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 469311 34 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
3468 350117 13 None 1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
4138 350117 13 None 1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 350117 13 None 1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
DB00406 350117 13 None 1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
6726 2642 44 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 2642 44 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 2642 44 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 2642 44 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 2642 44 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3191 202914 68 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
977 202914 68 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 202914 68 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
DB11742 202914 68 None -5 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
2320 468583 19 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
4976 468583 19 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 468583 19 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
DB00344 468583 19 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
10660 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1224 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
441281 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL1200406 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB00985 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB13636 2953 69 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1427 4113 43 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 4113 43 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 4113 43 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 4113 43 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 4113 43 None -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1821 410750 60 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
4212 410750 60 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
CHEMBL58 410750 60 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
DB01204 410750 60 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
1530 4450 49 None -109 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 4450 49 None -109 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 4450 49 None -109 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 4450 49 None -109 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 4450 49 None -109 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
1971 5840 38 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 5840 38 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 5840 38 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 5840 38 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 5840 38 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
3158 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
667468 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
956 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
CHEMBL101740 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
CHEMBL1628227 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
DB01142 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
DB14750 18465 32 None -13 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccccc21 None
2200 6369 35 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 6369 35 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 6369 35 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 6369 35 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 6369 35 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3652 8876 57 None -3 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 8876 57 None -3 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 8876 57 None -3 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 8876 57 None -3 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 8876 57 None -3 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
3155 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
5284550 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
951 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL108947 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL1492500 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
DB09167 77368 13 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
1634 163834 36 None -8 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
4011 163834 36 None -8 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 163834 36 None -8 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
DB00934 163834 36 None -8 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
2284 6466 25 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 6466 25 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 6466 25 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 6466 25 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 6466 25 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2726 1895 54 None -14 48 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 1895 54 None -14 48 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 1895 54 None -14 48 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 1895 54 None -14 48 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 1895 54 None -14 48 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3055 2955 32 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
313 2955 32 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
7163 2955 32 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
CHEMBL936 2955 32 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
DB01231 2955 32 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
2335 26122 15 None 1 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
3018 26122 15 None 1 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 26122 15 None 1 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
DB11125 26122 15 None 1 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
2068 370177 47 None -26 8 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
43815 370177 47 None -26 8 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 370177 47 None -26 8 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
DB00715 370177 47 None -26 8 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
135398745 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1982 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4585 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 5933 69 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
124087 2860 75 None -10 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 2860 75 None -10 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 2860 75 None -10 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 2860 75 None -10 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 2860 75 None -10 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
1688 296777 35 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
6075 296777 35 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 296777 35 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
1712 5065 36 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 5065 36 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 5065 36 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 5065 36 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 5065 36 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1999 473057 30 None 1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
4601 473057 30 None 1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 473057 30 None 1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
DB01173 473057 30 None 1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
1379 116475 17 None 1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 None
5282593 116475 17 None 1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 None
CHEMBL1618018 116475 17 None 1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 None
DB11181 116475 17 None 1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 None
2398 1965 48 None -1 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 1965 48 None -1 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 1965 48 None -1 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 1965 48 None -1 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 1965 48 None -1 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
62865 2630 0 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 2630 0 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 2630 0 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 2630 0 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 2630 0 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
100 8289 46 None -4 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 8289 46 None -4 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 8289 46 None -4 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 8289 46 None -4 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 8289 46 None -4 34 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
321 2732 0 None -12 8 Human 8.1 pKi = 8.1 Binding
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 2732 0 None -12 8 Human 8.1 pKi = 8.1 Binding
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 2732 0 None -12 8 Human 8.1 pKi = 8.1 Binding
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 2732 0 None -12 8 Human 8.1 pKi = 8.1 Binding
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 2732 0 None -12 8 Human 8.1 pKi = 8.1 Binding
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
180 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2276 473216 16 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
4919 473216 16 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 473216 16 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
DB00387 473216 16 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
1371 3935 8 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
24199 3935 8 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
323 3935 8 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
CHEMBL1201325 3935 8 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
DB06787 3935 8 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
2800 159972 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
5648 159972 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
CHEMBL2111176 159972 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
DB13497 159972 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
2028 6066 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 6066 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 6066 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 6066 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 6066 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
2774 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
688595 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1457550 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 8415 68 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
2705 8363 46 None -1 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 8363 46 None -1 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 8363 46 None -1 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 8363 46 None -1 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 8363 46 None -1 11 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
2705 8363 46 None -1 11 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 8363 46 None -1 11 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 8363 46 None -1 11 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 8363 46 None -1 11 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 8363 46 None -1 11 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
26987 1955 32 None -38 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 1955 32 None -38 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 1955 32 None -38 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 1955 32 None -38 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 1955 32 None -38 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2263 311473 35 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
4904 311473 35 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
CHEMBL404215 311473 35 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
DB13642 311473 35 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
277 2680 45 None -8 34 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 2680 45 None -8 34 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 2680 45 None -8 34 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 2680 45 None -8 34 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 2680 45 None -8 34 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1201549 1234 18 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 1234 18 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 1234 18 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 1234 18 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 1234 18 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
2286 6468 43 None -3 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 6468 43 None -3 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 6468 43 None -3 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 6468 43 None -3 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 6468 43 None -3 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
3494 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
4302 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
7459 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
9933193 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
CHEMBL1201335 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
DB00986 3732 12 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
1475 116491 8 None -3 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657308 116491 8 None -3 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657309 116491 8 None -3 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1621597 116491 8 None -3 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
DB00332 116491 8 None -3 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
10129 6757 53 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
11753673 6757 53 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
5303 6757 53 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
CHEMBL3833319 6757 53 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
DB11855 6757 53 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
1402 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
154417 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
174174 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
260 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
320 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL1331216 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL517712 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00424 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00572 1082 53 None -1 16 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
2424 509454 0 None -1 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)[C@H](CO)C1=CC=CC=C1 None
3042 2911 27 None -1 13 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 2911 27 None -1 13 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 2911 27 None -1 13 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 2911 27 None -1 13 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 2911 27 None -1 13 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
1402 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
154417 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
174174 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
260 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
320 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL1331216 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL517712 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00424 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00572 1082 53 None -1 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
2039 6072 14 None None None Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
5749 6072 14 None None None Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
7257 6072 14 None None None Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
CHEMBL1201286 6072 14 None None None Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
DB00219 6072 14 None None None Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
1402 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
154417 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
174174 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
260 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
320 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL1331216 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
CHEMBL517712 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00424 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
DB00572 1082 53 None -1 16 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C None
10104 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
12963076 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
21855 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
6604866 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
903 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL1493369 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL22108 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL564226 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
DB08801 7246 46 None -58 6 Human 6.5 pKi = 6.5 Binding
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
10129 6757 53 None -1 5 Human 9.3 pKi = 9.3 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
11753673 6757 53 None -1 5 Human 9.3 pKi = 9.3 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
5303 6757 53 None -1 5 Human 9.3 pKi = 9.3 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
CHEMBL3833319 6757 53 None -1 5 Human 9.3 pKi = 9.3 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
DB11855 6757 53 None -1 5 Human 9.3 pKi = 9.3 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
2684 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
584 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
9658 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
CHEMBL168815 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
DB00185 1823 20 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
11434515 536 9 None 1 5 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
4484 536 9 None 1 5 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
7449 536 9 None 1 5 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
CHEMBL1194325 536 9 None 1 5 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
DB08897 536 9 None 1 5 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
2293 6474 18 None 1 4 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
329 6474 18 None 1 4 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
4934 6474 18 None 1 4 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
CHEMBL1180725 6474 18 None 1 4 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
DB00782 6474 18 None 1 4 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
11519070 8553 4 None -2 5 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
4816 8553 4 None -2 5 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
7354 8553 4 None -2 5 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
CHEMBL1187833 8553 4 None -2 5 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
DB09076 8553 4 None -2 5 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
367 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
367 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
5487427 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
5487427 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL1900528 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL1900528 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL3305968 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL3305968 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
DB01409 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
DB01409 8326 0 None 1 5 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
23056 231 0 None None None Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
3260 231 0 None None None Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
CHEMBL12980 231 0 None None None Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
11548 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
11548 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
2370 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
2370 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
297 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
297 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
358 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
358 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
CHEMBL1482 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
CHEMBL1482 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
DB01019 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
DB01019 1286 20 None -1 5 Human 4.0 pKi = 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
2551 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
2551 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
298 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
298 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
488 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
488 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
5831 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
5831 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
CHEMBL965 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
CHEMBL965 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
DB00411 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
DB00411 1644 11 None -38 11 Human 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
187 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
187 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
294 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
294 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
65 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
65 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
CHEMBL667 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
CHEMBL667 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
DB03128 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
DB03128 524 25 None -3 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
302 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
302 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
4630 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
4630 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
CHEMBL7634 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
CHEMBL7634 6062 14 None -2 7 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
2166 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
2166 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
305 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
305 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
5910 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
5910 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
91468 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
91468 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
CHEMBL550 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
CHEMBL550 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
CHEMBL91776 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
CHEMBL91776 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
DB01085 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
DB01085 6354 42 None -1148 8 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
2230 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
2230 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
2230 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
296 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
296 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
296 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
CHEMBL7303 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
CHEMBL7303 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
CHEMBL7303 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
DB04365 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
DB04365 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
DB04365 961 44 None -436 10 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
1726 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1726 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
7438 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
CHEMBL978 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
DB06709 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 5075 9 None -32 5 Rat 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
24768606 8737 49 None -79 5 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
3274 8737 49 None -79 5 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
CHEMBL1628667 8737 49 None -79 5 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
129786 3867 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
3276 3867 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
154059 7390 37 None -5 8 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2457 7390 37 None -5 8 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
7483 7390 37 None -5 8 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
CHEMBL1734 7390 37 None -5 8 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
DB01591 7390 37 None -5 8 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2774 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
5593 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
688595 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
7319 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
CHEMBL1200604 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
CHEMBL1457550 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
DB00809 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
DB01199 8415 68 None 1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
154734599 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
154734599 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
154734599 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
154734599 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
327 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
327 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
327 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
327 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
4108 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
4108 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
4108 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
4108 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
CHEMBL27673 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
CHEMBL27673 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
CHEMBL27673 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
CHEMBL27673 5087 6 None -6 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
20980871 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
5282426 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
7549 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL108947 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL1492500 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
DB09167 3021 0 None -15 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
2200 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
2200 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
2200 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
2200 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
2200 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
328 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
328 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
328 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
328 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
328 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
4848 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
4848 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
4848 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
4848 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
4848 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
CHEMBL9967 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
CHEMBL9967 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
CHEMBL9967 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
CHEMBL9967 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
CHEMBL9967 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
DB00670 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
DB00670 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
DB00670 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
DB00670 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
DB00670 6369 35 None -3 11 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
11498 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
11498 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
4995951 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
4995951 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
CHEMBL59898 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
CHEMBL59898 6149 38 None 19 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
3652 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
3652 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
3652 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
3652 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
57 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
57 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
57 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
60809 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
60809 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
60809 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
CHEMBL21536 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
CHEMBL21536 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
CHEMBL21536 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
DB15357 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
DB15357 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
DB15357 8876 57 None -3 18 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
119357 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
119357 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
3264 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
3264 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
CHEMBL279453 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
CHEMBL279453 625 0 None -3 5 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
321 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
321 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
321 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
444031 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
444031 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
444031 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
784 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
784 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
784 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
CHEMBL1346 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
CHEMBL1346 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
CHEMBL1346 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
DB00496 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
DB00496 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
DB00496 2732 0 None -12 8 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
132947 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
361 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
CHEMBL265256 8408 6 None -34 9 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
129989 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
129989 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
8584 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
8584 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
CHEMBL43383 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
CHEMBL43383 933 31 None -2 11 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
324 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
324 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
324 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
6436265 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
6436265 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
6436265 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
CHEMBL277642 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
CHEMBL277642 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
CHEMBL277642 3939 17 None 1 7 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
2200 6369 35 None -3 11 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
328 6369 35 None -3 11 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
4848 6369 35 None -3 11 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
CHEMBL9967 6369 35 None -3 11 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
DB00670 6369 35 None -3 11 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
180 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
200 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
2160 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
CHEMBL629 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
DB00321 829 44 None -2 32 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
10894911 6147 0 None None None Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
11499 6147 0 None None None Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
CHEMBL88223 6147 0 None None None Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
3042 2911 27 None -1 13 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
355 2911 27 None -1 13 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
868 2911 27 None -1 13 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
CHEMBL1123 2911 27 None -1 13 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
DB00804 2911 27 None -1 13 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
2705 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
2705 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
360 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
360 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
443879 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
443879 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
CHEMBL1382 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
CHEMBL1382 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
DB01036 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
DB01036 8363 46 None -1 11 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
129140 8544 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
129140 8544 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
8583 8544 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
8583 8544 0 None 1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
324 3939 17 None 1 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 29860464
6436265 3939 17 None 1 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 29860464
CHEMBL277642 3939 17 None 1 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 29860464
313 5488 0 None 2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29860464
P81031 5488 0 None 2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29860464
2028 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
2028 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
359 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
359 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
4634 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
4634 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
CHEMBL1231 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
CHEMBL1231 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
DB01062 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
DB01062 6066 59 None -1 10 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
313 5488 0 None 2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
313 5488 0 None 2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9862767
P81031 5488 0 None 2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
P81031 5488 0 None 2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9862767
1734 239 5 None -1 10 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
307 239 5 None -1 10 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
CHEMBL168067 239 5 None -1 10 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
1402 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
1402 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
1402 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
1402 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
154417 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
154417 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
154417 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
154417 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
174174 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
174174 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
174174 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
174174 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
260 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
260 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
260 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
260 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
320 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
320 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
320 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
320 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
CHEMBL1331216 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
CHEMBL1331216 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
CHEMBL1331216 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
CHEMBL1331216 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
CHEMBL517712 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
CHEMBL517712 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
CHEMBL517712 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
CHEMBL517712 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
DB00424 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
DB00424 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
DB00424 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
DB00424 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
DB00572 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
DB00572 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
DB00572 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
DB00572 1082 53 None -1 16 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
325 4217 10 None -2 8 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3746 4217 10 None -2 8 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
657308 4217 10 None -2 8 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
CHEMBL1615433 4217 10 None -2 8 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
DB00332 4217 10 None -2 8 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3000322 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
3000322 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
330 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
330 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
CHEMBL569713 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
CHEMBL569713 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
DB00747 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
DB00747 7238 26 None -8 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
10470 5055 7 None 4 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
1689 5055 7 None 4 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
4057 5055 7 None 4 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
CHEMBL524004 5055 7 None 4 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
DB04843 5055 7 None 4 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
8586 619 0 None -2 4 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
9862598 619 0 None -2 4 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
3494 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
4302 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
4302 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
7459 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
7459 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
9933193 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
9933193 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
CHEMBL1201335 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
CHEMBL1201335 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
DB00986 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
DB00986 3732 12 None 1 5 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
1402 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
154417 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
174174 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
260 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
320 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
CHEMBL1331216 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
CHEMBL517712 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
DB00424 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
DB00572 1082 53 None -1 16 Rat 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
2039 6072 14 None None None Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
5749 6072 14 None None None Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
7257 6072 14 None None None Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
CHEMBL1201286 6072 14 None None None Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
DB00219 6072 14 None None None Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
314 5490 0 None -1122018 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
Q8QGR0 5490 0 None -1122018 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
1150 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 473039 11 None -1 19 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
2865 8961 54 None -10 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 8961 54 None -10 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 8961 54 None -10 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 8961 54 None -10 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 8961 54 None -10 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
3220 509462 0 None -1 8 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 311 5 0 3 3.8 COC1=CC=C(OC[C@H]2CN(C)CC[C@@H]2C2=CC=CC=C2)C=C1 None
11976 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
623 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667466 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 1897 43 None -1 14 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1707 469523 59 None -1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
4066 469523 59 None -1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 469523 59 None -1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
DB01071 469523 59 None -1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
10938 3497 0 None -1 4 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
299 3497 0 None -1 4 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
3256 3497 0 None -1 4 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
CHEMBL2110739 3497 0 None -1 4 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
300 5101 11 None -3 5 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
4141 5101 11 None -3 5 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
CHEMBL92387 5101 11 None -3 5 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
303 6064 15 None -70 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
4629 6064 15 None -70 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
CHEMBL44674 6064 15 None -70 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
22991950 4744 0 None -5 6 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
326 4744 0 None -5 6 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
301 5148 16 None -3 5 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
9571002 5148 16 None -3 5 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
CHEMBL151938 5148 16 None -3 5 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
2229 959 17 None -2 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
295 959 17 None -2 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
CHEMBL128365 959 17 None -2 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
312 5486 0 None -3 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
P18328 5486 0 None -3 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
290 5025 4 None -1 7 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
4022 5025 4 None -1 7 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
5926 5025 4 None -1 7 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
CHEMBL40554 5025 4 None -1 7 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
CHEMBL74300 5025 4 None -1 7 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
107867 6054 42 None -7 10 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
309 6054 42 None -7 10 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
CHEMBL17045 6054 42 None -7 10 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
310 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
3602 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
3602 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
3603 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
3603 3933 0 None -5 9 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
124226 3931 0 None -7 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
322 3931 0 None -7 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
311 5484 0 None -2 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
P81030 5484 0 None -2 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
2200 6369 35 None -7 11 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
328 6369 35 None -7 11 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
4848 6369 35 None -7 11 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
CHEMBL9967 6369 35 None -7 11 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
DB00670 6369 35 None -7 11 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
306 7028 17 None -2 5 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
3536 7028 17 None -2 5 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
9577995 7028 17 None -2 5 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
CHEMBL134641 7028 17 None -2 5 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
308 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
308 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
3603 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
3603 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
CHEMBL1256682 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
CHEMBL1256682 4213 15 None -5 6 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
10426487 5794 8 None -3 5 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
291 5794 8 None -3 5 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
CHEMBL99521 5794 8 None -3 5 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
310 3933 0 None -1 9 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
3602 3933 0 None -1 9 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
3603 3933 0 None -1 9 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
293 5798 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
9985526 5798 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
1371 3935 8 None -1 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
24199 3935 8 None -1 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
323 3935 8 None -1 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
CHEMBL1201325 3935 8 None -1 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
DB06787 3935 8 None -1 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
130169 7328 0 None -2 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
331 7328 0 None -2 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
11757797 5796 0 None -31 5 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
292 5796 0 None -31 5 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
10062394 6203 1 None 1 4 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
304 6203 1 None 1 4 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
CHEMBL130715 6203 1 None 1 4 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
1734 239 5 None -1 10 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
307 239 5 None -1 10 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
CHEMBL168067 239 5 None -1 10 Rat 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587