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

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 Smiles

 DOI
53322111 120162 0 None 125 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 482 7 4 8 3.4 C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/ml100229v
CHEMBL1651721 120162 0 None 125 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 482 7 4 8 3.4 C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/ml100229v
53320793 120164 1 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651723 120164 1 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
11618319 161242 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 403 4 1 8 4.6 COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL211871 161242 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 403 4 1 8 4.6 COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
11509369 161468 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 390 3 2 6 4.3 CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
CHEMBL212815 161468 0 None None None Human 5.9 pEC50 = 5.9 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 390 3 2 6 4.3 CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
44440750 197637 0 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 610 13 3 7 6.2 CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL269261 197637 0 None None None Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 610 13 3 7 6.2 CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44440752 333649 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 568 13 4 7 5.1 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL439392 333649 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 568 13 4 7 5.1 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
11502667 159976 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 420 4 2 7 4.3 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F 10.1021/jm060247s
CHEMBL211129 159976 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 420 4 2 7 4.3 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F 10.1021/jm060247s
44572264 353329 28 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
CHEMBL474041 353329 28 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
44440751 194245 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 554 12 4 7 5.3 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL247700 194245 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 554 12 4 7 5.3 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
44440753 295203 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 537 12 2 5 5.5 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL393847 295203 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 537 12 2 5 5.5 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.12.062
11531195 276149 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 388 3 3 7 3.9 CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
CHEMBL378091 276149 0 None None None Human 5.7 pEC50 = 5.7 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 388 3 3 7 3.9 CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
9915237 193940 2 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL246321 193940 2 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44440784 184171 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL245663 184171 0 None None None Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 10.1016/j.bmcl.2006.12.062
53320759 120181 1 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651829 120181 1 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440746 299351 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL397316 299351 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
53323417 120175 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651823 120175 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
9887381 161015 33 None 25 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL211405 161015 33 None 25 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
9887381 161015 33 None 25 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/acs.jmedchem.4c01525
CHEMBL211405 161015 33 None 25 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/acs.jmedchem.4c01525
53324744 120184 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651831 120184 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53320758 120176 1 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651824 120176 1 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
167398412 374583 4 None -234422 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at LSHR (unknown origin) by arrestin technology based assayAgonist activity at LSHR (unknown origin) by arrestin technology based assay
ChEMBL 682 9 3 5 7.8 COc1cc(F)c(O[C@H]2CC[C@@](C)(C(=O)O)CC2)cc1C(=O)N[C@@H]1[C@H]2CC[C@H](C2)[C@@H]1C(=O)Nc1ccc(F)c(S(F)(F)(F)(F)F)c1 10.1021/acs.jmedchem.3c02183
CHEMBL5194101 374583 4 None -234422 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at LSHR (unknown origin) by arrestin technology based assayAgonist activity at LSHR (unknown origin) by arrestin technology based assay
ChEMBL 682 9 3 5 7.8 COc1cc(F)c(O[C@H]2CC[C@@](C)(C(=O)O)CC2)cc1C(=O)N[C@@H]1[C@H]2CC[C@H](C2)[C@@H]1C(=O)Nc1ccc(F)c(S(F)(F)(F)(F)F)c1 10.1021/acs.jmedchem.3c02183
2887926 122034 7 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 468 7 1 5 6.3 COc1ccc(C2Nc3ccccc3C(=O)N2Cc2ccco2)cc1COc1c(C)cccc1C 10.1021/acs.jmedchem.4c01525
CHEMBL1703522 122034 7 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 468 7 1 5 6.3 COc1ccc(C2Nc3ccccc3C(=O)N2Cc2ccco2)cc1COc1c(C)cccc1C 10.1021/acs.jmedchem.4c01525
44255904 120180 1 None 79 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 682 17 4 14 3.9 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651828 120180 1 None 79 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 682 17 4 14 3.9 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440748 194284 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 609 8 3 6 6.6 CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL247945 194284 0 None None None Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 609 8 3 6 6.6 CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 10.1016/j.bmcl.2006.12.062
53324743 120178 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651826 120178 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53318121 120174 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651822 120174 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53324742 120177 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651825 120177 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53324741 120173 1 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651821 120173 1 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440754 331961 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 496 10 2 5 6.0 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)NCCc2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL429108 331961 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 496 10 2 5 6.0 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)NCCc2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
53320760 120183 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651830 120183 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
11654606 275788 1 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 416 4 1 7 4.5 COc1cccc(-c2nc(SC)nc3sc(C(=O)N(C)C(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL377399 275788 1 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 416 4 1 7 4.5 COc1cccc(-c2nc(SC)nc3sc(C(=O)N(C)C(C)(C)C)c(N)c23)c1 10.1021/jm060247s
11539288 276029 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 432 5 2 8 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1OC 10.1021/jm060247s
CHEMBL377769 276029 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 432 5 2 8 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1OC 10.1021/jm060247s
155566723 349899 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 457 4 1 3 6.3 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4587440 349899 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 457 4 1 3 6.3 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155563159 349322 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4573509 349322 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.9b01382
155546314 347637 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 478 4 1 3 7.5 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4531781 347637 0 None None None Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 478 4 1 3 7.5 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155558589 348790 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 402 2 1 2 6.2 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1 10.1021/acs.jmedchem.9b01382
CHEMBL4560733 348790 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 402 2 1 2 6.2 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1 10.1021/acs.jmedchem.9b01382
155524816 335542 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 425 4 2 4 4.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(F)c(C(N)=O)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4456365 335542 0 None None None Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 425 4 2 4 4.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(F)c(C(N)=O)c2)cc1 10.1021/acs.jmedchem.9b01382
155516839 334668 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1ccc(F)c(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4443605 334668 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1ccc(F)c(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600336 335678 23 None -4 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4458424 335678 23 None -4 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155530584 336087 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 438 2 1 2 6.5 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(F)c(F)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4464604 336087 0 None None None Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 438 2 1 2 6.5 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(F)c(F)c1 10.1021/acs.jmedchem.9b01382
155528786 335920 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 394 4 1 4 4.9 COc1cc(NC(=O)N2CCc3sccc3[C@@H]2c2ccccc2)cc(OC)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4461980 335920 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 394 4 1 4 4.9 COc1cc(NC(=O)N2CCc3sccc3[C@@H]2c2ccccc2)cc(OC)c1 10.1021/acs.jmedchem.9b01382
155542952 347293 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 424 5 1 5 5.0 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4522381 347293 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 424 5 1 5 5.0 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
2741928 346718 2 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4593222 346718 2 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None 28 3 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None 28 3 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155555227 348405 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 419 2 2 3 4.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(=O)[nH]c1 10.1021/acs.jmedchem.9b01382
CHEMBL4551301 348405 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 419 2 2 3 4.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(=O)[nH]c1 10.1021/acs.jmedchem.9b01382
155532999 336333 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 416 2 1 2 6.5 Cc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4468163 336333 0 None None None Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 416 2 1 2 6.5 Cc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155561384 349675 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4581889 349675 0 None None None Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155555948 348561 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 458 4 1 4 5.7 O=C(Nc1ccc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4555151 348561 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 458 4 1 4 5.7 O=C(Nc1ccc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155567488 349929 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccc(F)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4588196 349929 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccc(F)c1 10.1021/acs.jmedchem.9b01382
155564366 349175 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1F 10.1021/acs.jmedchem.9b01382
CHEMBL4570127 349175 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1F 10.1021/acs.jmedchem.9b01382
155565197 349569 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 460 4 1 3 7.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4579421 349569 0 None None None Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 460 4 1 3 7.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155535600 336578 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 440 5 1 5 5.1 COc1ccc(C2c3ccsc3CCN2C(=S)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471875 336578 0 None None None Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 440 5 1 5 5.1 COc1ccc(C2c3ccsc3CCN2C(=S)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
155533073 336342 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 2 1 2 7.3 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4468307 336342 0 None None None Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 2 1 2 7.3 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01382
2741928 346718 2 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4593222 346718 2 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
29993669 336551 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471621 336551 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
29993669 336551 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471621 336551 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
139600336 335678 23 None 4 3 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4458424 335678 23 None 4 3 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155568207 350045 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 436 2 1 2 6.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4590976 350045 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 436 2 1 2 6.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
29993670 335084 0 None 1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4449797 335084 0 None 1 2 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155563505 349320 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccncc1 10.1021/acs.jmedchem.9b01382
CHEMBL4573451 349320 0 None None None Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccncc1 10.1021/acs.jmedchem.9b01382
155561534 349631 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 392 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4580951 349631 0 None None None Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 392 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.9b01382
29993670 335084 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4449797 335084 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155534855 336515 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccnc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471103 336515 0 None None None Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccnc1 10.1021/acs.jmedchem.9b01382
155527311 335792 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 3 1 3 6.6 O=C(Nc1ccc(F)c(OC(F)(F)F)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4460075 335792 0 None None None Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 3 1 3 6.6 O=C(Nc1ccc(F)c(OC(F)(F)F)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
57325683 156621 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 368 2 1 2 5.6 O=C(Nc1ccccc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL2032175 156621 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 368 2 1 2 5.6 O=C(Nc1ccccc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None -28 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None -28 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL412984 488257 0 None None None Rat 9.4 pKd = 9.4 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1451 38 17 15 -0.5 CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00130a019
44314940 163542 0 None None None Rat 9.3 pKd = 9.3 Functional
Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL216617 163542 0 None None None Rat 9.3 pKd = 9.3 Functional
Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44315218 198713 0 None None None Rat 8.7 pKd = 8.7 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275694 198713 0 None None None Rat 8.7 pKd = 8.7 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314845 317404 0 None None None Rat 8.0 pKd = 8.0 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL415109 317404 0 None None None Rat 8.0 pKd = 8.0 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314939 316878 0 None None None Rat 7.9 pKd = 7.9 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL412573 316878 0 None None None Rat 7.9 pKd = 7.9 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
14557614 180218 0 None None None Rat 7.8 pKd = 7.8 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369800 180218 0 None None None Rat 7.8 pKd = 7.8 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369798 477588 0 None None None Rat 7.8 pKd = 7.8 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1016 25 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1ccc2ccccc2c1 10.1021/jm00130a019
14557592 180214 0 None None None Rat 6.7 pKd = 6.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369791 180214 0 None None None Rat 6.7 pKd = 6.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
14557629 180221 0 None None None Rat 5.7 pKd = 5.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369809 180221 0 None None None Rat 5.7 pKd = 5.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
14557620 180222 0 None None None Rat 6.7 pKd = 6.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369810 180222 0 None None None Rat 6.7 pKd = 6.7 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
44314797 332185 0 None None None Rat 7.6 pKd = 7.6 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL429543 332185 0 None None None Rat 7.6 pKd = 7.6 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557600 180223 0 None None None Rat 6.6 pKd = 6.6 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369813 180223 0 None None None Rat 6.6 pKd = 6.6 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557594 180213 0 None None None Rat 5.6 pKd = 5.6 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369790 180213 0 None None None Rat 5.6 pKd = 5.6 Functional
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
44314843 197058 0 None None None Rat 8.5 pKd = 8.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL264298 197058 0 None None None Rat 8.5 pKd = 8.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314937 197188 0 None None None Rat 8.5 pKd = 8.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
CHEMBL265413 197188 0 None None None Rat 8.5 pKd = 8.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
44314846 198555 0 None None None Rat 8.4 pKd = 8.4 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL274609 198555 0 None None None Rat 8.4 pKd = 8.4 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314897 316142 0 None None None Rat 7.5 pKd = 7.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL411175 316142 0 None None None Rat 7.5 pKd = 7.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369793 477587 0 None None None Rat 6.5 pKd = 6.5 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1008 26 11 11 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1ccc(OC)cc1 10.1021/jm00130a019
14557590 180220 0 None None None Rat 6.4 pKd = 6.4 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369808 180220 0 None None None Rat 6.4 pKd = 6.4 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44315053 198717 0 None None None Rat 8.2 pKd = 8.2 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275709 198717 0 None None None Rat 8.2 pKd = 8.2 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369807 477589 0 None None None Rat 8.2 pKd = 8.2 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1016 25 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369787 477585 0 None None None Rat 7.2 pKd = 7.2 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1008 26 11 11 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C\c1ccc(OC)cc1 10.1021/jm00130a019
44314898 279047 0 None None None Rat 7.1 pKd = 7.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL386525 279047 0 None None None Rat 7.1 pKd = 7.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44315220 317280 0 None None None Rat 8.1 pKd = 8.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL413887 317280 0 None None None Rat 8.1 pKd = 8.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557616 180216 0 None None None Rat 6.1 pKd = 6.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369799 180216 0 None None None Rat 6.1 pKd = 6.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557588 180219 0 None None None Rat 6.1 pKd = 6.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369806 180219 0 None None None Rat 6.1 pKd = 6.1 Functional
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
1159 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
1159 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
CHEMBL1201419 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
CHEMBL1201419 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
DB00044 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
DB00044 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
P01215 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
P01215 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
P01229 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
P01229 4722 0 None None None Human 10.4 pIC50 = 10.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095


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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
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 Reference
ligand		 Fold
selectivity		 # Tested
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 p-value
(-log)		 Activity
Type		 Activity
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Type		 Assay
Description		 Source

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weight		 Rot
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 DOI
9887381 161015 33 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1039/c1md00145k
CHEMBL211405 161015 33 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1039/c1md00145k
139600337 347870 19 None None None Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600336 335678 23 None None None Human 6.7 pIC50 = 6.7 Binding
Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL5210121
CHEMBL4458424 335678 23 None None None Human 6.7 pIC50 = 6.7 Binding
Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL5210121
139600336 335678 23 None None None Human 6.7 pIC50 = 6.7 Binding
Cell-based assay (LH Antagonism)Cell-based assay (LH Antagonism)
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL4507317
CHEMBL4458424 335678 23 None None None Human 6.7 pIC50 = 6.7 Binding
Cell-based assay (LH Antagonism)Cell-based assay (LH Antagonism)
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL4507317
139600337 347870 19 None None None Human 6.7 pIC50 = 6.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 6.7 pIC50 = 6.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
44572264 353329 28 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
CHEMBL474041 353329 28 None None None Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
139600337 347870 19 None None None Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 347870 19 None None None Human 7.0 pIC50 = 7.0 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 347870 19 None None None Human 7.0 pIC50 = 7.0 Binding
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
44267887 198747 0 None None None Rat 9.9 pKd = 9.9 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 198747 0 None None None Rat 9.9 pKd = 9.9 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267907 40220 0 None None None Rat 9.3 pKd = 9.3 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 40220 0 None None None Rat 9.3 pKd = 9.3 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
9854500 202358 0 None -1 2 Rat 8.8 pKd = 8.8 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 202358 0 None -1 2 Rat 8.8 pKd = 8.8 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267812 198398 0 None None None Rat 8.8 pKd = 8.8 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 198398 0 None None None Rat 8.8 pKd = 8.8 Binding
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL412984 488257 0 None None None Rat 10.7 pKi = 10.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1451 38 17 15 -0.5 CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00130a019
44350635 313121 0 None None None Rat 10.6 pKi = 10.6 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1292 32 15 13 0.5 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL407606 313121 0 None None None Rat 10.6 pKi = 10.6 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1292 32 15 13 0.5 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL407123 487942 0 None None None Rat 10.4 pKi = 10.4 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1337 33 15 15 -0.7 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)O 10.1021/jm00099a017
44350493 311683 0 None None None Rat 10.1 pKi = 10.1 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1296 32 15 14 -0.4 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL405737 311683 0 None None None Rat 10.1 pKi = 10.1 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1296 32 15 14 -0.4 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350501 278809 0 None None None Rat 10.0 pKi = 10.0 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1220 32 14 14 -0.8 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL385042 278809 0 None None None Rat 10.0 pKi = 10.0 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1220 32 14 14 -0.8 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350636 317451 0 None None None Rat 9.8 pKi = 9.8 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1200 33 14 15 -1.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL415571 317451 0 None None None Rat 9.8 pKi = 9.8 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1200 33 14 15 -1.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
1175 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
1559 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
44350565 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
657181 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
CHEMBL1201199 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
CHEMBL385468 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
DB00007 4680 30 None 8 2 Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)CC(C)C)CC(C)C)CCCN=C(N)N 10.1021/jm00099a017
44350487 332031 0 None None None Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1306 32 14 13 0.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL429240 332031 0 None None None Rat 9.7 pKi = 9.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1306 32 14 13 0.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44314940 163542 0 None None None Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL216617 163542 0 None None None Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
9915237 193940 2 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [125I]hCG from LH receptorDisplacement of [125I]hCG from LH receptor
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL246321 193940 2 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [125I]hCG from LH receptorDisplacement of [125I]hCG from LH receptor
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44350502 333474 0 None None None Rat 9.4 pKi = 9.4 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1298 33 14 14 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
CHEMBL437798 333474 0 None None None Rat 9.4 pKi = 9.4 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1298 33 14 14 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
44314937 197188 0 None None None Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
CHEMBL265413 197188 0 None None None Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
44315218 198713 0 None None None Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275694 198713 0 None None None Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314843 197058 0 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL264298 197058 0 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
2958 484159 19 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
638793 484159 19 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
CHEMBL1007 484159 19 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
DB00644 484159 19 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
44315220 317280 0 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL413887 317280 0 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369787 477585 0 None None None Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1008 26 11 11 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C\c1ccc(OC)cc1 10.1021/jm00130a019
44350492 197276 0 None None None Rat 8.9 pKi = 8.9 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1223 32 14 14 -1.1 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL266205 197276 0 None None None Rat 8.9 pKi = 8.9 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1223 32 14 14 -1.1 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44314797 332185 0 None None None Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL429543 332185 0 None None None Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44314939 316878 0 None None None Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL412573 316878 0 None None None Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
14557596 180206 0 None None None Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 960 27 11 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369780 180206 0 None None None Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 960 27 11 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557594 180213 0 None None None Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369790 180213 0 None None None Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
14557629 180221 0 None None None Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369809 180221 0 None None None Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369793 477587 0 None None None Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1008 26 11 11 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1ccc(OC)cc1 10.1021/jm00130a019
14557588 180219 0 None None None Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369806 180219 0 None None None Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557627 180208 0 None None None Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 908 26 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccnc1 10.1021/jm00130a019
CHEMBL2369783 180208 0 None None None Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 908 26 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccnc1 10.1021/jm00130a019
44314897 316142 0 None None None Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL411175 316142 0 None None None Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557582 180209 0 None None None Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 946 26 11 10 0.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369784 180209 0 None None None Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 946 26 11 10 0.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44350488 163848 0 None None None Rat 8.7 pKi = 8.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1219 32 14 13 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL217405 163848 0 None None None Rat 8.7 pKi = 8.7 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1219 32 14 13 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL2369807 477589 0 None None None Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1016 25 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
10418860 198564 0 None None None Rat 8.6 pKi = 8.6 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1211 33 14 14 -1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
CHEMBL274682 198564 0 None None None Rat 8.6 pKi = 8.6 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1211 33 14 14 -1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
44315053 198717 0 None None None Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275709 198717 0 None None None Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557592 180214 0 None None None Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369791 180214 0 None None None Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
44314857 317331 0 None None None Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1047 29 9 10 3.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL414382 317331 0 None None None Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1047 29 9 10 3.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557600 180223 0 None None None Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369813 180223 0 None None None Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314845 317404 0 None None None Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL415109 317404 0 None None None Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369798 477588 0 None None None Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1016 25 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1ccc2ccccc2c1 10.1021/jm00130a019
14557616 180216 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369799 180216 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314846 198555 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL274609 198555 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369788 477586 0 None None None Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1019 26 12 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369814 477590 0 None None None Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1034 26 13 11 0.4 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
14557590 180220 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369808 180220 0 None None None Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557620 180222 0 None None None Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369810 180222 0 None None None Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
44314898 279047 0 None None None Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL386525 279047 0 None None None Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557608 180211 0 None None None Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 943 25 10 10 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369789 180211 0 None None None Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 943 25 10 10 1.0 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557606 180207 0 None None None Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 929 24 10 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369781 180207 0 None None None Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 929 24 10 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)c1cccc2ccccc12 10.1021/jm00130a019
14557576 180215 0 None None None Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 961 26 12 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369794 180215 0 None None None Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 961 26 12 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
44350486 317306 0 None None None Rat 8.0 pKi = 8.0 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1204 32 14 14 -1.3 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL414071 317306 0 None None None Rat 8.0 pKi = 8.0 Binding
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1204 32 14 14 -1.3 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
14557614 180218 0 None None None Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369800 180218 0 None None None Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
3860 1534 0 None -77 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 1239 32 15 15 -1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)COC(C)(C)C)CC(C)C)CCCN=C(N)N None
436 1534 0 None -77 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 1239 32 15 15 -1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)COC(C)(C)C)CC(C)C)CCCN=C(N)N None
50225 1534 0 None -77 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 1239 32 15 15 -1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)COC(C)(C)C)CC(C)C)CCCN=C(N)N None
CHEMBL2110824 1534 0 None -77 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 1239 32 15 15 -1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)COC(C)(C)C)CC(C)C)CCCN=C(N)N None
DB06719 1534 0 None -77 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 1239 32 15 15 -1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)CO)COC(C)(C)C)CC(C)C)CCCN=C(N)N None
1160 3919 0 None None None Human 10.9 pKd = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
1160 3919 0 None None None Human 10.9 pKd = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
2958 484159 19 None None None Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
638793 484159 19 None None None Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 484159 19 None None None Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
DB00644 484159 19 None None None Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1182 31 17 15 -4.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None