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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(-log)		 Activity
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 DOI
12607 8248 37 None 1 4 Human 10.4 pEC50 = 10.4 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
16033 8248 37 None 1 4 Human 10.4 pEC50 = 10.4 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
CHEMBL3559801 8248 37 None 1 4 Human 10.4 pEC50 = 10.4 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
14061 8781 12 None -2 6 Human 10.3 pEC50 = 10.3 Functional
Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )
ChEMBL 369 5 1 5 1.9 CC1=CC=CC=C1OCC(=O)NC2=CC(=CN(C2=O)C)C(=O)N3CCCC3 10.1021/acs.jmedchem.3c00383
45498171 8781 12 None -2 6 Human 10.3 pEC50 = 10.3 Functional
Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )
ChEMBL 369 5 1 5 1.9 CC1=CC=CC=C1OCC(=O)NC2=CC(=CN(C2=O)C)C(=O)N3CCCC3 10.1021/acs.jmedchem.3c00383
CHEMBL5420881 8781 12 None -2 6 Human 10.3 pEC50 = 10.3 Functional
Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM )
ChEMBL 369 5 1 5 1.9 CC1=CC=CC=C1OCC(=O)NC2=CC(=CN(C2=O)C)C(=O)N3CCCC3 10.1021/acs.jmedchem.3c00383
CHEMBL4281479 478156 6 None 5 6 Human 10.0 pEC50 = 10 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4308 134 63 59 -15.8 CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279973 478145 0 None 2 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4284905 478177 0 None 10 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4270 132 63 60 -17.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 478186 0 None -1 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4239 132 59 58 -16.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4279973 478145 0 None 2 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4284905 478177 0 None 10 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4270 132 63 60 -17.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 478186 0 None -1 4 Human 9.7 pEC50 = 9.7 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4239 132 59 58 -16.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
3260593 235929 6 None -1 2 Human 5.0 pEC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 434 2 0 4 6.1 Clc1ccc(-n2c(-c3cccc(Br)c3)nc3nc4ccccc4nc32)cc1 nan
CHEMBL3392057 235929 6 None -1 2 Human 5.0 pEC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 434 2 0 4 6.1 Clc1ccc(-n2c(-c3cccc(Br)c3)nc3nc4ccccc4nc32)cc1 nan
135469963 218683 4 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 443 6 1 6 4.1 O=C(/C(=N/Nc1cccc([N+](=O)[O-])c1)C(=O)C(F)(F)F)c1ccc(Br)cc1 nan
CHEMBL3213459 218683 4 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 443 6 1 6 4.1 O=C(/C(=N/Nc1cccc([N+](=O)[O-])c1)C(=O)C(F)(F)F)c1ccc(Br)cc1 nan
1192552 45946 10 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1 nan
CHEMBL1322039 45946 10 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1 nan
2803877 44883 2 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1 nan
CHEMBL1311742 44883 2 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1 nan
693933 100991 9 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 327 3 1 3 3.9 Nc1cc(-c2ccc(Br)cc2)nn1Cc1ccccc1 nan
CHEMBL1547757 100991 9 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 327 3 1 3 3.9 Nc1cc(-c2ccc(Br)cc2)nn1Cc1ccccc1 nan
2809885 99859 2 None None None Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 317 6 2 3 2.8 OC(CNC1Cc2ccccc2C1)COc1ccc(Cl)cc1 nan
CHEMBL1538224 99859 2 None None None Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 317 6 2 3 2.8 OC(CNC1Cc2ccccc2C1)COc1ccc(Cl)cc1 nan
3235884 104583 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 466 8 3 9 1.7 CCSc1nnc(NC(=O)CCNS(=O)(=O)c2cc(Br)cnc2N)s1 nan
CHEMBL1581332 104583 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 466 8 3 9 1.7 CCSc1nnc(NC(=O)CCNS(=O)(=O)c2cc(Br)cnc2N)s1 nan
9665691 218674 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 273 2 1 4 3.5 Fc1ccc2c(c1)/C(=N/Nc1ccccn1)CCS2 nan
CHEMBL3213319 218674 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 273 2 1 4 3.5 Fc1ccc2c(c1)/C(=N/Nc1ccccn1)CCS2 nan
56209 43344 22 None 2 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 296 6 1 3 3.5 CCN(CC)CC(O)Cn1c2ccccc2c2ccccc21 nan
CHEMBL1299267 43344 22 None 2 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 296 6 1 3 3.5 CCN(CC)CC(O)Cn1c2ccccc2c2ccccc21 nan
CHEMBL4294277 478221 0 None -12 3 Human 6.9 pEC50 = 6.9 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
1799038 83903 10 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 355 4 2 3 4.9 CC(=O)C(=Nc1ccc(Cl)cc1Cl)NNc1cccc(Cl)c1 nan
CHEMBL1482637 83903 10 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 355 4 2 3 4.9 CC(=O)C(=Nc1ccc(Cl)cc1Cl)NNc1cccc(Cl)c1 nan
3431315 106845 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 551 7 2 5 4.7 O=C(Nc1cc(S(=O)(=O)N2CCCCC2)ccc1Cl)c1ccccc1NS(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1602800 106845 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 551 7 2 5 4.7 O=C(Nc1cc(S(=O)(=O)N2CCCCC2)ccc1Cl)c1ccccc1NS(=O)(=O)c1ccc(F)cc1 nan
CHEMBL4294277 478221 0 None -12 3 Human 6.9 pEC50 = 6.9 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
1192552 45946 10 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1 nan
CHEMBL1322039 45946 10 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1 nan
3244114 46730 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 431 8 2 5 3.6 CCN(CC)S(=O)(=O)c1ccc2ncc(C(=O)NCCC3=CCCCC3)c(O)c2c1 nan
CHEMBL1329027 46730 2 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 431 8 2 5 3.6 CCN(CC)S(=O)(=O)c1ccc2ncc(C(=O)NCCC3=CCCCC3)c(O)c2c1 nan
CHEMBL3099724 486468 0 None -131 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4005 127 61 56 -17.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
136217230 97813 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 442 6 1 9 3.7 COc1ccc(Nc2oc(/C=C3/SC(=S)N(CC4CCCO4)C3=O)nc2C#N)cc1 nan
CHEMBL1519588 97813 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 442 6 1 9 3.7 COc1ccc(Nc2oc(/C=C3/SC(=S)N(CC4CCCO4)C3=O)nc2C#N)cc1 nan
CHEMBL2371911 477717 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesisAgonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesis
ChEMBL 1723 55 26 20 -3.8 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
CHEMBL3099723 477867 0 None -2 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4006 127 60 57 -17.4 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
44667100 385934 8 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 281 4 1 3 3.8 CN(C)Cc1c(O)ccc2oc(Cc3ccccc3)cc12 nan
657581 385934 8 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 281 4 1 3 3.8 CN(C)Cc1c(O)ccc2oc(Cc3ccccc3)cc12 nan
CHEMBL526034 385934 8 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 281 4 1 3 3.8 CN(C)Cc1c(O)ccc2oc(Cc3ccccc3)cc12 nan
2191297 86573 7 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 408 7 0 8 3.3 C=CCN1C(=O)/C(=C/c2ccc(OC(C)=O)c(OCC)c2[N+](=O)[O-])SC1=S nan
CHEMBL1505552 86573 7 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 408 7 0 8 3.3 C=CCN1C(=O)/C(=C/c2ccc(OC(C)=O)c(OCC)c2[N+](=O)[O-])SC1=S nan
CHEMBL4278700 478140 0 None -79 4 Human 7.8 pEC50 = 7.8 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4211 131 60 58 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 478215 0 None -15 4 Human 7.8 pEC50 = 7.8 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4048 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
682797 103101 17 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 316 3 2 4 4.2 Oc1ccccc1Cn1c(-c2ccccc2O)nc2ccccc21 nan
CHEMBL1567983 103101 17 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 316 3 2 4 4.2 Oc1ccccc1Cn1c(-c2ccccc2O)nc2ccccc21 nan
3911588 104785 4 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 418 6 2 3 4.5 O=C(Cc1ccc(Cl)cc1)Nc1cccc(S(=O)(=O)Nc2ccccc2F)c1 nan
CHEMBL1583097 104785 4 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 418 6 2 3 4.5 O=C(Cc1ccc(Cl)cc1)Nc1cccc(S(=O)(=O)Nc2ccccc2F)c1 nan
CHEMBL4278700 478140 0 None -79 4 Human 7.8 pEC50 = 7.8 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4211 131 60 58 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 478215 0 None -15 4 Human 7.8 pEC50 = 7.8 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4048 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3099724 486468 0 None -131 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4005 127 61 56 -17.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
9700449 222133 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 10 2 5 4.4 CCCOc1ccc(/C=N/Nc2ccc(C(=O)O)cc2)c(OCCC)c1 nan
CHEMBL3303291 222133 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 10 2 5 4.4 CCCOc1ccc(/C=N/Nc2ccc(C(=O)O)cc2)c(OCCC)c1 nan
2167979 78306 8 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 369 3 2 2 4.2 O=C(CC(O)(C(F)(F)F)C(F)(F)F)Nc1ccc(Cl)c(Cl)c1 nan
CHEMBL1431189 78306 8 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 369 3 2 2 4.2 O=C(CC(O)(C(F)(F)F)C(F)(F)F)Nc1ccc(Cl)c(Cl)c1 nan
3093479 44575 8 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 510 6 3 5 4.9 COc1ccc(N=C(S)NC(NC(=O)c2cccc(Cl)c2)C(Cl)(Cl)Cl)c([N+](=O)[O-])c1 nan
CHEMBL1309183 44575 8 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 510 6 3 5 4.9 COc1ccc(N=C(S)NC(NC(=O)c2cccc(Cl)c2)C(Cl)(Cl)Cl)c([N+](=O)[O-])c1 nan
67275 100660 46 None -1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 311 2 2 2 4.8 Cc1ccc(Cl)cc1NC(=O)c1cc2ccccc2cc1O nan
CHEMBL1544847 100660 46 None -1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 311 2 2 2 4.8 Cc1ccc(Cl)cc1NC(=O)c1cc2ccccc2cc1O nan
2090677 62449 2 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 337 3 2 3 4.5 O=C(Nc1sc2c(c1-c1nc3ccccc3[nH]1)CCCC2)C1CC1 nan
CHEMBL1378687 62449 2 None None None Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 337 3 2 3 4.5 O=C(Nc1sc2c(c1-c1nc3ccccc3[nH]1)CCCC2)C1CC1 nan
3641052 102218 1 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 375 4 0 8 3.1 CCn1nc([N+](=O)[O-])c(C(C#N)c2nc3ccccc3s2)c(Cl)c1=O nan
CHEMBL1560379 102218 1 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 375 4 0 8 3.1 CCn1nc([N+](=O)[O-])c(C(C#N)c2nc3ccccc3s2)c(Cl)c1=O nan
984148 100267 2 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 6 3 6 3.9 CCCc1cc(-c2[nH]ncc2-c2ccc(C(=O)OCC)o2)c(O)cc1O nan
CHEMBL1541596 100267 2 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 6 3 6 3.9 CCCc1cc(-c2[nH]ncc2-c2ccc(C(=O)OCC)o2)c(O)cc1O nan
1326639 78374 8 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 373 4 1 4 3.7 O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1 nan
CHEMBL1431891 78374 8 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 373 4 1 4 3.7 O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1 nan
1479154 99775 10 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 359 5 1 5 3.1 COc1ccc(Cn2cnc3c(NS(C)(=O)=O)c(C)c(C)cc32)cc1 nan
CHEMBL1537587 99775 10 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 359 5 1 5 3.1 COc1ccc(Cn2cnc3c(NS(C)(=O)=O)c(C)c(C)cc32)cc1 nan
16200926 484354 10 None -144 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c00740
CHEMBL439904 484354 10 None -144 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c00740
2985425 118669 9 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 263 5 1 3 2.5 Cc1ccccc1OCC(O)CN1CCC(C)CC1 nan
CHEMBL1623239 118669 9 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 263 5 1 3 2.5 Cc1ccccc1OCC(O)CN1CCC(C)CC1 nan
4539353 58545 8 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 442 4 1 5 3.6 O=C(O)C1CC=CCC1C(=O)N1CCN(c2nc(-c3ccccc3)c3ccccc3n2)CC1 nan
660299 58545 8 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 442 4 1 5 3.6 O=C(O)C1CC=CCC1C(=O)N1CCN(c2nc(-c3ccccc3)c3ccccc3n2)CC1 nan
CHEMBL1345141 58545 8 None None None Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 442 4 1 5 3.6 O=C(O)C1CC=CCC1C(=O)N1CCN(c2nc(-c3ccccc3)c3ccccc3n2)CC1 nan
1636339 97623 13 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 452 2 0 7 6.2 Cc1cc2c(cc1C)N(C(=O)CSC1=NCCS1)C(C)(C)c1ssc(=S)c1-2 nan
CHEMBL1517881 97623 13 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 452 2 0 7 6.2 Cc1cc2c(cc1C)N(C(=O)CSC1=NCCS1)C(C)(C)c1ssc(=S)c1-2 nan
CHEMBL3099721 477865 0 None -741 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4006 127 60 57 -17.4 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL2371908 477714 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesisAgonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesis
ChEMBL 1707 55 26 22 -3.7 CC(C)C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)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)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050907d
2315927 117998 0 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 427 5 0 1 7.0 CN(C)c1ccc(-[n+]2c(-c3ccccc3)cc(-c3ccccc3)cc2-c2ccccc2)cc1 nan
CHEMBL1617313 117998 0 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 427 5 0 1 7.0 CN(C)c1ccc(-[n+]2c(-c3ccccc3)cc(-c3ccccc3)cc2-c2ccccc2)cc1 nan
2816767 43753 3 None 1 2 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 3 2 6 5.1 Nc1sc(-c2ccccc2)cc1-c1nnc(S)n1C1CCCCC1 nan
CHEMBL1302519 43753 3 None 1 2 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 356 3 2 6 5.1 Nc1sc(-c2ccccc2)cc1-c1nnc(S)n1C1CCCCC1 nan
2945839 64123 11 None -1 2 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 487 8 2 8 3.5 COC(=O)c1ccc(NC(=O)CSc2nnc(C(C)NC(=O)c3ccccc3Cl)n2C)cc1 nan
CHEMBL1392858 64123 11 None -1 2 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 487 8 2 8 3.5 COC(=O)c1ccc(NC(=O)CSc2nnc(C(C)NC(=O)c3ccccc3Cl)n2C)cc1 nan
12004459 66940 1 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 407 6 2 6 3.4 O=C1C2CC=CCC2C(=O)N1c1ccc(NCCc2ccc(O)cc2)c([N+](=O)[O-])c1 nan
CHEMBL1418821 66940 1 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 407 6 2 6 3.4 O=C1C2CC=CCC2C(=O)N1c1ccc(NCCc2ccc(O)cc2)c([N+](=O)[O-])c1 nan
1929802 82163 9 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 414 5 4 3 5.1 CCOc1ccc(NC(S)=NN=C(S)Nc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL1465891 82163 9 None None None Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 414 5 4 3 5.1 CCOc1ccc(NC(S)=NN=C(S)Nc2cccc(C(F)(F)F)c2)cc1 nan
660707 79939 9 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 251 2 1 2 4.1 CC(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 nan
CHEMBL1447448 79939 9 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 251 2 1 2 4.1 CC(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 nan
653127 117943 8 None 1 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 275 1 1 3 3.8 Cc1cccc(N2CCc3c2nc2ccccc2c3N)c1 nan
CHEMBL1616892 117943 8 None 1 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 275 1 1 3 3.8 Cc1cccc(N2CCc3c2nc2ccccc2c3N)c1 nan
CHEMBL4277676 478132 0 None -63 3 Human 6.5 pEC50 = 6.5 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 478149 0 None -39 4 Human 6.5 pEC50 = 6.5 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277676 478132 0 None -63 3 Human 6.5 pEC50 = 6.5 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 478149 0 None -39 4 Human 6.5 pEC50 = 6.5 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
5883623 144879 1 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 288 4 2 5 2.2 N#C/C(=N/Nc1ccc(OC(F)(F)F)cc1)C(N)=S nan
CHEMBL1995800 144879 1 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 288 4 2 5 2.2 N#C/C(=N/Nc1ccc(OC(F)(F)F)cc1)C(N)=S nan
3148028 47629 17 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 313 5 1 6 2.7 O=C(COc1ccc(Cl)cc1)Nc1ncc([N+](=O)[O-])s1 nan
CHEMBL1336098 47629 17 None None None Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 313 5 1 6 2.7 O=C(COc1ccc(Cl)cc1)Nc1ncc([N+](=O)[O-])s1 nan
16192803 101159 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl nan
CHEMBL1549309 101159 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl nan
1786 5120 49 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 5120 49 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 5120 49 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 5120 49 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 5120 49 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
570353 86480 3 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 464 5 2 6 4.9 O=C(NC(Nc1nc2ccc([N+](=O)[O-])cc2s1)(C(F)(F)F)C(F)(F)F)c1ccccc1 nan
CHEMBL1504701 86480 3 None -1 2 Human 4.5 pEC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 464 5 2 6 4.9 O=C(NC(Nc1nc2ccc([N+](=O)[O-])cc2s1)(C(F)(F)F)C(F)(F)F)c1ccccc1 nan
CHEMBL3099722 477866 0 None -173 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4006 127 60 57 -17.4 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)O[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
16200926 484354 10 None -144 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Y1R expressed in HEK293 cells by FLIPR assayAgonist activity at human Y1R expressed in HEK293 cells by FLIPR assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.ejmech.2022.115036
CHEMBL439904 484354 10 None -144 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human Y1R expressed in HEK293 cells by FLIPR assayAgonist activity at human Y1R expressed in HEK293 cells by FLIPR assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.ejmech.2022.115036
16200926 484354 10 None -144 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL439904 484354 10 None -144 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
2836861 66060 5 None 2 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1 nan
CHEMBL1411397 66060 5 None 2 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1 nan
16192803 101159 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl nan
CHEMBL1549309 101159 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
ChEMBL 413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl nan
2803877 44883 2 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1 nan
CHEMBL1311742 44883 2 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1 nan
7066599 97779 7 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 293 3 1 4 4.5 Fc1ccc(Nc2c(-c3ccco3)nc3ccccn23)cc1 nan
CHEMBL1519263 97779 7 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 293 3 1 4 4.5 Fc1ccc(Nc2c(-c3ccco3)nc3ccccn23)cc1 nan
1078087 61786 30 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 220 2 2 3 2.1 Cc1c(C(=O)O)[nH]c2ccc([N+](=O)[O-])cc12 nan
CHEMBL1373205 61786 30 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 220 2 2 3 2.1 Cc1c(C(=O)O)[nH]c2ccc([N+](=O)[O-])cc12 nan
2836861 66060 5 None 2 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1 nan
CHEMBL1411397 66060 5 None 2 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1 nan
1206899 103741 10 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 174 1 2 5 1.0 N#Cc1c(Cl)nsc1NN nan
CHEMBL1573719 103741 10 None 1 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 174 1 2 5 1.0 N#Cc1c(Cl)nsc1NN nan
2185441 43680 9 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 443 6 2 7 5.2 CCn1c(SCC(=O)Nc2ccc3c(c2)oc2ccccc23)nnc1-c1ccc(N)cc1 nan
CHEMBL1301994 43680 9 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 443 6 2 7 5.2 CCn1c(SCC(=O)Nc2ccc3c(c2)oc2ccccc23)nnc1-c1ccc(N)cc1 nan
2405497 62042 3 None -1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 431 5 2 5 5.9 Nc1c(-c2ccccc2)c(CSc2nc3ccccc3[nH]2)nn1-c1ccc(Cl)cc1 nan
CHEMBL1374954 62042 3 None -1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 431 5 2 5 5.9 Nc1c(-c2ccccc2)c(CSc2nc3ccccc3[nH]2)nn1-c1ccc(Cl)cc1 nan
3562031 103610 11 None -1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 445 4 2 3 4.1 O=C(Nc1ccc(Cl)cc1Cl)NC1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
CHEMBL1572588 103610 11 None -1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 445 4 2 3 4.1 O=C(Nc1ccc(Cl)cc1Cl)NC1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
CHEMBL4277590 478130 0 None -50 3 Human 7.1 pEC50 = 7.1 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4050 129 60 55 -15.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277590 478130 0 None -50 3 Human 7.1 pEC50 = 7.1 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4050 129 60 55 -15.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279794 478144 0 None -794 4 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4121 129 62 56 -15.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279794 478144 0 None -794 4 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL 4121 129 62 56 -15.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
4055293 117938 5 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 392 2 0 2 6.1 Cc1sc2cc3c(c(C(=O)c4ccccc4)[n+]2c1C)-c1cccc2cccc-3c12 nan
CHEMBL1616832 117938 5 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 392 2 0 2 6.1 Cc1sc2cc3c(c(C(=O)c4ccccc4)[n+]2c1C)-c1cccc2cccc-3c12 nan
3237370 101078 4 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 366 8 1 4 3.3 C=CCc1ccccc1OCC(O)CN1CCN(c2ccc(C)cc2)CC1 nan
CHEMBL1548605 101078 4 None 1 2 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 366 8 1 4 3.3 C=CCc1ccccc1OCC(O)CN1CCN(c2ccc(C)cc2)CC1 nan
5710119 217627 11 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 283 4 1 4 3.5 N#C/C(=N\Nc1ccc(Cl)cc1)C(=O)c1ccccc1 nan
CHEMBL3194195 217627 11 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 283 4 1 4 3.5 N#C/C(=N\Nc1ccc(Cl)cc1)C(=O)c1ccccc1 nan
2919986 118124 5 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 387 8 1 7 2.2 COc1ccc(N2CCN(CC(O)COc3ccccc3[N+](=O)[O-])CC2)cc1 nan
CHEMBL1618362 118124 5 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 387 8 1 7 2.2 COc1ccc(N2CCN(CC(O)COc3ccccc3[N+](=O)[O-])CC2)cc1 nan
1786 5120 49 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 5120 49 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 5120 49 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 5120 49 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 5120 49 None -1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
708088 45032 9 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 328 4 1 5 3.6 Cn1cc([N+](=O)[O-])c(C(=O)Nc2ccc(C3CCCCC3)cc2)n1 nan
CHEMBL1312767 45032 9 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
ChEMBL 328 4 1 5 3.6 Cn1cc([N+](=O)[O-])c(C(=O)Nc2ccc(C3CCCCC3)cc2)n1 nan
1364 371049 49 None None None Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
3598 371049 49 None None None Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 371049 49 None None None Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
DB00756 371049 49 None None None Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
3117655 82798 3 None 1 2 Human 5.0 pEC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 322 4 1 5 3.3 CC1=NC(=O)C(N=Nc2ccccc2C(=O)O)N1c1ccccc1 nan
CHEMBL1471202 82798 3 None 1 2 Human 5.0 pEC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
ChEMBL 322 4 1 5 3.3 CC1=NC(=O)C(N=Nc2ccccc2C(=O)O)N1c1ccccc1 nan
162647593 366972 0 None None None Human 10.3 pIC50 = 10.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802520 366972 0 None None None Human 10.3 pIC50 = 10.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162667448 367070 0 None None None Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803593 367070 0 None None None Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162655600 367010 0 None None None Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802951 367010 0 None None None Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162673313 367104 0 None None None Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803933 367104 0 None None None Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162675643 367117 0 None None None Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4804067 367117 0 None None None Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162645700 366963 0 None None None Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802419 366963 0 None None None Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162652126 366989 0 None None None Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802763 366989 0 None None None Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162653845 367001 0 None None None Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802860 367001 0 None None None Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162649085 366976 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802600 366976 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162659745 367033 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803174 367033 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162653308 366999 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802829 366999 0 None None None Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162669845 367081 0 None None None Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803729 367081 0 None None None Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162672910 367103 0 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803913 367103 0 None None None Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
9959777 393706 10 None None None Human 8.9 pIC50 = 8.9 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 571 10 2 8 6.8 CCc1sc(CCc2cc(N3CCOCC3)cc(NC(C)c3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL564536 393706 10 None None None Human 8.9 pIC50 = 8.9 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 571 10 2 8 6.8 CCc1sc(CCc2cc(N3CCOCC3)cc(NC(C)c3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2009.05.069
44288313 328109 0 None None None Human 7.0 pIC50 = 7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 525 11 5 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL417711 328109 0 None None None Human 7.0 pIC50 = 7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 525 11 5 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
44288022 331348 0 None None None Human 6.0 pIC50 = 6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 499 10 6 4 3.1 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NC1CCc2cc(O)ccc21 10.1016/s0960-894x(00)00292-4
CHEMBL42793 331348 0 None None None Human 6.0 pIC50 = 6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 499 10 6 4 3.1 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NC1CCc2cc(O)ccc21 10.1016/s0960-894x(00)00292-4
563820 118358 4 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 321 3 1 2 4.3 OC1(c2ccccc2)CCN(Cc2ccccc2)C2CCCCC21 nan
CHEMBL1620460 118358 4 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 321 3 1 2 4.3 OC1(c2ccccc2)CCN(Cc2ccccc2)C2CCCCC21 nan
2942743 85231 8 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 367 5 1 2 6.1 CC(Sc1ccc(Cl)cc1)C(=O)Nc1ccccc1-c1ccccc1 nan
CHEMBL1493277 85231 8 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 367 5 1 2 6.1 CC(Sc1ccc(Cl)cc1)C(=O)Nc1ccccc1-c1ccccc1 nan
9594209 217613 2 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 538 12 2 7 3.0 COc1ccc(/C=N/NC(=O)CN(CCc2ccccc2)S(=O)(=O)c2ccc(NC(C)=O)cc2)cc1OC nan
CHEMBL3194054 217613 2 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 538 12 2 7 3.0 COc1ccc(/C=N/NC(=O)CN(CCc2ccccc2)S(=O)(=O)c2ccc(NC(C)=O)cc2)cc1OC nan
3340390 63245 5 None -6 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 528 14 0 2 7.7 O=P(CCCCCCCCCP(=O)(c1ccccc1)c1ccccc1)(c1ccccc1)c1ccccc1 nan
CHEMBL1385608 63245 5 None -6 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 528 14 0 2 7.7 O=P(CCCCCCCCCP(=O)(c1ccccc1)c1ccccc1)(c1ccccc1)c1ccccc1 nan
44634614 145125 0 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 528 2 3 5 3.8 C/C1=C/[C@@H](C)C/C=C/[C@H]2[C@@H]3O[C@]3(C)[C@@H](C)[C@H]3[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@@]23C(=O)/C=C\C(=O)[C@@H]1O nan
CHEMBL2004475 145125 0 None -2 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 528 2 3 5 3.8 C/C1=C/[C@@H](C)C/C=C/[C@H]2[C@@H]3O[C@]3(C)[C@@H](C)[C@H]3[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@@]23C(=O)/C=C\C(=O)[C@@H]1O nan
16192223 77764 4 None None None Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 403 7 1 5 4.6 Cc1ccc(-n2cc(CNCCn3nc(C)cc3C)c(-c3ccc(F)cc3)n2)cc1 nan
CHEMBL1426722 77764 4 None None None Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 403 7 1 5 4.6 Cc1ccc(-n2cc(CNCCn3nc(C)cc3C)c(-c3ccc(F)cc3)n2)cc1 nan
162670721 367085 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803781 367085 0 None None None Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44288140 200518 0 None None None Human 7.0 pIC50 = 7.0 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 457 11 5 3 2.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL289620 200518 0 None None None Human 7.0 pIC50 = 7.0 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 457 11 5 3 2.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
44288235 333304 0 None None None Human 6.0 pIC50 = 6.0 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 531 9 4 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL43627 333304 0 None None None Human 6.0 pIC50 = 6.0 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 531 9 4 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
865459 59106 3 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 244 3 0 4 3.2 CCSc1nc2ccc(OC)cc2cc1C#N nan
CHEMBL1349920 59106 3 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 244 3 0 4 3.2 CCSc1nc2ccc(OC)cc2cc1C#N nan
2948077 58190 14 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 327 4 0 6 3.6 O=C(CSc1nc2ccccc2o1)c1ccc2c(c1)OCCO2 nan
CHEMBL1342128 58190 14 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 327 4 0 6 3.6 O=C(CSc1nc2ccccc2o1)c1ccc2c(c1)OCCO2 nan
44287731 317283 0 None None None Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 472 12 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(00)00292-4
CHEMBL41392 317283 0 None None None Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 472 12 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(00)00292-4
2788869 67480 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 444 8 0 6 5.4 CCC(Oc1ccc2c(=O)c(-c3ccccc3OC)coc2c1)C(=O)OCc1ccccc1 nan
CHEMBL1423382 67480 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 444 8 0 6 5.4 CCC(Oc1ccc2c(=O)c(-c3ccccc3OC)coc2c1)C(=O)OCc1ccccc1 nan
2243399 81001 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 254 4 1 4 2.8 C=CCNc1nc(N2CCCC2)nc2ccccc12 nan
CHEMBL1456185 81001 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 254 4 1 4 2.8 C=CCNc1nc(N2CCCC2)nc2ccccc12 nan
44287938 200570 0 None -20 3 Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL290175 200570 0 None -20 3 Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL4281479 478156 6 None None None Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 4308 134 63 59 -15.8 CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
44288311 311586 0 None None None Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 565 9 4 3 4.8 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL40475 311586 0 None None None Human 4.9 pIC50 = 4.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 565 9 4 3 4.8 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
1504749 63019 9 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 308 4 1 6 2.5 Cc1ccc(COC(=O)c2nn(-c3ccccc3)nc2N)cc1 nan
CHEMBL1383610 63019 9 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 308 4 1 6 2.5 Cc1ccc(COC(=O)c2nn(-c3ccccc3)nc2N)cc1 nan
5140222 99419 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 402 8 1 4 4.5 CCC(C)(C(=O)NC1CCCCC1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
CHEMBL1533962 99419 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 402 8 1 4 4.5 CCC(C)(C(=O)NC1CCCCC1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
2085549 106637 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 357 5 0 7 5.2 c1ccc(-c2nc(CSc3nnc(-c4cccs4)o3)cs2)cc1 nan
CHEMBL1600727 106637 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 357 5 0 7 5.2 c1ccc(-c2nc(CSc3nnc(-c4cccs4)o3)cs2)cc1 nan
45267382 393194 0 None None None Human 4.9 pIC50 = 4.9 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 374 9 1 7 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCOC)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL562677 393194 0 None None None Human 4.9 pIC50 = 4.9 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 374 9 1 7 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCOC)n2)nc1C 10.1016/j.bmcl.2009.05.069
2862130 43538 14 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 386 4 0 4 4.5 CCC1=Nc2ccc(Br)cc2C(c2ccccc2)N1CC(=O)OC nan
CHEMBL1300782 43538 14 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 386 4 0 4 4.5 CCC1=Nc2ccc(Br)cc2C(c2ccccc2)N1CC(=O)OC nan
1816029 60107 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 294 5 0 4 3.6 CCCCOc1nc2ccccc2c(=O)n1-c1ccccc1 nan
CHEMBL1359694 60107 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 294 5 0 4 3.6 CCCCOc1nc2ccccc2c(=O)n1-c1ccccc1 nan
854958 66204 10 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 324 3 3 5 3.4 CCc1cc(-c2[nH]ncc2-c2ccc3c(c2)OCO3)c(O)cc1O nan
CHEMBL1412538 66204 10 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 324 3 3 5 3.4 CCc1cc(-c2[nH]ncc2-c2ccc3c(c2)OCO3)c(O)cc1O nan
2285391 59306 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 349 8 1 3 4.1 Cc1cccc(CSCCNC(=O)COc2ccc(Cl)cc2)c1 nan
CHEMBL1351633 59306 7 None None None Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 349 8 1 3 4.1 Cc1cccc(CSCCNC(=O)COc2ccc(Cl)cc2)c1 nan
860841 79040 4 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 327 3 0 6 3.7 Clc1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1 nan
CHEMBL1439255 79040 4 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 327 3 0 6 3.7 Clc1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1 nan
667608 117937 6 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 299 4 0 3 4.3 CN1CCC(Oc2ccccc2Sc2ccccc2)CC1 nan
CHEMBL1616825 117937 6 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 299 4 0 3 4.3 CN1CCC(Oc2ccccc2Sc2ccccc2)CC1 nan
12004848 60744 2 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 246 5 1 3 2.5 CCCCOc1ccc(C2=NNC(=O)CC2)cc1 nan
CHEMBL1365319 60744 2 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 246 5 1 3 2.5 CCCCOc1ccc(C2=NNC(=O)CC2)cc1 nan
5132730 59486 11 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 354 9 2 4 2.7 CCCCCCNS(=O)(=O)c1ccc(NC(=O)C2CCCO2)cc1 nan
CHEMBL1353075 59486 11 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 354 9 2 4 2.7 CCCCCCNS(=O)(=O)c1ccc(NC(=O)C2CCCO2)cc1 nan
162655171 367007 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802928 367007 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44287998 308763 0 None None None Human 5.9 pIC50 = 5.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
CHEMBL40430 308763 0 None None None Human 5.9 pIC50 = 5.9 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
11958626 63923 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 352 8 2 5 3.3 CCCCNC(=O)c1onc(CSc2ccccc2F)c1C(=O)O nan
CHEMBL1391119 63923 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 352 8 2 5 3.3 CCCCNC(=O)c1onc(CSc2ccccc2F)c1C(=O)O nan
9869677 124403 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 7 4.9 CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771260 124403 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 7 4.9 CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
44229545 392587 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 375 6 1 8 3.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)sc1C 10.1016/j.bmcl.2009.05.069
CHEMBL560382 392587 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 375 6 1 8 3.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)sc1C 10.1016/j.bmcl.2009.05.069
45269118 393210 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 402 9 1 8 2.5 CCOC(=O)CNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
CHEMBL562831 393210 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 402 9 1 8 2.5 CCOC(=O)CNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
3487983 118820 0 None None None Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 289 1 0 1 3.9 CC1CC(C)CN(C2=CC(=[N+]3CCCC3)CC(C)(C)C2)C1 nan
CHEMBL1624501 118820 0 None None None Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 289 1 0 1 3.9 CC1CC(C)CN(C2=CC(=[N+]3CCCC3)CC(C)(C)C2)C1 nan
162662291 367047 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803298 367047 0 None None None Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
45268225 393703 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 344 7 1 6 3.0 CCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
CHEMBL564513 393703 0 None None None Human 4.8 pIC50 = 4.8 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 344 7 1 6 3.0 CCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
16192231 86412 6 None None None Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 375 7 0 4 4.6 CCOC(=O)C1(CCCc2ccccc2)CCN(C2CCSCC2)CC1 nan
CHEMBL1504083 86412 6 None None None Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 375 7 0 4 4.6 CCOC(=O)C1(CCCc2ccccc2)CCN(C2CCSCC2)CC1 nan
11958550 101698 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 368 8 2 5 3.8 CCCCNC(=O)c1onc(CSc2ccc(Cl)cc2)c1C(=O)O nan
CHEMBL1555711 101698 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 368 8 2 5 3.8 CCCCNC(=O)c1onc(CSc2ccc(Cl)cc2)c1C(=O)O nan
1485 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
21129772 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
5311023 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
9869458 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL2440929 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL332347 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL44246 1304 7 None 7943 2 Human 7.8 pIC50 = 7.8 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
2669460 100712 2 None None None Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 323 4 1 3 4.5 CC(C)(C)NC(=O)c1oc2ccccc2c1COc1ccccc1 nan
CHEMBL1545205 100712 2 None None None Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 323 4 1 3 4.5 CC(C)(C)NC(=O)c1oc2ccccc2c1COc1ccccc1 nan
3849628 218017 11 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 377 7 1 7 3.9 CCOC(=O)C(/C=N/c1cc(C)nn1-c1ccc(Cl)cc1)=C(\O)OCC nan
CHEMBL3198593 218017 11 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 377 7 1 7 3.9 CCOC(=O)C(/C=N/c1cc(C)nn1-c1ccc(Cl)cc1)=C(\O)OCC nan
1915932 59165 5 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 412 5 1 4 5.1 CC(C)OC(=O)/C(=C/c1ccc2c(c1)c1ccccc1n2C)NC(=O)c1ccccc1 nan
CHEMBL1350415 59165 5 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 412 5 1 4 5.1 CC(C)OC(=O)/C(=C/c1ccc2c(c1)c1ccccc1n2C)NC(=O)c1ccccc1 nan
1283502 99925 10 None None None Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 440 7 1 7 4.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2ccc(O)c(CN3CCOCC3)c12 nan
CHEMBL1538792 99925 10 None None None Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 440 7 1 7 4.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2ccc(O)c(CN3CCOCC3)c12 nan
44287999 317979 0 None 275 2 Human 6.7 pIC50 = 6.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41673 317979 0 None 275 2 Human 6.7 pIC50 = 6.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
4896972 58151 7 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 457 5 1 6 4.6 Cc1ccc(-c2nn3c(C)nnc3c3ccccc23)cc1S(=O)(=O)NC(C)c1ccccc1 nan
CHEMBL1341841 58151 7 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 457 5 1 6 4.6 Cc1ccc(-c2nn3c(C)nnc3c3ccccc23)cc1S(=O)(=O)NC(C)c1ccccc1 nan
9805674 124404 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 491 9 2 7 5.3 CCCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771261 124404 0 None None None Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 491 9 2 7 5.3 CCCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
44229547 390025 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 373 7 1 8 3.0 CCc1oc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL551197 390025 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 373 7 1 8 3.0 CCc1oc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
45270796 390997 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 355 7 1 7 2.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL556183 390997 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 355 7 1 7 2.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
44288023 201433 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
CHEMBL296523 201433 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
4876785 97151 4 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 442 5 2 7 2.8 COc1ccc(NC(=O)c2nnc(O)c3ccccc23)cc1S(=O)(=O)N1CCCCC1 nan
CHEMBL1511420 97151 4 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 442 5 2 7 2.8 COc1ccc(NC(=O)c2nnc(O)c3ccccc23)cc1S(=O)(=O)N1CCCCC1 nan
44287730 316615 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 457 11 5 3 3.0 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41166 316615 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 457 11 5 3 3.0 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
11755611 333392 0 None None None Human 5.7 pIC50 = 5.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 497 9 4 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL43710 333392 0 None None None Human 5.7 pIC50 = 5.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 497 9 4 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
44229621 392646 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 369 8 1 7 2.9 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL560921 392646 0 None None None Human 4.7 pIC50 = 4.7 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 369 8 1 7 2.9 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCC#N)n2)nc1C 10.1016/j.bmcl.2009.05.069
44288257 333443 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL43753 333443 0 None None None Human 4.7 pIC50 = 4.7 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
647823 117180 6 None None None Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 470 9 1 9 4.1 COc1ccccc1CN(Cc1cc2cc(C)ccc2nc1O)Cc1nnnn1Cc1ccco1 nan
CHEMBL1608455 117180 6 None None None Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 470 9 1 9 4.1 COc1ccccc1CN(Cc1cc2cc(C)ccc2nc1O)Cc1nnnn1Cc1ccco1 nan
44288137 327716 0 None None None Human 5.6 pIC50 = 5.6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 471 11 4 3 3.2 C[C@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL433627 327716 0 None None None Human 5.6 pIC50 = 5.6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 471 11 4 3 3.2 C[C@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
45272520 391859 0 None None None Human 4.6 pIC50 = 4.6 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 358 7 1 6 3.4 CCc1oc(CCc2cc(N3CCOCC3)cc(NC(C)C)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL557648 391859 0 None None None Human 4.6 pIC50 = 4.6 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 358 7 1 6 3.4 CCc1oc(CCc2cc(N3CCOCC3)cc(NC(C)C)n2)nc1C 10.1016/j.bmcl.2009.05.069
9651051 218699 5 None -1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 334 7 1 6 2.1 CCCCC(=O)N/N=C/c1ccc(N2CCOCC2)c([N+](=O)[O-])c1 nan
CHEMBL3213775 218699 5 None -1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 334 7 1 6 2.1 CCCCC(=O)N/N=C/c1ccc(N2CCOCC2)c([N+](=O)[O-])c1 nan
2330392 45662 4 None None None Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 286 0 1 3 4.4 Nc1c2c(nc3sc4c(c13)CCCC4)CCCCCC2 nan
CHEMBL1319576 45662 4 None None None Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 286 0 1 3 4.4 Nc1c2c(nc3sc4c(c13)CCCC4)CCCCCC2 nan
162651924 354233 0 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5195 171 80 72 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
CHEMBL4751466 354233 0 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5195 171 80 72 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
44517723 387839 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAntagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 581 8 1 4 6.0 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)F)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL540466 387839 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAntagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 581 8 1 4 6.0 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)F)cc1 10.1016/j.bmcl.2009.06.050
44288067 331185 0 None 57 2 Human 6.6 pIC50 = 6.6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL42747 331185 0 None 57 2 Human 6.6 pIC50 = 6.6 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
162652708 366994 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802795 366994 0 None None None Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44288395 318059 0 None 3 3 Human 5.5 pIC50 = 5.5 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
CHEMBL41686 318059 0 None 3 3 Human 5.5 pIC50 = 5.5 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
1454987 102479 3 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 412 6 1 4 4.6 COc1ccccc1N(CC(=O)NC1CCCC1)C(=O)c1oc(C(C)(C)C)cc1C nan
CHEMBL1562842 102479 3 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 412 6 1 4 4.6 COc1ccccc1N(CC(=O)NC1CCCC1)C(=O)c1oc(C(C)(C)C)cc1C nan
826220 62203 22 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 289 4 1 2 4.9 O=C(O)c1ccc(N(c2ccccc2)c2ccccc2)cc1 nan
CHEMBL1376342 62203 22 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 289 4 1 2 4.9 O=C(O)c1ccc(N(c2ccccc2)c2ccccc2)cc1 nan
45271626 404448 0 None None None Human 4.5 pIC50 = 4.5 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 330 6 1 6 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NC)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL571013 404448 0 None None None Human 4.5 pIC50 = 4.5 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 330 6 1 6 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NC)n2)nc1C 10.1016/j.bmcl.2009.05.069
649706 44344 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 420 5 0 7 4.3 CCN(C(=O)c1ccc(C(C)(C)C)cc1)c1nnc(Cn2nnc3ccccc32)s1 nan
CHEMBL1307319 44344 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 420 5 0 7 4.3 CCN(C(=O)c1ccc(C(C)(C)C)cc1)c1nnc(Cn2nnc3ccccc32)s1 nan
3200707 117328 0 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 479 7 1 8 3.5 O=C(NC1CCCCC1)C(c1ccncc1)N(Cc1ccc2c(c1)OCO2)C(=O)c1cnsn1 nan
CHEMBL1609697 117328 0 None None None Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 479 7 1 8 3.5 O=C(NC1CCCCC1)C(c1ccncc1)N(Cc1ccc2c(c1)OCO2)C(=O)c1cnsn1 nan
3206677 44949 1 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 351 5 2 3 4.1 Cc1cc2cc(C)c(NCCNC(=O)c3cccc(F)c3)nc2cc1C nan
CHEMBL1312220 44949 1 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 351 5 2 3 4.1 Cc1cc2cc(C)c(NCCNC(=O)c3cccc(F)c3)nc2cc1C nan
4287464 118188 0 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 351 2 0 1 5.1 Cc1ccc(-[n+]2c(-c3ccccc3)cn3c2CCc2ccccc2-3)c(C)c1 nan
CHEMBL1619019 118188 0 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 351 2 0 1 5.1 Cc1ccc(-[n+]2c(-c3ccccc3)cn3c2CCc2ccccc2-3)c(C)c1 nan
44288053 333308 0 None None None Human 5.4 pIC50 = 5.4 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 458 11 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccn1 10.1016/s0960-894x(00)00292-4
CHEMBL43628 333308 0 None None None Human 5.4 pIC50 = 5.4 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 458 11 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccn1 10.1016/s0960-894x(00)00292-4
44229544 389628 0 None None None Human 4.4 pIC50 = 4.4 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 372 6 1 8 2.5 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)n(C)c1C 10.1016/j.bmcl.2009.05.069
CHEMBL549699 389628 0 None None None Human 4.4 pIC50 = 4.4 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 372 6 1 8 2.5 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)n(C)c1C 10.1016/j.bmcl.2009.05.069
5708012 58569 6 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 340 5 0 3 5.3 COc1ccc(Cn2c(/C=C/c3ccccc3)nc3ccccc32)cc1 nan
CHEMBL1345334 58569 6 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 340 5 0 3 5.3 COc1ccc(Cn2c(/C=C/c3ccccc3)nc3ccccc32)cc1 nan
5806576 78005 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 373 4 0 5 4.8 N#CC(C#N)=C1C=CC=CN1/C(=C\c1ccco1)C(=O)c1ccc(Cl)cc1 nan
CHEMBL1428935 78005 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 373 4 0 5 4.8 N#CC(C#N)=C1C=CC=CN1/C(=C\c1ccco1)C(=O)c1ccc(Cl)cc1 nan
4140078 59540 9 None -2 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 377 4 0 4 4.6 Cc1cccc(-n2ccnc2SCC(=O)N2CCCc3ccccc32)c1C nan
CHEMBL1353428 59540 9 None -2 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 377 4 0 4 4.6 Cc1cccc(-n2ccnc2SCC(=O)N2CCCc3ccccc32)c1C nan
162651402 354063 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5221 175 80 73 -23.1 CC[C@H](C)[C@H](NC(=O)C(Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
CHEMBL4749279 354063 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5221 175 80 73 -23.1 CC[C@H](C)[C@H](NC(=O)C(Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
5740982 64989 5 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 366 5 0 3 5.1 Cc1ccccc1/C=C/c1nc2ccccc2c(=O)n1CCc1ccccc1 nan
CHEMBL1402158 64989 5 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 366 5 0 3 5.1 Cc1ccccc1/C=C/c1nc2ccccc2c(=O)n1CCc1ccccc1 nan
45269121 392564 0 None None None Human 5.4 pIC50 = 5.4 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 398 7 1 6 3.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC(F)(F)F)n2)nc1C 10.1016/j.bmcl.2009.05.069
CHEMBL560182 392564 0 None None None Human 5.4 pIC50 = 5.4 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 398 7 1 6 3.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC(F)(F)F)n2)nc1C 10.1016/j.bmcl.2009.05.069
2897425 45024 8 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 394 9 1 5 4.2 CCN(CC)CC(O)COc1ccc2c(c1)c(C(C)=O)c(C)n2-c1ccccc1 nan
CHEMBL1312713 45024 8 None 1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 394 9 1 5 4.2 CCN(CC)CC(O)COc1ccc2c(c1)c(C(C)=O)c(C)n2-c1ccccc1 nan
1186757 86274 9 None None None Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 375 4 1 7 2.1 O=c1c2ccccc2nc2c3ccccc3c(NCCN3CCOCC3)nn12 nan
CHEMBL1502859 86274 9 None None None Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 375 4 1 7 2.1 O=c1c2ccccc2nc2c3ccccc3c(NCCN3CCOCC3)nn12 nan
1249075 104468 5 None None None Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 429 4 1 4 5.3 CN1CCN(c2ccccc2NC(=O)c2ccc(-c3ccc(Cl)cc3Cl)o2)CC1 nan
CHEMBL1580409 104468 5 None None None Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 429 4 1 4 5.3 CN1CCN(c2ccccc2NC(=O)c2ccc(-c3ccc(Cl)cc3Cl)o2)CC1 nan
254021 328119 24 None -3 3 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 223 0 1 3 2.3 Nc1ccc2c(c1)C(=O)C(=O)c1ccccc1-2 nan
CHEMBL417727 328119 24 None -3 3 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 223 0 1 3 2.3 Nc1ccc2c(c1)C(=O)C(=O)c1ccccc1-2 nan
162651028 366985 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802711 366985 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
1201829 99169 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 437 8 1 5 4.7 COc1cccc(-c2ccc(C#N)c(SCC(=O)NCCc3ccc(Cl)cc3)n2)c1 nan
CHEMBL1531745 99169 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 437 8 1 5 4.7 COc1cccc(-c2ccc(C#N)c(SCC(=O)NCCc3ccc(Cl)cc3)n2)c1 nan
102509168 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287924 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287982 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL42686 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL43523 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL4776204 331090 0 None -208 3 Human 5.3 pIC50 = 5.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
1505224 66965 9 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 392 5 2 9 2.1 COC(=O)c1ccccc1NC(=O)Cn1c(-c2nonc2N)nc2ccccc21 nan
CHEMBL1419096 66965 9 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 392 5 2 9 2.1 COC(=O)c1ccccc1NC(=O)Cn1c(-c2nonc2N)nc2ccccc21 nan
4526399 82865 9 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 500 5 0 7 5.1 COC(=O)c1c(C)oc2ccc(N(C(=O)c3ccncc3)S(=O)(=O)c3ccc4ccccc4c3)cc12 nan
CHEMBL1471779 82865 9 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 500 5 0 7 5.1 COC(=O)c1c(C)oc2ccc(N(C(=O)c3ccncc3)S(=O)(=O)c3ccc4ccccc4c3)cc12 nan
1220296 85873 9 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 396 3 1 4 5.2 Cc1ccc(-c2cc(C(=O)Nc3ccc4c(c3)OCCO4)c3ccccc3n2)cc1 nan
CHEMBL1499276 85873 9 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 396 3 1 4 5.2 Cc1ccc(-c2cc(C(=O)Nc3ccc4c(c3)OCCO4)c3ccccc3n2)cc1 nan
9566117 218517 11 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 317 5 2 2 3.4 S=C(NCCc1ccccc1)N/N=C/c1ccccc1Cl nan
CHEMBL3211272 218517 11 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 317 5 2 2 3.4 S=C(NCCc1ccccc1)N/N=C/c1ccccc1Cl nan
2376964 82449 2 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 414 5 1 5 5.3 Nn1c(Cc2cccc3ccccc23)nnc1SCc1c(Cl)cccc1Cl nan
CHEMBL1468302 82449 2 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 414 5 1 5 5.3 Nn1c(Cc2cccc3ccccc23)nnc1SCc1c(Cl)cccc1Cl nan
44288236 331700 0 None None None Human 4.3 pIC50 = 4.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 573 10 4 3 4.7 N=C(N)NCCCC(NC(=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL42861 331700 0 None None None Human 4.3 pIC50 = 4.3 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 573 10 4 3 4.7 N=C(N)NCCCC(NC(=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
831603 105083 21 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 330 5 0 5 4.3 COc1ccc(-c2noc(COc3ccc(Cl)c(C)c3)n2)cc1 nan
CHEMBL1585445 105083 21 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 330 5 0 5 4.3 COc1ccc(-c2noc(COc3ccc(Cl)c(C)c3)n2)cc1 nan
3198 461850 54 None -18 34 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None -18 34 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None -18 34 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None -18 34 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
1302588 118457 7 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 346 8 2 3 4.0 O=C(COc1ccccc1CNCc1ccccc1)Nc1ccccc1 nan
CHEMBL1621407 118457 7 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 346 8 2 3 4.0 O=C(COc1ccccc1CNCc1ccccc1)Nc1ccccc1 nan
2609912 102100 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 392 5 0 7 4.1 COC(=O)c1ccc(CSc2nc3ccccc3c(=O)n2-c2ccccc2)o1 nan
CHEMBL1559259 102100 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 392 5 0 7 4.1 COC(=O)c1ccc(CSc2nc3ccccc3c(=O)n2-c2ccccc2)o1 nan
162648914 366975 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802592 366975 0 None None None Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
3706900 77866 6 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 405 7 1 4 3.5 CCC(NCCC(c1ccccc1)c1ccccc1)=C1C(=O)N(C)C(=O)N(C)C1=O nan
CHEMBL1427745 77866 6 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 405 7 1 4 3.5 CCC(NCCC(c1ccccc1)c1ccccc1)=C1C(=O)N(C)C(=O)N(C)C1=O nan
6413289 98137 11 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 372 3 0 3 5.8 Clc1ccc(CSc2cc3c(nn2)-c2ccccc2CC3)cc1Cl nan
CHEMBL1522356 98137 11 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 372 3 0 3 5.8 Clc1ccc(CSc2cc3c(nn2)-c2ccccc2CC3)cc1Cl nan
1183477 45023 14 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 375 4 1 4 4.7 COC(=O)c1cc(Cl)c(NC(=O)c2ccc(C(C)(C)C)cc2)cc1OC nan
CHEMBL1312703 45023 14 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 375 4 1 4 4.7 COC(=O)c1cc(Cl)c(NC(=O)c2ccc(C(C)(C)C)cc2)cc1OC nan
20846851 217699 3 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 398 6 1 4 4.4 O=C(N/N=C/c1ccco1)c1ccccc1OCc1ccc(Br)cc1 nan
CHEMBL3195229 217699 3 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 398 6 1 4 4.4 O=C(N/N=C/c1ccco1)c1ccccc1OCc1ccc(Br)cc1 nan
2181167 117909 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 367 7 1 2 5.0 Cc1cc(Cl)c(OCCCNCc2ccccc2)c(Br)c1 nan
CHEMBL1616638 117909 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 367 7 1 2 5.0 Cc1cc(Cl)c(OCCCNCc2ccccc2)c(Br)c1 nan
1477664 99832 21 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 359 5 0 4 5.7 Cc1nc(-c2ccccc2)sc1C(=O)CSc1ccc(Cl)cc1 nan
CHEMBL1537995 99832 21 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 359 5 0 4 5.7 Cc1nc(-c2ccccc2)sc1C(=O)CSc1ccc(Cl)cc1 nan
5338258 103137 4 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 259 3 0 2 4.1 O=C(/C=C/c1cccc2ccccc12)c1ccncc1 nan
CHEMBL1568243 103137 4 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 259 3 0 2 4.1 O=C(/C=C/c1cccc2ccccc12)c1ccncc1 nan
1894428 78284 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 388 8 0 7 3.8 CCOc1nc(SCCOc2ccc(Cl)cc2Cl)nc(N(C)C)n1 nan
CHEMBL1431004 78284 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 388 8 0 7 3.8 CCOc1nc(SCCOc2ccc(Cl)cc2Cl)nc(N(C)C)n1 nan
665164 117962 4 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 363 7 0 5 3.6 CC(C)COc1ccc(C(=O)OC2CC(C)(C)OCC2CN(C)C)cc1 nan
CHEMBL1617044 117962 4 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 363 7 0 5 3.6 CC(C)COc1ccc(C(=O)OC2CC(C)(C)OCC2CN(C)C)cc1 nan
647568 84411 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 335 4 0 6 4.1 CC(C)c1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1 nan
CHEMBL1487131 84411 3 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 335 4 0 6 4.1 CC(C)c1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1 nan
1543852 77408 11 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 371 4 0 4 5.6 N#Cc1ccc(-c2cccnc2)nc1SCc1ccc(Cl)c(Cl)c1 nan
CHEMBL1423799 77408 11 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 371 4 0 4 5.6 N#Cc1ccc(-c2cccnc2)nc1SCc1ccc(Cl)c(Cl)c1 nan
2198291 77839 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 401 6 1 2 6.5 O=C(CSCc1c(Cl)cccc1Cl)Nc1ccccc1-c1ccccc1 nan
CHEMBL1427504 77839 8 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 401 6 1 2 6.5 O=C(CSCc1c(Cl)cccc1Cl)Nc1ccccc1-c1ccccc1 nan
2450538 80706 2 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 407 6 1 3 5.8 O=C(COC(=O)c1ccc(-c2ccccc2)cc1)Nc1ccccc1-c1ccccc1 nan
CHEMBL1453672 80706 2 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 407 6 1 3 5.8 O=C(COC(=O)c1ccc(-c2ccccc2)cc1)Nc1ccccc1-c1ccccc1 nan
2385257 85263 2 None 3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 444 7 1 5 5.9 CCc1cccc(CC)c1NC(=O)COC(=O)c1ccccc1-c1nc2ccccc2s1 nan
CHEMBL1493500 85263 2 None 3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 444 7 1 5 5.9 CCc1cccc(CC)c1NC(=O)COC(=O)c1ccccc1-c1nc2ccccc2s1 nan
5281371 77777 16 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 426 5 0 7 4.4 C/C=C(/C)C(=O)O[C@@H]1c2c(ccc3ccc(=O)oc23)O[C@@H]1C(C)(C)OC(=O)/C(C)=C\C nan
CHEMBL1426896 77777 16 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 426 5 0 7 4.4 C/C=C(/C)C(=O)O[C@@H]1c2c(ccc3ccc(=O)oc23)O[C@@H]1C(C)(C)OC(=O)/C(C)=C\C nan
44288112 200378 2 None 2238 2 Human 7.2 pIC50 = 7.2 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
CHEMBL288355 200378 2 None 2238 2 Human 7.2 pIC50 = 7.2 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
826626 117927 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 293 4 0 2 5.1 CN(C)Cc1ccccc1Sc1cccc2ccccc12 nan
CHEMBL1616775 117927 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 293 4 0 2 5.1 CN(C)Cc1ccccc1Sc1cccc2ccccc12 nan
876519 118412 4 None 1 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 345 4 0 2 4.4 Cc1ccc(C(=O)C[n+]2cc(-c3ccccc3)n3c2CCCCC3)cc1 nan
CHEMBL1621027 118412 4 None 1 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 345 4 0 2 4.4 Cc1ccc(C(=O)C[n+]2cc(-c3ccccc3)n3c2CCCCC3)cc1 nan
2446403 47505 1 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 391 6 1 3 5.2 O=C(COC(=O)/C=C/c1ccc(Cl)cc1)Nc1ccccc1-c1ccccc1 nan
CHEMBL1335124 47505 1 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 391 6 1 3 5.2 O=C(COC(=O)/C=C/c1ccc(Cl)cc1)Nc1ccccc1-c1ccccc1 nan
1141823 62503 4 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 422 6 2 4 4.8 Cc1cccc(N=C(S)N(CCN(C)C)Cc2cc3cc(C)cc(C)c3nc2O)c1 nan
CHEMBL1379143 62503 4 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 422 6 2 4 4.8 Cc1cccc(N=C(S)N(CCN(C)C)Cc2cc3cc(C)cc(C)c3nc2O)c1 nan
9550576 64209 5 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 458 8 1 5 3.6 Cc1ccccc1C(=O)c1cccn1CC(=O)NCCN1CCN(c2cccc(C)c2C)CC1 nan
CHEMBL1393538 64209 5 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 458 8 1 5 3.6 Cc1ccccc1C(=O)c1cccn1CC(=O)NCCN1CCN(c2cccc(C)c2C)CC1 nan
6871377 217317 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 295 3 1 4 3.7 CC(C)COC(=O)c1cccc2c1-c1ccccc1/C2=N\O nan
CHEMBL3190644 217317 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 295 3 1 4 3.7 CC(C)COC(=O)c1cccc2c1-c1ccccc1/C2=N\O nan
714054 46569 7 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 331 4 0 5 4.2 N#Cc1nc(COc2ccc(Cl)cc2)oc1N1CCCCCC1 nan
CHEMBL1327690 46569 7 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 331 4 0 5 4.2 N#Cc1nc(COc2ccc(Cl)cc2)oc1N1CCCCCC1 nan
955150 47657 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 335 4 0 3 5.2 O=C(c1ccco1)c1cn(Cc2ccc(Cl)cc2)c2ccccc12 nan
CHEMBL1336318 47657 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 335 4 0 3 5.2 O=C(c1ccco1)c1cn(Cc2ccc(Cl)cc2)c2ccccc12 nan
1490113 65587 11 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 446 4 0 4 5.6 Cc1c(OCc2c(F)cccc2Cl)c(=O)ccn1-c1ncc(C(F)(F)F)cc1Cl nan
CHEMBL1407634 65587 11 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 446 4 0 4 5.6 Cc1c(OCc2c(F)cccc2Cl)c(=O)ccn1-c1ncc(C(F)(F)F)cc1Cl nan
1460705 118330 2 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 326 3 1 2 4.4 CC1=CC(C)(C)N(C(=O)CNC2CCCCC2)c2cc(C)ccc21 nan
CHEMBL1620238 118330 2 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 326 3 1 2 4.4 CC1=CC(C)(C)N(C(=O)CNC2CCCCC2)c2cc(C)ccc21 nan
2744454 79789 12 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 314 3 1 3 4.7 O=C(Nc1ccc(Cl)cc1)c1csc(-c2ccccc2)n1 nan
CHEMBL1446166 79789 12 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 314 3 1 3 4.7 O=C(Nc1ccc(Cl)cc1)c1csc(-c2ccccc2)n1 nan
2577652 103837 3 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 390 4 0 8 3.5 COC(=O)c1ccc(CSc2nc3sc4c(c3c(=O)n2C)CCCC4)o1 nan
CHEMBL1574689 103837 3 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 390 4 0 8 3.5 COC(=O)c1ccc(CSc2nc3sc4c(c3c(=O)n2C)CCCC4)o1 nan
5854588 117411 9 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 328 5 0 4 5.2 Clc1ccccc1CSc1nnc(/C=C/c2ccccc2)o1 nan
CHEMBL1610409 117411 9 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 328 5 0 4 5.2 Clc1ccccc1CSc1nnc(/C=C/c2ccccc2)o1 nan
4525145 118460 2 None -16 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21 nan
6140197 118460 2 None -16 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21 nan
73945770 118460 2 None -16 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21 nan
CHEMBL1621471 118460 2 None -16 3 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21 nan
9869041 124402 12 None None None Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771259 124402 12 None None None Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
162654570 367003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802896 367003 0 None None None Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44229546 393246 0 None None None Human 4.2 pIC50 = 4.2 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 6 1 8 2.8 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)oc1C 10.1016/j.bmcl.2009.05.069
CHEMBL563011 393246 0 None None None Human 4.2 pIC50 = 4.2 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 6 1 8 2.8 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)oc1C 10.1016/j.bmcl.2009.05.069
6858398 218359 10 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 322 6 0 6 3.1 COc1cc(/C=N/n2cnnc2)ccc1OCc1ccc(C)cc1 nan
CHEMBL3208997 218359 10 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 322 6 0 6 3.1 COc1cc(/C=N/n2cnnc2)ccc1OCc1ccc(C)cc1 nan
9563579 144710 9 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 325 5 0 4 4.7 C/C(=N\OC(=O)c1ccc(OC(C)C)cc1)c1ccc(C)c(C)c1 nan
CHEMBL1990096 144710 9 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 325 5 0 4 4.7 C/C(=N\OC(=O)c1ccc(OC(C)C)cc1)c1ccc(C)c(C)c1 nan
4557532 46722 4 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 434 3 1 5 5.6 Cc1nc(N2CCCCC2)c2c(C)c(C(=O)Nc3ccccc3C(F)(F)F)sc2n1 nan
CHEMBL1328939 46722 4 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 434 3 1 5 5.6 Cc1nc(N2CCCCC2)c2c(C)c(C(=O)Nc3ccccc3C(F)(F)F)sc2n1 nan
649757 100801 12 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 383 3 1 5 5.0 Cc1onc(-c2ccccc2Cl)c1C(=O)Nc1sc2c(c1C#N)CCC2 nan
CHEMBL1545971 100801 12 None -1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 383 3 1 5 5.0 Cc1onc(-c2ccccc2Cl)c1C(=O)Nc1sc2c(c1C#N)CCC2 nan
3235942 83677 5 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 415 4 1 7 3.4 COc1ccc(-n2nc(C(=O)Nc3ccc4c(c3)OCO4)c3ccccc3c2=O)cc1 nan
CHEMBL1480648 83677 5 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 415 4 1 7 3.4 COc1ccc(-n2nc(C(=O)Nc3ccc4c(c3)OCO4)c3ccccc3c2=O)cc1 nan
664856 44489 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 281 1 0 4 3.9 Cc1nc(N2CCC(C)CC2)c2oc3ccccc3c2n1 nan
CHEMBL1308461 44489 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 281 1 0 4 3.9 Cc1nc(N2CCC(C)CC2)c2oc3ccccc3c2n1 nan
1183030 393814 11 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 394 6 1 4 5.5 Cc1ccc(CCC(=O)Nc2ncc(Cc3cc(Cl)ccc3Cl)s2)o1 nan
CHEMBL564979 393814 11 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 394 6 1 4 5.5 Cc1ccc(CCC(=O)Nc2ncc(Cc3cc(Cl)ccc3Cl)s2)o1 nan
1998473 63362 9 None 2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 313 6 0 4 3.7 CN(C)CCCSc1nc(-c2ccccc2)nc2c1CCC2 nan
CHEMBL1386511 63362 9 None 2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 313 6 0 4 3.7 CN(C)CCCSc1nc(-c2ccccc2)nc2c1CCC2 nan
2311088 118472 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 387 3 0 2 5.2 COc1ccc(-[n+]2c(-c3ccc(Cl)cc3)cn3c2CCc2ccccc2-3)cc1 nan
CHEMBL1621585 118472 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 387 3 0 2 5.2 COc1ccc(-[n+]2c(-c3ccc(Cl)cc3)cn3c2CCc2ccccc2-3)cc1 nan
2173045 63016 5 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 346 5 2 3 3.1 Cc1ccc(NC(=O)C(=O)NCCOc2ccc(Cl)cc2)c(C)c1 nan
CHEMBL1383592 63016 5 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 346 5 2 3 3.1 Cc1ccc(NC(=O)C(=O)NCCOc2ccc(Cl)cc2)c(C)c1 nan
972410 118471 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 325 4 1 2 4.7 CC(C)(C)NCc1cc(Br)ccc1OC1CCCC1 nan
CHEMBL1621543 118471 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 325 4 1 2 4.7 CC(C)(C)NCc1cc(Br)ccc1OC1CCCC1 nan
663290 44857 10 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 426 6 0 6 5.0 Brc1ccc(CSc2nnc(-c3ccccn3)n2Cc2ccco2)cc1 nan
CHEMBL1311570 44857 10 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 426 6 0 6 5.0 Brc1ccc(CSc2nnc(-c3ccccn3)n2Cc2ccco2)cc1 nan
102509168 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287924 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287982 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL42686 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL43523 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL4776204 331090 0 None -208 3 Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287829 330997 0 None None None Human 4.1 pIC50 = 4.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 497 9 4 3 3.6 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL42625 330997 0 None None None Human 4.1 pIC50 = 4.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 497 9 4 3 3.6 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2ccccc2C1 10.1016/s0960-894x(00)00292-4
2940376 99978 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 496 10 1 8 4.0 COc1ccc(NC(=O)CSc2nc3ccccc3c(=O)n2CCCN2CCCCC2)c(OC)c1 nan
CHEMBL1539256 99978 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 496 10 1 8 4.0 COc1ccc(NC(=O)CSc2nc3ccccc3c(=O)n2CCCN2CCCCC2)c(OC)c1 nan
5290139 46794 9 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 496 11 2 10 4.6 CCOC(=O)CCCCC(=O)c1[nH]c(O)nc1CSc1nnc2c3ccccc3n(C(C)C)c2n1 nan
CHEMBL1329549 46794 9 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 496 11 2 10 4.6 CCOC(=O)CCCCC(=O)c1[nH]c(O)nc1CSc1nnc2c3ccccc3n(C(C)C)c2n1 nan
1798157 60897 9 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 342 5 2 2 4.2 CCCCCC(=O)NC(=S)Nc1ccc(Br)cc1C nan
CHEMBL1366620 60897 9 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 342 5 2 2 4.2 CCCCCC(=O)NC(=S)Nc1ccc(Br)cc1C nan
1235256 63798 12 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 311 1 1 2 5.2 Oc1cccc(-c2nc3ccc4ccccc4c3c3c2CCC3)c1 nan
CHEMBL1389982 63798 12 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 311 1 1 2 5.2 Oc1cccc(-c2nc3ccc4ccccc4c3c3c2CCC3)c1 nan
8178372 106519 1 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 282 3 1 2 4.1 O=C(/C=C/c1cccc(Cl)c1)c1nc2ccccc2[nH]1 nan
CHEMBL1599610 106519 1 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 282 3 1 2 4.1 O=C(/C=C/c1cccc(Cl)c1)c1nc2ccccc2[nH]1 nan
15944687 58299 4 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 370 4 0 6 4.7 COC(=O)c1cc2occc2n1Cc1nc(-c2ccccc2Cl)oc1C nan
CHEMBL1342925 58299 4 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 370 4 0 6 4.7 COC(=O)c1cc2occc2n1Cc1nc(-c2ccccc2Cl)oc1C nan
664816 79122 6 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 349 6 1 6 4.4 COc1ccc(-c2nc(C#N)c(NC(C)c3ccccc3)o2)cc1OC nan
CHEMBL1439981 79122 6 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 349 6 1 6 4.4 COc1ccc(-c2nc(C#N)c(NC(C)c3ccccc3)o2)cc1OC nan
2890146 103441 9 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 441 6 1 5 4.9 COc1ccc(-c2[nH]nc3c2C(c2ccc(OC)c(OC)c2)N(c2ccccc2)C3=O)cc1 nan
CHEMBL1570844 103441 9 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 441 6 1 5 4.9 COc1ccc(-c2[nH]nc3c2C(c2ccc(OC)c(OC)c2)N(c2ccccc2)C3=O)cc1 nan
2930337 82479 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 331 2 0 3 2.6 O=C1C2CC=C(Cl)CC2C(=O)N1CC1Cc2ccccc2CO1 nan
CHEMBL1468490 82479 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 331 2 0 3 2.6 O=C1C2CC=C(Cl)CC2C(=O)N1CC1Cc2ccccc2CO1 nan
101430 193616 15 None -1698 4 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 343 4 4 9 0.2 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccccc4)ncnc32)[C@H](O)[C@@H]1O nan
CHEMBL262083 193616 15 None -1698 4 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 343 4 4 9 0.2 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccccc4)ncnc32)[C@H](O)[C@@H]1O nan
44288390 317349 0 None 22 3 Human 7.1 pIC50 = 7.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41457 317349 0 None 22 3 Human 7.1 pIC50 = 7.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
44287923 278848 0 None None None Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 516 12 7 5 1.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
CHEMBL38531 278848 0 None None None Human 5.1 pIC50 = 5.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 516 12 7 5 1.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
162658382 354895 0 None -4 2 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5831 196 92 80 -23.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
CHEMBL4759334 354895 0 None -4 2 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
ChEMBL 5831 196 92 80 -23.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c01783
9590479 218727 7 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 386 6 1 3 5.0 O=C(CSCc1ccc(Cl)cc1)N/N=C/c1c(Cl)cccc1Cl nan
CHEMBL3214137 218727 7 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 386 6 1 3 5.0 O=C(CSCc1ccc(Cl)cc1)N/N=C/c1c(Cl)cccc1Cl nan
2182602 118540 3 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 361 8 0 2 5.0 Cc1ccc(OCCCCN(C)Cc2ccccc2)c(Br)c1 nan
CHEMBL1622175 118540 3 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 361 8 0 2 5.0 Cc1ccc(OCCCCN(C)Cc2ccccc2)c(Br)c1 nan
2235311 86848 7 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 461 7 0 4 6.4 O=C(CCc1nc(-c2ccccc2)c(-c2ccccc2)o1)OCc1ccc(Br)cc1 nan
CHEMBL1507807 86848 7 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 461 7 0 4 6.4 O=C(CCc1nc(-c2ccccc2)c(-c2ccccc2)o1)OCc1ccc(Br)cc1 nan
650606 102515 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 481 8 1 7 4.1 O=C(CN(Cc1ccc2c(c1)OCO2)C(=O)CSc1nc2ccccc2o1)NC1CCCCC1 nan
CHEMBL1563162 102515 8 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 481 8 1 7 4.1 O=C(CN(Cc1ccc2c(c1)OCO2)C(=O)CSc1nc2ccccc2o1)NC1CCCCC1 nan
659248 386853 8 None -1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 258 5 1 2 3.5 CCCCCCn1c2c(c(=N)c3c1CCC3)CCC2 nan
CHEMBL528708 386853 8 None -1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 258 5 1 2 3.5 CCCCCCn1c2c(c(=N)c3c1CCC3)CCC2 nan
2313223 118735 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 353 3 0 2 4.5 COc1ccccc1-n1c(-c2ccccc2)c[n+]2c1CCc1ccccc1-2 nan
CHEMBL1623694 118735 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
ChEMBL 353 3 0 2 4.5 COc1ccccc1-n1c(-c2ccccc2)c[n+]2c1CCc1ccccc1-2 nan
943274 87080 6 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 348 2 1 2 5.2 Cc1nc2ccc(F)cc2cc1C(=O)Nc1ccc(Cl)c(Cl)c1 nan
CHEMBL1509886 87080 6 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 348 2 1 2 5.2 Cc1nc2ccc(F)cc2cc1C(=O)Nc1ccc(Cl)c(Cl)c1 nan
6892993 217891 1 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 378 7 1 6 3.8 CCOc1ccc(Oc2c(/C=N/NC(C)=O)c(C)nn2-c2ccccc2)cc1 nan
CHEMBL3197426 217891 1 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 378 7 1 6 3.8 CCOc1ccc(Oc2c(/C=N/NC(C)=O)c(C)nn2-c2ccccc2)cc1 nan
44287971 328417 0 None 165 2 Human 6.1 pIC50 = 6.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41981 328417 0 None 165 2 Human 6.1 pIC50 = 6.1 Functional
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
45269117 392425 0 None None None Human 5.1 pIC50 = 5.1 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 358 8 1 6 3.4 CCCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
CHEMBL559593 392425 0 None None None Human 5.1 pIC50 = 5.1 Functional
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
ChEMBL 358 8 1 6 3.4 CCCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1 10.1016/j.bmcl.2009.05.069
1481087 63463 12 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 328 4 1 4 4.7 O=C(Nc1ccccc1)OCc1cc(-c2ccccc2Cl)on1 nan
CHEMBL1387309 63463 12 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 328 4 1 4 4.7 O=C(Nc1ccccc1)OCc1cc(-c2ccccc2Cl)on1 nan
1780041 62352 12 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 338 6 0 6 4.0 Clc1ccc(OCCSc2nnnn2C2CCCCC2)cc1 nan
CHEMBL1377743 62352 12 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 338 6 0 6 4.0 Clc1ccc(OCCSc2nnnn2C2CCCCC2)cc1 nan
2169010 105111 9 None -4 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 377 10 1 4 4.6 COc1ccccc1CCNCc1ccc(OC)c(OCc2ccccc2)c1 nan
CHEMBL1585652 105111 9 None -4 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 377 10 1 4 4.6 COc1ccccc1CCNCc1ccc(OC)c(OCc2ccccc2)c1 nan
4246341 60189 2 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 405 4 0 8 3.2 COc1ccc(-c2nnc3sc(C(C)N4C(=O)c5ccccc5C4=O)nn23)cc1 nan
CHEMBL1360426 60189 2 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 405 4 0 8 3.2 COc1ccc(-c2nnc3sc(C(C)N4C(=O)c5ccccc5C4=O)nn23)cc1 nan
2297248 118394 3 None None None Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 339 9 0 3 4.9 c1ccc(COc2ccc(OCCCCN3CCCCC3)cc2)cc1 nan
CHEMBL1620870 118394 3 None None None Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 339 9 0 3 4.9 c1ccc(COc2ccc(OCCCCN3CCCCC3)cc2)cc1 nan
162661307 367040 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803242 367040 0 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
ChEMBL 677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
665910 98726 4 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 390 2 1 6 3.8 Clc1ccc(C2=Nn3c(nnc3-c3[nH]nc4c3CCC4)SC2)cc1Cl nan
CHEMBL1527817 98726 4 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 390 2 1 6 3.8 Clc1ccc(C2=Nn3c(nnc3-c3[nH]nc4c3CCC4)SC2)cc1Cl nan
972422 106906 8 None 1 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 314 3 2 3 3.9 Cc1ccc(NC(S)=NCc2ccc3c(c2)OCO3)cc1C nan
CHEMBL1603366 106906 8 None 1 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
ChEMBL 314 3 2 3 3.9 Cc1ccc(NC(S)=NCc2ccc3c(c2)OCO3)cc1C nan
3081064 447432 7 None None None Human 4.4 pKd = 4.4 Functional
pA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cellspA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cells
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1 10.1016/0960-894X(95)00369-5
CHEMBL59832 447432 7 None None None Human 4.4 pKd = 4.4 Functional
pA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cellspA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cells
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1 10.1016/0960-894X(95)00369-5
9916525 213053 1 None None None Human 8.7 pKi = 8.7 Functional
Ability to reverse Neuropeptide Y receptor type 1-induced inhibition of forskolin-induced inhibition of forskolin-stimulated cAMPAbility to reverse Neuropeptide Y receptor type 1-induced inhibition of forskolin-induced inhibition of forskolin-stimulated cAMP
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
CHEMBL329536 213053 1 None None None Human 8.7 pKi = 8.7 Functional
Ability to reverse Neuropeptide Y receptor type 1-induced inhibition of forskolin-induced inhibition of forskolin-stimulated cAMPAbility to reverse Neuropeptide Y receptor type 1-induced inhibition of forskolin-induced inhibition of forskolin-stimulated cAMP
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
CHEMBL187555 139429 0 None None None Human 8.7 pKi = 8.7 Functional
Antagonist activity towards Neuropeptide Y receptor type 1Antagonist activity towards Neuropeptide Y receptor type 1
ChEMBL 591 10 4 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmcl.2004.10.005
10458754 80330 0 None None None Human 5.9 pKi = 5.9 Functional
Functional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cellsFunctional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cells
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145056 80330 0 None None None Human 5.9 pKi = 5.9 Functional
Functional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cellsFunctional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cells
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
9982218 201875 5 None None None Rat 4.7 pKi = 4.7 Functional
Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with Neuropeptide Y receptor type 1Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with Neuropeptide Y receptor type 1
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL299879 201875 5 None None None Rat 4.7 pKi = 4.7 Functional
Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with Neuropeptide Y receptor type 1Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with Neuropeptide Y receptor type 1
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL187620 139444 0 None None None Human 8.4 pKi = 8.4 Functional
Antagonist activity towards Neuropeptide Y receptor type 1Antagonist activity towards Neuropeptide Y receptor type 1
ChEMBL 615 10 4 10 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3OC)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
44362574 77464 0 None None None Human 5.3 pKi = 5.3 Functional
Functional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cellsFunctional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cells
ChEMBL 462 7 0 4 6.4 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142427 77464 0 None None None Human 5.3 pKi = 5.3 Functional
Functional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cellsFunctional Neuropeptide Y receptor type 1 antagonism was evaluated by its ability to reverse NPY induced inhibition of forskolin-stimulated cyclic AMP production in SK-N-MC cells
ChEMBL 462 7 0 4 6.4 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
1545 4687 0 None None None Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8590988
1504 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
44288922 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
CHEMBL438945 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
P01303 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
P07808 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
P57774 5725 8 None -16 4 Rat 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 1316999
1528 1302 21 None -8 5 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 9806339
5311022 1302 21 None -8 5 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 9806339
6324607 1302 21 None -8 5 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 9806339
CHEMBL1774204 1302 21 None -8 5 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 9806339
CHEMBL5315638 1302 21 None -8 5 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 9806339
1522 690 0 None -158 5 Human 6.0 pIC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12069595
1508 5882 0 None None None Rat 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4089 128 58 57 -18.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10694200
155817417 5882 0 None None None Rat 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 4089 128 58 57 -18.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10694200
1526 4693 0 None -3 2 Rat 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10694200
1514 6215 0 None None None Rat 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10694200
1514 6215 0 None None None Rat 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1316999
P10082 6215 0 None None None Rat 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10694200
P10082 6215 0 None None None Rat 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1316999
1545 4687 0 None -4 2 Rat 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1316999
1524 4689 0 None 1 2 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10694200
1529 3787 0 None 1 2 Rat 9.5 pIC50 None 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10694200
1528 1302 21 None 8 5 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10694200
5311022 1302 21 None 8 5 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10694200
6324607 1302 21 None 8 5 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10694200
CHEMBL1774204 1302 21 None 8 5 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10694200
CHEMBL5315638 1302 21 None 8 5 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10694200


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
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 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

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weight		 Rot
Bonds		 H don

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1821 410750 60 None None None Human 6.0 pAC50 = 6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
4212 410750 60 None None None Human 6.0 pAC50 = 6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL58 410750 60 None None None Human 6.0 pAC50 = 6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
DB01204 410750 60 None None None Human 6.0 pAC50 = 6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
72093 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
DB13500 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
4413 198369 45 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 198369 45 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
DB12598 198369 45 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
135409453 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2579 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
5362436 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
DB01079 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2335 26122 15 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3018 26122 15 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 26122 15 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
DB11125 26122 15 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
6436173 117955 32 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 117955 32 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
DB01220 117955 32 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
41684 64851 70 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 64851 70 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
DB00507 64851 70 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
214 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2350 39438 57 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
5029 39438 57 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
CHEMBL1219 39438 57 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
DB01129 39438 57 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
1016 8173 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 8173 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 8173 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 8173 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 8173 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2713 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
DB00878 470127 64 None None None Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
135398735 270475 30 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 270475 30 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
5381226 270475 30 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 270475 30 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
DB01045 270475 30 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
1887 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 5630 45 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
100 8289 46 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 8289 46 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 8289 46 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 8289 46 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 8289 46 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
3883 366871 80 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 366871 80 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
DB00448 366871 80 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
216416 221077 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 221077 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
DB06202 221077 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
2585 1662 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 1662 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 1662 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 1662 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 1662 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2600 8239 59 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 8239 59 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 8239 59 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 8239 59 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 8239 59 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2540 18749 72 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
475 18749 72 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 18749 72 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
DB00796 18749 72 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
51755 120201 39 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1651990 120201 39 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
DB13434 120201 39 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
3149 26881 13 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 26881 13 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
DB11594 26881 13 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
2327 23153 32 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 257 5 7 7 -1.8 NC(CO)C(=O)NNCc1ccc(O)c(O)c1O 10.1038/s41467-023-40064-9
CHEMBL1096979 23153 32 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 257 5 7 7 -1.8 NC(CO)C(=O)NNCc1ccc(O)c(O)c1O 10.1038/s41467-023-40064-9
DB12783 23153 32 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 257 5 7 7 -1.8 NC(CO)C(=O)NNCc1ccc(O)c(O)c1O 10.1038/s41467-023-40064-9
5329102 387203 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 387203 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
DB01268 387203 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
11980903 38402 12 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 38402 12 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 38402 12 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 38402 12 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
DB06816 38402 12 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
11626560 450637 63 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 450637 63 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
DB08865 450637 63 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
2179 332289 56 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 332289 56 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
DB00276 332289 56 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
2194 125802 64 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
CHEMBL178862 125802 64 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
DB13853 125802 64 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NPY1R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
171344683 386190 0 None None None Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5168 150 68 75 -11.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5271459 386190 0 None None None Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5168 150 68 75 -11.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171342457 386172 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4731 140 64 66 -12.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5270985 386172 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4731 140 64 66 -12.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171354036 386438 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5106 152 68 70 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5277749 386438 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5106 152 68 70 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171342457 386172 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4731 140 64 66 -12.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5270985 386172 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4731 140 64 66 -12.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171344683 386190 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5168 150 68 75 -11.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5271459 386190 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5168 150 68 75 -11.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171354036 386438 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5106 152 68 70 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5277749 386438 0 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5106 152 68 70 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171343037 386202 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4251 131 62 59 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5271764 386202 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4251 131 62 59 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171343037 386202 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4251 131 62 59 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5271764 386202 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4251 131 62 59 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171344725 386782 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4254 127 60 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5285523 386782 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4254 127 60 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171344725 386782 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4254 127 60 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5285523 386782 0 None None None Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 4254 127 60 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171347326 386253 0 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5916 174 76 83 -12.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5273099 386253 0 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5916 174 76 83 -12.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
171347326 386253 0 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5916 174 76 83 -12.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL5273099 386253 0 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysisAgonist activity at human Y1R expressed in myo-[2-3H]-inositol labelled African green monkey COS7 cells coexpressing chimeric Galphadelta6qi4myr protein assessed as accumulation of [2-3H]-IP after 1 hr by scintillation counting analysis
ChEMBL 5916 174 76 83 -12.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)c1ccc(N(C)Cc2cnc3nc(N)nc(N)c3n2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.6b00043
CHEMBL269503 484242 0 None None None Human 10.7 pIC50 = 10.7 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 4239 131 59 59 -17.6 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/jm000052z
10008757 372175 0 None None None Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 10.2 pIC50 = 10.2 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 10.2 pIC50 = 10.2 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
1504 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
44288922 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
CHEMBL438945 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
P01303 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
P07808 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
P57774 5725 8 None None None Human 10.2 pIC50 = 10.2 Binding
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2013.03.016
10030299 372365 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041306 274475 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.0 pIC50 = 10 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041306 274475 0 None None None Human 10.0 pIC50 = 10.0 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 10.0 pIC50 = 10.0 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10030299 372365 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487448 394124 0 None None None Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 9 1 8 5.0 CCc1sc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1CF 10.1016/j.bmcl.2009.07.030
CHEMBL567112 394124 0 None None None Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 9 1 8 5.0 CCc1sc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1CF 10.1016/j.bmcl.2009.07.030
72548703 317107 0 None None None Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 317107 0 None None None Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
1504 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
44288922 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
CHEMBL438945 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P01303 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P07808 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P57774 5725 8 None None None Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
127041306 274475 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487490 425689 0 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 441 7 1 8 4.8 Cc1cccc(CNc2cc(N3CCSCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL585669 425689 0 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 441 7 1 8 4.8 Cc1cccc(CNc2cc(N3CCSCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
127041306 274475 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
16132350 484239 20 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of radiolabeled NPY from human neuropeptide Y1 receptorDisplacement of radiolabeled NPY from human neuropeptide Y1 receptor
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL267633 484239 20 None None None Human 9.8 pIC50 = 9.8 Binding
Displacement of radiolabeled NPY from human neuropeptide Y1 receptorDisplacement of radiolabeled NPY from human neuropeptide Y1 receptor
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm8007618
16132350 484239 20 None None None Human 9.8 pIC50 = 9.8 Binding
Inhibition of Y1 (unknown origin)Inhibition of Y1 (unknown origin)
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acschembio.7b00481
CHEMBL267633 484239 20 None None None Human 9.8 pIC50 = 9.8 Binding
Inhibition of Y1 (unknown origin)Inhibition of Y1 (unknown origin)
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acschembio.7b00481
127041327 274545 0 None None None Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
45487447 425730 0 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(CF)c(C)s3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL585711 425730 0 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(CF)c(C)s3)n2)n1 10.1016/j.bmcl.2009.07.030
1504 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
44288922 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
CHEMBL438945 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
P01303 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
P07808 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
P57774 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmc.2016.11.014
127041327 274545 0 None None None Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
1504 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
44288922 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
CHEMBL438945 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P01303 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P07808 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P57774 5725 8 None None None Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
10030299 372365 0 None None None Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487489 393967 0 None None None Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 445 7 1 8 4.7 Cc1nc(SCc2cc(N3CCSCC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL566020 393967 0 None None None Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 445 7 1 8 4.7 Cc1nc(SCc2cc(N3CCSCC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
45487435 393970 0 None None None Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 441 7 1 8 4.6 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)s3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL566041 393970 0 None None None Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 441 7 1 8 4.6 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)s3)n2)n1 10.1016/j.bmcl.2009.07.030
127041619 274547 0 None None None Human 9.5 pIC50 = 9.5 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.5 pIC50 = 9.5 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041306 274475 0 None None None Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041327 274545 0 None None None Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
1528 1302 21 None None None Human 9.4 pIC50 = 9.4 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
5311022 1302 21 None None None Human 9.4 pIC50 = 9.4 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
6324607 1302 21 None None None Human 9.4 pIC50 = 9.4 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL1774204 1302 21 None None None Human 9.4 pIC50 = 9.4 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL5315638 1302 21 None None None Human 9.4 pIC50 = 9.4 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
45487524 394123 0 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 439 8 1 8 4.4 CCc1oc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1C 10.1016/j.bmcl.2009.07.030
CHEMBL567101 394123 0 None None None Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 439 8 1 8 4.4 CCc1oc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1C 10.1016/j.bmcl.2009.07.030
127041619 274547 0 None None None Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None None None Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487434 393969 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 451 7 1 8 4.4 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc4c(o3)CCCC4)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL566040 393969 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 451 7 1 8 4.4 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc4c(o3)CCCC4)n2)n1 10.1016/j.bmcl.2009.07.030
10030299 372365 0 None None None Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041306 274475 0 None None None Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487440 394005 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(CF)s3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL566255 394005 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(CF)s3)n2)n1 10.1016/j.bmcl.2009.07.030
45487464 394214 0 None None None Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 425 7 1 8 4.1 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL567719 394214 0 None None None Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 425 7 1 8 4.1 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
1528 1302 21 None None None Human 9.2 pIC50 = 9.2 Binding
Radioligand binding assay (NPY1R, BHK)Radioligand binding assay (NPY1R, BHK)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
5311022 1302 21 None None None Human 9.2 pIC50 = 9.2 Binding
Radioligand binding assay (NPY1R, BHK)Radioligand binding assay (NPY1R, BHK)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
6324607 1302 21 None None None Human 9.2 pIC50 = 9.2 Binding
Radioligand binding assay (NPY1R, BHK)Radioligand binding assay (NPY1R, BHK)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL1774204 1302 21 None None None Human 9.2 pIC50 = 9.2 Binding
Radioligand binding assay (NPY1R, BHK)Radioligand binding assay (NPY1R, BHK)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL5315638 1302 21 None None None Human 9.2 pIC50 = 9.2 Binding
Radioligand binding assay (NPY1R, BHK)Radioligand binding assay (NPY1R, BHK)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
10008757 372175 0 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
1528 1302 21 None None None Rat 9.1 pIC50 = 9.1 Binding
Radioligand binding assay (NPY1R, HEK293, rat)Radioligand binding assay (NPY1R, HEK293, rat)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
5311022 1302 21 None None None Rat 9.1 pIC50 = 9.1 Binding
Radioligand binding assay (NPY1R, HEK293, rat)Radioligand binding assay (NPY1R, HEK293, rat)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
6324607 1302 21 None None None Rat 9.1 pIC50 = 9.1 Binding
Radioligand binding assay (NPY1R, HEK293, rat)Radioligand binding assay (NPY1R, HEK293, rat)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL1774204 1302 21 None None None Rat 9.1 pIC50 = 9.1 Binding
Radioligand binding assay (NPY1R, HEK293, rat)Radioligand binding assay (NPY1R, HEK293, rat)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL5315638 1302 21 None None None Rat 9.1 pIC50 = 9.1 Binding
Radioligand binding assay (NPY1R, HEK293, rat)Radioligand binding assay (NPY1R, HEK293, rat)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
127041619 274547 0 None None None Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041327 274545 0 None None None Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
16132350 484239 20 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm801018u
CHEMBL267633 484239 20 None None None Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm801018u
1504 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
44288922 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
CHEMBL438945 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
P01303 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
P07808 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
P57774 5725 8 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/np900287e
10030299 372365 0 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44294536 371608 0 None None None Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 557 10 2 8 6.3 CCc1sc(CCc2cc(N3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL50184 371608 0 None None None Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 557 10 2 8 6.3 CCc1sc(CCc2cc(N3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
127041306 274475 0 None None None Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487522 394255 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL567928 394255 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
127041327 274545 0 None None None Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
45487523 394099 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 7 1 9 3.5 Cc1cccc(CNc2cc(N3CCS(=O)(=O)CC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL566889 394099 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 7 1 9 3.5 Cc1cccc(CNc2cc(N3CCS(=O)(=O)CC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
10414488 466724 0 None None None Rat 8.8 pIC50 = 8.8 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in rat
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm980521l
CHEMBL61532 466724 0 None None None Rat 8.8 pIC50 = 8.8 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in rat
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm980521l
CHEMBL4299523 478252 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assay
ChEMBL 4251 131 63 59 -17.8 CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC 10.1021/acs.jmedchem.5b00925
45487445 394256 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 443 8 1 8 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(CF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL567941 394256 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 443 8 1 8 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(CF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
45487433 394084 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 487 11 1 9 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(COCCF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL566664 394084 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 487 11 1 9 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(COCCF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL188790 139675 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 585 9 4 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
3474 7886 30 None None None Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None None None Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None None None Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
44409158 277956 0 None None None Human 7.0 pIC50 = 7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 523 5 1 5 6.2 CC1(F)CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL381510 277956 0 None None None Human 7.0 pIC50 = 7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 523 5 1 5 6.2 CC1(F)CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44271460 123113 0 None None None Human 6.0 pIC50 = 6 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 473 13 2 5 7.1 CCCCN(CCCC)CCCNc1nc(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL17450 123113 0 None None None Human 6.0 pIC50 = 6 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 473 13 2 5 7.1 CCCCN(CCCC)CCCNc1nc(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
44439436 181345 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCCNC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL238729 181345 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCCNC2)CC1 10.1016/j.bmcl.2006.11.034
16146918 316782 0 None None None Human 6.0 pIC50 = 6.0 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44342536 316782 0 None None None Human 6.0 pIC50 = 6.0 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
91931438 316782 0 None None None Human 6.0 pIC50 = 6.0 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL411800 316782 0 None None None Human 6.0 pIC50 = 6.0 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44294522 197115 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 556 11 2 7 7.7 CCc1sc(CCc2cc(OC3CCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL264820 197115 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 556 11 2 7 7.7 CCc1sc(CCc2cc(OC3CCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
44294698 385665 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 542 11 2 7 7.3 CCc1sc(CCc2cc(OC3CCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL52282 385665 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 542 11 2 7 7.3 CCc1sc(CCc2cc(OC3CCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
44439431 294054 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 530 5 0 5 6.0 CN1CCC(Cn2c3ccccc3c3cc(C(=O)N4CCN(C)CC4)cc(Oc4ccc(Cl)cc4)c32)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL392943 294054 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 530 5 0 5 6.0 CN1CCC(Cn2c3ccccc3c3cc(C(=O)N4CCN(C)CC4)cc(Oc4ccc(Cl)cc4)c32)CC1 10.1016/j.bmcl.2006.11.034
3474 7886 30 None None None Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None None None Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None None None Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL441007 488816 0 None None None Human 7.0 pIC50 = 7.0 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 3838 125 64 54 -18.2 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44294538 201749 0 None None None Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 530 11 2 7 7.2 CCc1sc(CCc2cc(OC(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL298983 201749 0 None None None Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 530 11 2 7 7.2 CCc1sc(CCc2cc(OC(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL124152 40508 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 591 10 3 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL324990 220042 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 606 10 3 8 6.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(S)=N/CCCN2CCC(c3cccc(OC)c3)CC2)c1 10.1016/s0960-894x(01)00765-x
9894291 157264 2 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 378 5 0 3 5.3 CCOc1cccc([C@]2(N3CCN(c4ccccc4)CC3)CC[C@@H](C)CC2)c1 10.1021/ml200265m
CHEMBL2046864 157264 2 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 378 5 0 3 5.3 CCOc1cccc([C@]2(N3CCN(c4ccccc4)CC3)CC[C@@H](C)CC2)c1 10.1021/ml200265m
10052173 120368 0 None None None Human 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
ChEMBL 513 6 1 6 4.5 COc1ccc2c(c1)CC(NCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL166606 120368 0 None None None Human 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
ChEMBL 513 6 1 6 4.5 COc1ccc2c(c1)CC(NCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44439493 182110 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 479 5 1 4 5.9 CN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL240221 182110 0 None None None Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 479 5 1 4 5.9 CN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
16144579 331898 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44342730 331898 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
91931426 331898 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL428992 331898 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL268409 486260 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1990 63 28 25 -7.0 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)O)C(C)C 10.1021/jm000052z
16146919 317217 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CN[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)Cc1ccc(O)cc1 10.1021/jm000052z
44342654 317217 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CN[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)Cc1ccc(O)cc1 10.1021/jm000052z
91931418 317217 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CN[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)Cc1ccc(O)cc1 10.1021/jm000052z
CHEMBL413232 317217 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CN[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)Cc1ccc(O)cc1 10.1021/jm000052z
21336511 119980 0 None None None Human 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL164897 119980 0 None None None Human 5.9 pIC50 = 5.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
62706261 157268 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1ccccc1[C@@]1(N2CCN(c3ccccc3)CC2)[C@H]2C[C@H](C)C[C@H]21 10.1021/ml200265m
CHEMBL2046869 157268 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1ccccc1[C@@]1(N2CCN(c3ccccc3)CC2)[C@H]2C[C@H](C)C[C@H]21 10.1021/ml200265m
1528 1302 21 None None None Human 5.9 pIC50 = 5.9 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
5311022 1302 21 None None None Human 5.9 pIC50 = 5.9 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
6324607 1302 21 None None None Human 5.9 pIC50 = 5.9 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL1774204 1302 21 None None None Human 5.9 pIC50 = 5.9 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
CHEMBL5315638 1302 21 None None None Human 5.9 pIC50 = 5.9 Binding
Radioligand binding assay (NPY1R, SK-N-MC)Radioligand binding assay (NPY1R, SK-N-MC)
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.6019/CHEMBL5463723
44409205 156696 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 534 7 0 6 5.5 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL203433 156696 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 534 7 0 6 5.5 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL115722 24438 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 583 9 3 8 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(S)=N/CCCN2CCN(C3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00765-x
16146061 333586 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CN[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
44342840 333586 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CN[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
91931430 333586 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CN[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
CHEMBL438923 333586 0 None None None Human 5.9 pIC50 = 5.9 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CN[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
44439439 181782 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 601 7 0 6 5.4 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCN(CC(=O)N(C)C)CC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL239568 181782 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 601 7 0 6 5.4 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCN(CC(=O)N(C)C)CC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL189036 139727 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 653 9 4 9 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C(F)(F)F)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
44377450 118401 0 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL162093 118401 0 None None None Human 4.9 pIC50 = 4.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44287999 317979 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41673 317979 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
44377460 105950 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 536 9 2 6 4.3 O=[N+]([O-])c1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL159450 105950 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 536 9 2 6 4.3 O=[N+]([O-])c1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
16147801 161945 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 63 30 26 -7.7 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44342360 161945 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 63 30 26 -7.7 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
91931424 161945 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 63 30 26 -7.7 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL214707 161945 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 63 30 26 -7.7 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44342809 316846 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 66 30 26 -7.3 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm000052z
91931442 316846 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 66 30 26 -7.3 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm000052z
CHEMBL412257 316846 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1989 66 30 26 -7.3 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm000052z
44409210 276366 0 None None None Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 521 7 0 6 5.6 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCOCC1 10.1016/j.bmcl.2005.11.104
CHEMBL378587 276366 0 None None None Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 521 7 0 6 5.6 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCOCC1 10.1016/j.bmcl.2005.11.104
CHEMBL266021 486183 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1930 66 29 26 -8.3 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm000052z
CHEMBL410792 488138 0 None None None Human 6.8 pIC50 = 6.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2014 62 29 26 -7.5 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
16146329 163906 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CN[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44342802 163906 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CN[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
91931419 163906 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CN[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL217692 163906 0 None None None Human 5.8 pIC50 = 5.8 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CN[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44294462 370118 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 544 13 2 7 7.6 CCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL48950 370118 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 544 13 2 7 7.6 CCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
44439430 316773 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCNCC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL411795 316773 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCNCC2)CC1 10.1016/j.bmcl.2006.11.034
3474 7886 30 None None None Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None None None Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None None None Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
44409242 278599 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL383763 278599 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44294563 201846 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 530 12 2 7 7.2 CCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL299598 201846 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 530 12 2 7 7.2 CCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
44294529 385712 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 556 12 2 7 7.6 CCc1sc(CCc2cc(OCC3(C)CC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL52325 385712 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 556 12 2 7 7.6 CCc1sc(CCc2cc(OCC3(C)CC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
62706424 157261 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 348 3 1 3 4.1 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(O)cc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
CHEMBL2046861 157261 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 348 3 1 3 4.1 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(O)cc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
44288390 317349 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41457 317349 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
44377440 120247 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 551 10 2 6 4.4 COc1cc2c(cc1OC)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL165556 120247 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 551 10 2 6 4.4 COc1cc2c(cc1OC)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL116864 24809 0 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 567 9 3 8 4.6 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCN(C3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00765-x
62706426 157263 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 350 3 0 2 4.5 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(F)cc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
CHEMBL2046863 157263 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 350 3 0 2 4.5 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(F)cc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
44377461 118402 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 505 8 2 4 4.7 Cc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL162094 118402 0 None None None Human 4.8 pIC50 = 4.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 505 8 2 4 4.7 Cc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL411200 488161 0 None None None Human 6.7 pIC50 = 6.7 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2003 65 30 26 -7.8 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm000052z
44287971 328417 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41981 328417 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
44439437 297409 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 574 6 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C3CC3)C[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL395640 297409 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 574 6 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C3CC3)C[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
44409237 278252 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCNC[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL382355 278252 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCNC[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44439491 182034 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 562 8 2 5 6.4 CN1CCCC1CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL240038 182034 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 562 8 2 5 6.4 CN1CCCC1CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
44409161 331011 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 527 5 1 5 6.1 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCC(F)(F)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL426314 331011 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 527 5 1 5 6.1 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCC(F)(F)CC1 10.1016/j.bmcl.2005.11.104
45487446 394293 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 10 1 9 4.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(OCCF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL568152 394293 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 473 10 1 9 4.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(OCCF)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
44288112 200378 2 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
CHEMBL288355 200378 2 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
62706421 157259 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 347 3 1 3 4.0 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1cccc(N)c1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
CHEMBL2046858 157259 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 347 3 1 3 4.0 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1cccc(N)c1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
44377689 120874 0 None None None Human 4.7 pIC50 = 4.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL167318 120874 0 None None None Human 4.7 pIC50 = 4.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44439444 293626 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 557 5 1 6 6.0 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCn2ccnc2C1 10.1016/j.bmcl.2006.11.034
CHEMBL392583 293626 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 557 5 1 6 6.0 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCn2ccnc2C1 10.1016/j.bmcl.2006.11.034
44439486 182088 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 536 8 1 5 5.8 CN(C)CCN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL240208 182088 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 536 8 1 5 5.8 CN(C)CCN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL187555 139429 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 591 10 4 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL188271 139577 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 561 9 4 8 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3)CC2)c1 10.1016/j.bmcl.2004.10.005
44396821 255521 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 606 10 4 10 4.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL366340 255521 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 606 10 4 10 4.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)c1 10.1016/j.bmcl.2004.10.005
25181112 352856 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
127041619 274547 0 None None None Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
1504 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
44288922 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
CHEMBL438945 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
P01303 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
P07808 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
P57774 5725 8 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2012.11.110
CHEMBL438411 484347 0 None None None Human 8.6 pIC50 = 8.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 4222 128 58 58 -15.7 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/jm000052z
10008757 372175 0 None None None Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44294565 370380 0 None None None Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 606 14 2 7 8.4 CCc1sc(CCc2cc(OCCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL49177 370380 0 None None None Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 606 14 2 7 8.4 CCc1sc(CCc2cc(OCCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
45487511 413245 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccc(F)nc3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL582790 413245 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccc(F)nc3)n2)oc1C 10.1016/j.bmcl.2009.07.030
44409121 157079 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44409155 157079 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL204050 157079 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL382836 157079 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
62706260 157267 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 332 3 0 2 4.4 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccccc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
CHEMBL2046868 157267 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 332 3 0 2 4.4 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccccc1)N1CCN(c2ccccc2)CC1 10.1021/ml200265m
44377854 238797 0 None None None Human 4.7 pIC50 = 4.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 507 10 2 5 3.8 COc1ccc2c(c1)CC(CNCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL351082 238797 0 None None None Human 4.7 pIC50 = 4.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 507 10 2 5 3.8 COc1ccc2c(c1)CC(CNCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
44287938 200570 0 None None None Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL290175 200570 0 None None None Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL432237 332773 0 None None None Human 6.6 pIC50 = 6.6 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 565 8 3 9 4.7 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(=N/CCCN2CCC(C(C)(C)C)CC2)NC#N)c1 10.1016/s0960-894x(01)00765-x
CHEMBL411637 488182 0 None None None Human 6.6 pIC50 = 6.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2076 62 31 26 -7.5 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44294671 371302 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 502 10 2 7 6.4 CCc1sc(CCc2cc(OC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL49795 371302 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 502 10 2 7 6.4 CCc1sc(CCc2cc(OC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
155512045 334189 0 None None None Human 6.6 pIC50 = 6.6 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1735 55 28 24 -2.7 COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC 10.1021/acs.jmedchem.6b00310
CHEMBL4436741 334189 0 None None None Human 6.6 pIC50 = 6.6 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1735 55 28 24 -2.7 COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC 10.1021/acs.jmedchem.6b00310
44294463 349878 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 578 12 2 7 8.0 CCc1sc(CCc2cc(OCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL45869 349878 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 578 12 2 7 8.0 CCc1sc(CCc2cc(OCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
44409268 276802 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCNC[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL379443 276802 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCNC[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
102509168 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287924 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
44287982 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL42686 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL43523 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL4776204 331090 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL187902 139506 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 645 10 4 9 5.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3OC(F)(F)F)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL412698 488243 0 None None None Human 6.6 pIC50 = 6.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2003 62 30 26 -8.2 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44409191 333828 0 None None None Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 423 3 0 5 4.2 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL440944 333828 0 None None None Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 423 3 0 5 4.2 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL430274 488569 0 None None None Human 6.6 pIC50 = 6.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1920 62 28 26 -8.5 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccsc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL268351 486257 0 None None None Human 4.6 pIC50 = 4.6 Binding
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
ChEMBL 1726 52 25 22 -5.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C1CCCCC1)C1CCCCC1 10.1016/S0960-894X(00)80696-4
44439489 331859 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 562 8 2 5 6.4 CCN1CCCC1CNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL428915 331859 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 562 8 2 5 6.4 CCN1CCCC1CNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
73353529 181839 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cnccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397200 181839 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cnccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL114040 24146 0 None None None Human 6.6 pIC50 = 6.6 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 585 9 3 9 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(=N/CCCN2CCC(c3ccccc3)CC2)NC#N)c1 10.1016/s0960-894x(01)00765-x
CHEMBL405527 487866 0 None None None Human 6.6 pIC50 = 6.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1990 64 28 25 -7.4 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL412378 488217 0 None None None Human 6.6 pIC50 = 6.6 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1990 63 28 25 -6.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44439433 181117 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL238517 181117 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL187782 139480 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 669 10 4 10 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3OC(F)(F)F)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
44377722 119992 0 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL164971 119992 0 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44439443 181894 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 557 5 2 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCc2[nH]cnc2C1 10.1016/j.bmcl.2006.11.034
CHEMBL239775 181894 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 557 5 2 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCc2[nH]cnc2C1 10.1016/j.bmcl.2006.11.034
44294503 370806 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 570 11 2 7 8.1 CCc1sc(CCc2cc(OC3CCCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL49461 370806 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 570 11 2 7 8.1 CCc1sc(CCc2cc(OC3CCCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
44377452 238837 0 None None None Human 4.5 pIC50 = 4.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(CNC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL351508 238837 0 None None None Human 4.5 pIC50 = 4.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(CNC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL187399 139395 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 586 9 4 9 4.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL187925 139512 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 631 10 4 10 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3SC)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
CHEMBL189412 139776 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 610 9 4 10 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C#N)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
16132350 484239 20 None None None Human 8.5 pIC50 = 8.5 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm000052z
CHEMBL267633 484239 20 None None None Human 8.5 pIC50 = 8.5 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm000052z
3474 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
5311023 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
CHEMBL332347 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
3474 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
44294383 370034 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 592 13 2 7 8.0 CCc1sc(CCc2cc(OCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL48897 370034 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 592 13 2 7 8.0 CCc1sc(CCc2cc(OCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
62706262 157269 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1 10.1021/ml200265m
CHEMBL2046870 157269 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1 10.1021/ml200265m
CHEMBL187492 139417 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 629 9 4 8 5.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C(F)(F)F)CC2)c1 10.1016/j.bmcl.2004.10.005
44294672 370114 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 516 11 2 7 6.8 CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL48947 370114 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 516 11 2 7 6.8 CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
44409177 330694 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 5 0 6 5.0 CN1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL424862 330694 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 5 0 6 5.0 CN1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.11.104
44409330 158409 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 7 1 6 5.2 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCNCC1 10.1016/j.bmcl.2005.11.104
CHEMBL206799 158409 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 7 1 6 5.2 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCNCC1 10.1016/j.bmcl.2005.11.104
44409236 157235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 519 7 0 5 6.7 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCCCC1 10.1016/j.bmcl.2005.11.104
CHEMBL204583 157235 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 519 7 0 5 6.7 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCCCC1 10.1016/j.bmcl.2005.11.104
44294315 367689 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 14 2 7 8.0 CCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL48456 367689 0 None None None Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 14 2 7 8.0 CCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL266077 486185 0 None None None Human 4.5 pIC50 = 4.5 Binding
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
ChEMBL 1674 54 25 22 -6.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1016/S0960-894X(00)80696-4
44377731 120238 0 None None None Human 4.5 pIC50 = 4.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 507 8 2 5 4.1 COc1ccc2c(c1)CC(NC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL165506 120238 0 None None None Human 4.5 pIC50 = 4.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 507 8 2 5 4.1 COc1ccc2c(c1)CC(NC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
131886627 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
155524657 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
85472343 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL4456247 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL4475071 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL4577373 335533 0 None None None Human 6.4 pIC50 = 6.4 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
44409367 277614 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 536 7 2 7 4.0 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCN(CCO)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL380654 277614 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 536 7 2 7 4.0 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCN(CCO)CC1 10.1016/j.bmcl.2005.11.104
44409173 156695 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 5 1 6 4.1 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1=O 10.1016/j.bmcl.2005.11.104
CHEMBL203430 156695 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 520 5 1 6 4.1 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1=O 10.1016/j.bmcl.2005.11.104
CHEMBL414482 488344 0 None None None Human 7.4 pIC50 = 7.4 Binding
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
ChEMBL 1700 53 25 22 -5.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C1CCCCC1 10.1016/S0960-894X(00)80696-4
CHEMBL189548 139796 0 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 615 10 3 10 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCCN2CCN(c3cccc(OC)c3)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
9931301 465360 0 None None None Human 7.4 pIC50 = 7.4 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1The compound was tested for the binding affinity against Neuropeptide Y receptor type 1
ChEMBL 408 7 0 4 5.3 CC[C@H]1CC[C@@](c2cccc(OCOC)c2)(N2CCN(c3ccccc3)CC2)CC1 10.1021/jm980521l
CHEMBL60737 465360 0 None None None Human 7.4 pIC50 = 7.4 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1The compound was tested for the binding affinity against Neuropeptide Y receptor type 1
ChEMBL 408 7 0 4 5.3 CC[C@H]1CC[C@@](c2cccc(OCOC)c2)(N2CCN(c3ccccc3)CC2)CC1 10.1021/jm980521l
CHEMBL410938 488146 0 None None None Human 6.4 pIC50 = 6.4 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2003 62 30 26 -8.2 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL187491 139416 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 575 9 4 8 4.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL187620 139444 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 615 10 4 10 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3OC)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
44396885 139635 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 630 10 4 11 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
CHEMBL188576 139635 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 630 10 4 11 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
CHEMBL361273 241725 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 599 9 4 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
14160 1380 35 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cellsBinding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00765-x
9960164 1380 35 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cellsBinding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00765-x
CHEMBL2046866 1380 35 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cellsBinding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00765-x
CHEMBL324554 1380 35 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cellsBinding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00765-x
127041327 274545 0 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None None None Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
45487432 394083 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 455 9 1 9 4.0 COCc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
CHEMBL566663 394083 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 455 9 1 9 4.0 COCc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1 10.1016/j.bmcl.2009.07.030
10053818 375566 0 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 572 11 2 8 7.0 CCc1sc(CCc2cc(OC3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL52108 375566 0 None None None Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 572 11 2 8 7.0 CCc1sc(CCc2cc(OC3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
71456264 160982 0 None None None Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 570 14 2 7 8.2 CC/C=C\CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL2113710 160982 0 None None None Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 570 14 2 7 8.2 CC/C=C\CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
16133800 1450 36 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cellsDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells
ChEMBL 1619 51 23 21 -6.8 CSCC[C@@H](C(=O)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1nc[nH]c1)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CCC(=O)N1)CCC(=O)N)CCCNC(=N)N)CC(C)C)CC(=O)N)CCC(=O)N)C)CC(C)C 10.1016/j.bmcl.2012.11.110
616 1450 36 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cellsDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells
ChEMBL 1619 51 23 21 -6.8 CSCC[C@@H](C(=O)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1nc[nH]c1)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CCC(=O)N1)CCC(=O)N)CCCNC(=N)N)CC(C)C)CC(=O)N)CCC(=O)N)C)CC(C)C 10.1016/j.bmcl.2012.11.110
CHEMBL437027 1450 36 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cellsDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells
ChEMBL 1619 51 23 21 -6.8 CSCC[C@@H](C(=O)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1nc[nH]c1)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CCC(=O)N1)CCC(=O)N)CCCNC(=N)N)CC(C)C)CC(=O)N)CCC(=O)N)C)CC(C)C 10.1016/j.bmcl.2012.11.110
DB11724 1450 36 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cellsDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells
ChEMBL 1619 51 23 21 -6.8 CSCC[C@@H](C(=O)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1nc[nH]c1)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CCC(=O)N1)CCC(=O)N)CCCNC(=N)N)CC(C)C)CC(=O)N)CCC(=O)N)C)CC(C)C 10.1016/j.bmcl.2012.11.110
72714999 181840 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4ccccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397201 181840 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4ccccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
73353531 181842 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 379 5 0 6 3.0 CCOc1cccc(C2(N3CCN(c4ncncn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397293 181842 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 379 5 0 6 3.0 CCOc1cccc(C2(N3CCN(c4ncncn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
44439438 333527 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 532 5 1 5 5.8 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2=C(F)CNCC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL438342 333527 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 532 5 1 5 5.8 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2=C(F)CNCC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL331578 232370 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 568 9 3 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(NC(=O)NCCCN2CCN(C3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00765-x
44409234 278178 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL382204 278178 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
73350550 181843 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cccnn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397294 181843 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cccnn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL415176 488388 0 None None None Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
ChEMBL 1700 53 25 22 -5.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C1CCCCC1 10.1016/S0960-894X(00)80696-4
CHEMBL262221 486048 0 None None None Human 6.4 pIC50 = 6.4 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1990 63 28 25 -7.0 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)C(c1ccccc1)c1ccccc1 10.1021/jm000052z
62706423 157260 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 346 3 0 2 4.7 Cc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1 10.1021/ml200265m
CHEMBL2046860 157260 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 346 3 0 2 4.7 Cc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1 10.1021/ml200265m
44439456 181386 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 6 1 5 6.0 CN(C)C1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)C1 10.1016/j.bmcl.2006.11.034
CHEMBL238736 181386 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 6 1 5 6.0 CN(C)C1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)C1 10.1016/j.bmcl.2006.11.034
CHEMBL2111764 485079 0 None None None Human 7.3 pIC50 = 7.3 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2003 62 30 26 -8.2 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL427594 488474 0 None None None Human 7.3 pIC50 = 7.3 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2006 64 29 26 -7.7 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
44409345 158397 1 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44409363 158397 1 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL206723 158397 1 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL439506 158397 1 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
155517347 334755 0 None None None Human 6.3 pIC50 = 6.3 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1703 54 30 22 -4.3 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)C/C=C\C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
155557900 334755 0 None None None Human 6.3 pIC50 = 6.3 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1703 54 30 22 -4.3 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)C/C=C\C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL4445077 334755 0 None None None Human 6.3 pIC50 = 6.3 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1703 54 30 22 -4.3 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)C/C=C\C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL4559081 334755 0 None None None Human 6.3 pIC50 = 6.3 Binding
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
ChEMBL 1703 54 30 22 -4.3 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)C/C=C\C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00310
CHEMBL362083 251743 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 607 10 4 9 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3SC)CC2)c1 10.1016/j.bmcl.2004.10.005
CHEMBL364380 253061 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 601 9 5 10 3.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3O)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
45487514 424981 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccnc(F)c3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL584908 424981 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccnc(F)c3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL113935 24128 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 584 9 3 8 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCCN2CCC(c3ccccc3)CC2)NC#N)c1 10.1016/s0960-894x(01)00765-x
11757487 372505 0 None None None Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 13 2 7 8.0 CCc1sc(CCc2cc(OC(CC)CC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL51284 372505 0 None None None Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 13 2 7 8.0 CCc1sc(CCc2cc(OC(CC)CC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
1485 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
21129772 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
5311023 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
9869458 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL2440929 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL332347 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
CHEMBL44246 1304 7 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(00)00292-4
44439440 181892 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 544 7 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL239773 181892 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 544 7 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.11.034
44439485 310446 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 522 8 2 5 5.5 CN(C)CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
CHEMBL398782 310446 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 522 8 2 5 5.5 CN(C)CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F 10.1016/j.bmcl.2006.11.034
73348990 181845 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cncnc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397296 181845 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cncnc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
44439432 182343 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL240404 182343 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@@H]2F)CC1 10.1016/j.bmcl.2006.11.034
44439434 289765 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL392787 289765 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)CC1 10.1016/j.bmcl.2006.11.034
44288395 318059 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
CHEMBL41686 318059 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
72715000 181841 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4ncccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397291 181841 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4ncccn4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
44294516 329914 0 None None None Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 11 2 7 7.8 CCc1sc(CCc2cc(OCC(C)(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL422583 329914 0 None None None Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 558 11 2 7 7.8 CCc1sc(CCc2cc(OCC(C)(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
62706425 157262 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1 10.1021/ml200265m
CHEMBL2046862 157262 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 362 4 0 3 4.4 COc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1 10.1021/ml200265m
CHEMBL116230 24666 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 591 10 3 9 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(NC(=O)NCCCN2CCC(c3cccc(OC)c3)CC2)c1 10.1016/s0960-894x(01)00765-x
CHEMBL360205 241173 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 577 9 5 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3O)CC2)c1 10.1016/j.bmcl.2004.10.005
44294564 372513 0 None None None Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 607 14 2 8 7.8 CCc1sc(CCc2cc(OCCCc3cccnc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL51290 372513 0 None None None Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 607 14 2 8 7.8 CCc1sc(CCc2cc(OCCCc3cccnc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
20556258 136102 0 None None None Human 4.2 pIC50 = 4.2 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 419 4 1 7 2.9 COc1cc2nc(N3CCC(N4Cc5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
CHEMBL18016 136102 0 None None None Human 4.2 pIC50 = 4.2 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 419 4 1 7 2.9 COc1cc2nc(N3CCC(N4Cc5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
73353533 174422 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 376 5 0 3 4.8 CCOc1cccc(C2(N3CCN(c4ccccc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397299 174422 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 376 5 0 3 4.8 CCOc1cccc(C2(N3CCN(c4ccccc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
57384007 157266 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 376 5 0 3 4.8 CCOc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1 10.1021/ml200265m
CHEMBL2046867 157266 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 376 5 0 3 4.8 CCOc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1 10.1021/ml200265m
44294543 372663 0 None None None Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 572 15 2 7 8.4 CCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL51422 372663 0 None None None Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 572 15 2 7 8.4 CCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
44409307 158389 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 533 7 0 5 7.0 CC1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL206671 158389 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 533 7 0 5 7.0 CC1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44288067 331185 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL42747 331185 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL425095 488451 0 None None None Human 6.2 pIC50 = 6.2 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1848 60 27 24 -8.5 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
127041619 274547 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487512 394211 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccnc3F)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL567708 394211 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccnc3F)n2)oc1C 10.1016/j.bmcl.2009.07.030
44294626 367931 0 None None None Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 586 16 2 7 8.8 CCCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
CHEMBL48493 367931 0 None None None Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 586 16 2 7 8.8 CCCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1 10.1016/j.bmcl.2004.01.049
44409209 158195 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 436 6 0 4 6.3 O=C1CC[C@@H](Oc2ccc(Cl)cc2)c2c1c1ccccc1n2CCCN1CCCCC1 10.1016/j.bmcl.2005.11.104
CHEMBL206112 158195 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 436 6 0 4 6.3 O=C1CC[C@@H](Oc2ccc(Cl)cc2)c2c1c1ccccc1n2CCCN1CCCCC1 10.1016/j.bmcl.2005.11.104
16146616 331533 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
44342628 331533 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
91931428 331533 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
CHEMBL428292 331533 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
CHEMBL2314835 477550 0 None None None Human 7.1 pIC50 = 7.1 Binding
Binding affinity to Y1 receptor in human SK-N-MC cellsBinding affinity to Y1 receptor in human SK-N-MC cells
ChEMBL 3239 107 40 46 -9.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)[C@H](CCCCNC(=O)COCC(=O)NCCOCCOCC(=O)NCC(=O)Nc1ccc(C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)cc1)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2012.11.110
CHEMBL428320 488512 0 None None None Human 7.1 pIC50 = 7.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1953 62 29 25 -8.1 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL438935 488757 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 2002 62 29 25 -6.0 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
CHEMBL413612 488290 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1914 62 28 25 -8.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
16148366 333943 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CN[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
44342930 333943 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CN[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
91931417 333943 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CN[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
CHEMBL441936 333943 0 None None None Human 6.1 pIC50 = 6.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CN[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/jm000052z
44409345 158397 1 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44409363 158397 1 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL206723 158397 1 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL439506 158397 1 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44439445 181121 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 535 5 2 5 5.8 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCC(O)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL238527 181121 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 535 5 2 5 5.8 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCC(O)CC1 10.1016/j.bmcl.2006.11.034
10030299 372365 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
45487501 394037 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 477 7 1 9 3.4 Cc1nc(SCc2cc(N3CCS(=O)(=O)CC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL566441 394037 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
ChEMBL 477 7 1 9 3.4 Cc1nc(SCc2cc(N3CCS(=O)(=O)CC3)cc(NCc3cccc(F)n3)n2)oc1C 10.1016/j.bmcl.2009.07.030
CHEMBL187490 139415 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 619 9 4 9 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3cccc(Cl)c3)CC2)NC#N)c1 10.1016/j.bmcl.2004.10.005
CHEMBL360188 241151 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
ChEMBL 595 9 4 8 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2004.10.005
10008757 372175 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None None None Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44294458 328151 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 560 13 2 8 6.8 CCc1sc(CCc2cc(OC(C)COC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
CHEMBL417912 328151 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
ChEMBL 560 13 2 8 6.8 CCc1sc(CCc2cc(OC(C)COC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C 10.1016/j.bmcl.2004.01.049
3474 7886 30 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/np900287e
5311023 7886 30 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/np900287e
CHEMBL332347 7886 30 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/np900287e
CHEMBL2314835 477550 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 3239 107 40 46 -9.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)[C@H](CCCCNC(=O)COCC(=O)NCCOCCOCC(=O)NCC(=O)Nc1ccc(C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)cc1)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2012.11.110
44271463 123099 0 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 307 6 3 5 3.0 NCCCCNc1nc(N)c2cc(-c3ccccc3)ccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL17441 123099 0 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 307 6 3 5 3.0 NCCCCNc1nc(N)c2cc(-c3ccccc3)ccc2n1 10.1016/s0960-894x(00)00177-3
44439441 310876 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 564 7 2 6 4.9 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CCO)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL400631 310876 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 564 7 2 6 4.9 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CCO)CC1 10.1016/j.bmcl.2006.11.034
1562 1855 11 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for human Neuropeptide Y receptor type 1Compound was tested for human Neuropeptide Y receptor type 1
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
5312114 1855 11 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for human Neuropeptide Y receptor type 1Compound was tested for human Neuropeptide Y receptor type 1
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL17645 1855 11 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for human Neuropeptide Y receptor type 1Compound was tested for human Neuropeptide Y receptor type 1
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL195380 1855 11 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for human Neuropeptide Y receptor type 1Compound was tested for human Neuropeptide Y receptor type 1
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
44377468 119299 0 None None None Human 5.1 pIC50 = 5.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 525 8 2 4 5.0 O=S(=O)(NCCN1CCC(CNC2CCCc3ccc(Cl)cc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL163470 119299 0 None None None Human 5.1 pIC50 = 5.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 525 8 2 4 5.0 O=S(=O)(NCCN1CCC(CNC2CCCc3ccc(Cl)cc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
44439446 181379 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 560 6 1 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F)N1CCN(C2CC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL238733 181379 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 560 6 1 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F)N1CCN(C2CC2)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL429698 488556 0 None None None Human 7.1 pIC50 = 7.1 Binding
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
ChEMBL 1964 62 28 25 -7.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/jm000052z
12822578 123122 0 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 481 5 1 8 3.5 COc1cc2nc(N3CCC(N4C(=O)CC(C5CCCCC5)CC4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
CHEMBL17456 123122 0 None None None Human 5.1 pIC50 = 5.1 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
ChEMBL 481 5 1 8 3.5 COc1cc2nc(N3CCC(N4C(=O)CC(C5CCCCC5)CC4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
73353532 181844 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4cccnc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2397295 181844 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
ChEMBL 377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4cccnc4)CC3)C3CC(C)CC32)c1 10.1016/j.bmcl.2013.04.095
CHEMBL2314836 477551 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
ChEMBL 1607 47 22 23 -5.7 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)CC1)C(=O)O 10.1016/j.bmcl.2012.11.110
44409340 157621 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 534 6 1 6 5.4 CNC1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL205261 157621 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 534 6 1 6 5.4 CNC1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL265766 197223 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
ChEMBL 607 10 3 9 5.7 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(S)=N/CCCN2CCC(c3cccc(OC)c3)CC2)c1 10.1016/s0960-894x(01)00765-x
44439435 181336 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@H]2F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL238728 181336 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@H]2F)CC1 10.1016/j.bmcl.2006.11.034
10007341 238753 4 None None None Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL350620 238753 4 None None None Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
10007341 238753 4 None None None Human 5.0 pIC50 = 5.0 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL350620 238753 4 None None None Human 5.0 pIC50 = 5.0 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44409121 157079 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44409155 157079 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL204050 157079 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL382836 157079 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1 10.1016/j.bmcl.2005.11.104
44439442 181893 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 602 6 1 5 6.5 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CC(F)(F)F)CC1 10.1016/j.bmcl.2006.11.034
CHEMBL239774 181893 0 None None None Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
ChEMBL 602 6 1 5 6.5 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CC(F)(F)F)CC1 10.1016/j.bmcl.2006.11.034
127041619 274547 0 None None None Human 10.6 pKd = 10.6 Binding
Binding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constantBinding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constant
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.6 pKd = 10.6 Binding
Binding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constantBinding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constant
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.4 pKd = 10.4 Binding
Binding affinity to NPY1R in human SK-N-MC cellsBinding affinity to NPY1R in human SK-N-MC cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.4 pKd = 10.4 Binding
Binding affinity to NPY1R in human SK-N-MC cellsBinding affinity to NPY1R in human SK-N-MC cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.4 pKd = 10.4 Binding
Binding affinity to NPY1R in human SK-N-MC cells after 90 minsBinding affinity to NPY1R in human SK-N-MC cells after 90 mins
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.4 pKd = 10.4 Binding
Binding affinity to NPY1R in human SK-N-MC cells after 90 minsBinding affinity to NPY1R in human SK-N-MC cells after 90 mins
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.3 pKd = 10.3 Binding
Binding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysisBinding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.3 pKd = 10.3 Binding
Binding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysisBinding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.1 pKd = 10.1 Binding
Binding affinity to NPY1R in human MCF7 cellsBinding affinity to NPY1R in human MCF7 cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.1 pKd = 10.1 Binding
Binding affinity to NPY1R in human MCF7 cellsBinding affinity to NPY1R in human MCF7 cells
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 10.1 pKd = 10.1 Binding
Binding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysisBinding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 10.1 pKd = 10.1 Binding
Binding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysisBinding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None None None Human 9.9 pKd = 9.9 Binding
Binding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysisBinding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None None None Human 9.9 pKd = 9.9 Binding
Binding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysisBinding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
25181112 352856 0 None None None Human 9.0 pKd = 9.0 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experiment
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 9.0 pKd = 9.0 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experiment
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
25181112 352856 0 None None None Human 9.0 pKd = 9.0 Binding
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experiment
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 9.0 pKd = 9.0 Binding
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experiment
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
25181112 352856 0 None None None Human 8.9 pKd = 8.9 Binding
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cellsBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 8.9 pKd = 8.9 Binding
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cellsBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
25181112 352856 0 None None None Human 8.9 pKd = 8.9 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 8.9 pKd = 8.9 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
44346892 317435 0 None None None Human 7.0 pKd = 7 Binding
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
ChEMBL 3395 75 48 47 -15.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@]1(C)NC(=O)CC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm00098a009
91928654 317435 0 None None None Human 7.0 pKd = 7 Binding
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
ChEMBL 3395 75 48 47 -15.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@]1(C)NC(=O)CC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm00098a009
CHEMBL415353 317435 0 None None None Human 7.0 pKd = 7 Binding
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
ChEMBL 3395 75 48 47 -15.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@]1(C)NC(=O)CC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm00098a009
CHEMBL3559527 487132 0 None -112 2 Human 7.0 pKd = 7 Binding
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
ChEMBL 3536 105 51 48 -13.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00098a009
127042586 274416 2 None None None Human 8.7 pKd = 8.7 Binding
Binding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assay
ChEMBL 643 17 7 5 3.0 CCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746028 274416 2 None None None Human 8.7 pKd = 8.7 Binding
Binding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assay
ChEMBL 643 17 7 5 3.0 CCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
3474 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
25181112 352856 0 None None None Human 8.5 pKd = 8.5 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 8.5 pKd = 8.5 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
52953220 125869 0 None None None Human 8.3 pKd = 8.3 Binding
Binding affinity at Y1R in human MCF-7 cells by flow cytometryBinding affinity at Y1R in human MCF-7 cells by flow cytometry
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789732 125869 0 None None None Human 8.3 pKd = 8.3 Binding
Binding affinity at Y1R in human MCF-7 cells by flow cytometryBinding affinity at Y1R in human MCF-7 cells by flow cytometry
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL409167 488048 5 None -426 2 Human 6.1 pKd = 6.1 Binding
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
ChEMBL 2455 78 37 33 -9.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00098a009
162647593 366972 0 None None None Human 10.5 pKi = 10.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802520 366972 0 None None None Human 10.5 pKi = 10.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
10008757 372175 0 None 7585 2 Human 10.4 pKi = 10.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 10.4 pKi = 10.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
9987422 238617 0 None None None Human 10.3 pKi = 10.3 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 720 15 0 6 8.2 Ic1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL349328 238617 0 None None None Human 10.3 pKi = 10.3 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 720 15 0 6 8.2 Ic1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
162673313 367104 0 None None None Human 10.3 pKi = 10.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803933 367104 0 None None None Human 10.3 pKi = 10.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162646865 366968 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 601 14 7 5 1.9 CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802480 366968 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 601 14 7 5 1.9 CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
10008757 372175 0 None 7585 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10030299 372365 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
162659769 367034 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803176 367034 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162645700 366963 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802419 366963 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL2110365 484200 1 None 17 4 Human 10.2 pKi = 10.2 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2351 58 32 30 -7.6 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
162652126 366989 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802763 366989 0 None None None Human 10.2 pKi = 10.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162652761 366995 0 None None None Human 10.1 pKi = 10.1 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 629 16 7 5 2.6 CCC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802798 366995 0 None None None Human 10.1 pKi = 10.1 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 629 16 7 5 2.6 CCC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
127041619 274547 0 None 6456 2 Human 10.1 pKi = 10.1 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None 6456 2 Human 10.1 pKi = 10.1 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
1504 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
44288922 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
CHEMBL438945 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P01303 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P07808 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
P57774 5725 8 None -6 9 Human 10.0 pKi = 10.0 Binding
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.ejmech.2013.01.044
10008757 372175 0 None 7585 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL508974 372175 0 None 7585 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
10030299 372365 0 None None None Human 10.0 pKi = 10 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL511460 372365 0 None None None Human 10.0 pKi = 10 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
127041619 274547 0 None 6456 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None 6456 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44372750 101950 0 None None None Human 10.0 pKi = 10.0 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 615 16 0 7 7.2 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CCCN3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL155802 101950 0 None None None Human 10.0 pKi = 10.0 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 615 16 0 7 7.2 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CCCN3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
44372384 238467 0 None None None Human 10.0 pKi = 10.0 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 622 16 0 7 7.6 O=C(CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1)c1ccccc1 10.1016/s0960-894x(99)00082-7
CHEMBL347807 238467 0 None None None Human 10.0 pKi = 10.0 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 622 16 0 7 7.6 O=C(CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1)c1ccccc1 10.1016/s0960-894x(99)00082-7
162653845 367001 0 None None None Human 10.0 pKi = 10.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802860 367001 0 None None None Human 10.0 pKi = 10.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
16132350 484239 20 None -13 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to Y1 (unknown origin) assessed as inhibition constantBinding affinity to Y1 (unknown origin) assessed as inhibition constant
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acschembio.7b00481
CHEMBL267633 484239 20 None -13 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to Y1 (unknown origin) assessed as inhibition constantBinding affinity to Y1 (unknown origin) assessed as inhibition constant
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acschembio.7b00481
10008757 372175 0 None 7585 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
16132350 484239 20 None -13 2 Human 9.9 pKi = 9.9 Binding
Displacement of radiolabeled NPY from human neuropeptide Y1 receptorDisplacement of radiolabeled NPY from human neuropeptide Y1 receptor
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL267633 484239 20 None -13 2 Human 9.9 pKi = 9.9 Binding
Displacement of radiolabeled NPY from human neuropeptide Y1 receptorDisplacement of radiolabeled NPY from human neuropeptide Y1 receptor
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL4281479 478156 6 None 1 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4308 134 63 59 -15.8 CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
162667448 367070 0 None None None Human 9.9 pKi = 9.9 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803593 367070 0 None None None Human 9.9 pKi = 9.9 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4281479 478156 6 None 1 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4308 134 63 59 -15.8 CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
44372383 333675 0 None None None Human 9.9 pKi = 9.9 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 636 17 0 7 8.0 O=C(CCCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1)c1ccccc1 10.1016/s0960-894x(99)00082-7
CHEMBL439643 333675 0 None None None Human 9.9 pKi = 9.9 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 636 17 0 7 8.0 O=C(CCCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1)c1ccccc1 10.1016/s0960-894x(99)00082-7
162675643 367117 0 None None None Human 9.8 pKi = 9.8 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4804067 367117 0 None None None Human 9.8 pKi = 9.8 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
10030299 372365 0 None None None Human 9.8 pKi = 9.8 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.8 pKi = 9.8 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44372422 238330 0 None None None Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 606 15 0 6 8.1 C(=C\c1ccccc1)\CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL346243 238330 0 None None None Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 606 15 0 6 8.1 C(=C\c1ccccc1)\CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
44372692 238262 0 None None None Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 594 15 0 6 7.6 c1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL345581 238262 0 None None None Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 594 15 0 6 7.6 c1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
1504 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
44288922 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
CHEMBL438945 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P01303 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P07808 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
P57774 5725 8 None -6 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1016/j.bmcl.2013.01.025
10008757 372175 0 None 7585 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041619 274547 0 None 6456 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None 6456 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
162653308 366999 0 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802829 366999 0 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
10030299 372365 0 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in human HEL cells preincubated for 30 mins followed by radioligand addition at 60 to 90 mins by flow cytometric analysis
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL4284905 478177 0 None 1 4 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4270 132 63 60 -17.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
1528 1302 21 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.1016/j.bmc.2011.03.045
5311022 1302 21 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.1016/j.bmc.2011.03.045
6324607 1302 21 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.1016/j.bmc.2011.03.045
CHEMBL1774204 1302 21 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.1016/j.bmc.2011.03.045
CHEMBL5315638 1302 21 None None None Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 529 13 6 4 1.8 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)CNC(=O)N 10.1016/j.bmc.2011.03.045
CHEMBL4284905 478177 0 None 1 4 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4270 132 63 60 -17.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
155523949 335403 0 None 676 2 Human 9.6 pKi = 9.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2259 56 35 29 -7.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4454036 335403 0 None 676 2 Human 9.6 pKi = 9.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2259 56 35 29 -7.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL411117 488156 0 None 123 4 Human 9.6 pKi = 9.6 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2381 58 30 32 -6.2 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(=O)OC)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(=O)OC)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
155537755 336883 0 None 467 2 Human 9.6 pKi = 9.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2309 56 36 30 -7.8 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4476074 336883 0 None 467 2 Human 9.6 pKi = 9.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2309 56 36 30 -7.8 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
10008757 372175 0 None 7585 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44372776 102251 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 600 15 0 6 8.3 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CCC3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL156076 102251 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 600 15 0 6 8.3 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CCC3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
44373119 238501 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 560 15 0 6 7.4 CC(C)CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL348123 238501 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 560 15 0 6 7.4 CC(C)CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
10030299 372365 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assayDisplacement of [3H]propionyl-pNPY from NPY1R in human SK-N-MC cells compound treated immediately post radioligand treatment measured after 2 hrs by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
127041306 274475 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None 7585 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
162655600 367010 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802951 367010 0 None None None Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
127041619 274547 0 None 6456 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 274547 0 None 6456 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44372508 238781 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 610 15 1 7 7.3 Oc1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL350917 238781 0 None None None Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 610 15 1 7 7.3 Oc1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
127041327 274545 0 None 1445 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None 1445 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
44372691 238329 0 None None None Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 608 16 0 6 8.0 c1ccc(CCCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL346242 238329 0 None None None Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 608 16 0 6 8.0 c1ccc(CCCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1 10.1016/s0960-894x(99)00082-7
155517812 334768 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2266 54 33 29 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4445317 334768 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2266 54 33 29 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
162672910 367103 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803913 367103 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44372858 238500 0 None None None Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 586 14 0 6 7.9 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CC3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL348119 238500 0 None None None Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 586 14 0 6 7.9 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCN(CC3CCCCC3)CC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL4279973 478145 0 None -2 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279973 478145 0 None -2 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10030299 372365 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL511460 372365 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL4299523 478252 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 4251 131 63 59 -17.8 CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC 10.1021/acs.jmedchem.5b00925
CHEMBL4299523 478252 0 None None None Human 9.4 pKi = 9.4 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assay
ChEMBL 4251 131 63 59 -17.8 CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC 10.1021/acs.jmedchem.5b00925
10008757 372175 0 None 7585 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 372175 0 None 7585 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44283050 315324 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
91931647 315324 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
CHEMBL410166 315324 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
127041306 274475 0 None None None Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746870 274475 0 None None None Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
1504 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
44288922 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
CHEMBL438945 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
P01303 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
P07808 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
P57774 5725 8 None -6 9 Human 9.3 pKi = 9.3 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 10.1021/jm4008505
16132350 484239 20 None -13 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm801018u
CHEMBL267633 484239 20 None -13 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm801018u
CHEMBL429531 488552 17 None -6 4 Human 9.3 pKi = 9.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 4220 127 57 58 -17.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm010031k
127041327 274545 0 None 1445 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 274545 0 None 1445 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
155541756 347153 0 None 426 2 Human 9.2 pKi = 9.2 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2266 54 33 29 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4519035 347153 0 None 426 2 Human 9.2 pKi = 9.2 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2266 54 33 29 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4299523 478252 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 4251 131 63 59 -17.8 CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC 10.1021/acs.jmedchem.5b00925
162669845 367081 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803729 367081 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4299523 478252 0 None None None Human 9.2 pKi = 9.2 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 4251 131 63 59 -17.8 CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC 10.1021/acs.jmedchem.5b00925
44373122 333063 0 None None None Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 544 15 0 6 6.9 C=CCCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL434467 333063 0 None None None Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 544 15 0 6 6.9 C=CCCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
10326097 104033 0 None None None Human 9.1 pKi = 9.1 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCCC2CCCNC2)c2ccccc12 10.1016/s0960-894x(99)00082-7
CHEMBL157661 104033 0 None None None Human 9.1 pKi = 9.1 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCCC2CCCNC2)c2ccccc12 10.1016/s0960-894x(99)00082-7
9916525 213053 1 None None None Human 9.1 pKi = 9.1 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
CHEMBL329536 213053 1 None None None Human 9.1 pKi = 9.1 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
9916525 213053 1 None None None Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm9706630
CHEMBL329536 213053 1 None None None Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@@H]2CCCNC2)c2ccccc12 10.1021/jm9706630
CHEMBL4286615 478186 0 None -79 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4239 132 59 58 -16.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 478186 0 None -79 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4239 132 59 58 -16.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
44373166 105775 0 None None None Human 9.1 pKi = 9.1 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 546 14 0 6 7.0 CC(C)CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL159220 105775 0 None None None Human 9.1 pKi = 9.1 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 546 14 0 6 7.0 CC(C)CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL3349022 484266 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
46934142 40038 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 643 18 6 7 4.3 COC(=O)CCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1223992 40038 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 643 18 6 7 4.3 COC(=O)CCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
3474 7886 30 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
9869041 124402 12 None 3 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771259 124402 12 None 3 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
25181112 352856 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 9.0 pKi = 9 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL2110365 484200 1 None 17 4 Human 9.0 pKi = 9.0 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2351 58 32 30 -7.6 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)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)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
162659745 367033 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803174 367033 0 None None None Human 9.0 pKi = 9.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162649085 366976 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802600 366976 0 None None None Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL3349022 484266 0 None -3 2 Human 8.9 pKi = 8.9 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
25181112 352856 0 None None None Human 8.9 pKi = 8.9 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470495 352856 0 None None None Human 8.9 pKi = 8.9 Binding
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
ChEMBL 529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
3474 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2008.09.033
5311023 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2008.09.033
CHEMBL332347 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2008.09.033
3474 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
5311023 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
CHEMBL332347 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
3474 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2010.07.028
5311023 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2010.07.028
CHEMBL332347 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2010.07.028
3474 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2013.08.065
5311023 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2013.08.065
CHEMBL332347 7886 30 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2013.08.065
10531484 231955 0 None None None Human 8.9 pKi = 8.9 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
CHEMBL331937 231955 0 None None None Human 8.9 pKi = 8.9 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 590 11 1 6 6.8 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC[C@H]2CCCNC2)c2ccccc12 10.1021/jm970512x
CHEMBL3349022 484266 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
3474 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
5311023 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
CHEMBL332347 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
3474 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
3474 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 7886 30 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysisDisplacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL3349022 484266 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
44372820 104895 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 532 13 0 6 6.8 CC(C)N1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL158392 104895 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 532 13 0 6 6.8 CC(C)N1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
44372775 102099 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 504 12 0 6 6.0 CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL155925 102099 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 504 12 0 6 6.0 CN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
44372777 238466 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 530 14 0 6 6.5 C=CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL347804 238466 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 530 14 0 6 6.5 C=CCN1CCC(CCCn2c(COc3ccccc3)nc3c(OCCCN4CCCCC4)cccc32)CC1 10.1016/s0960-894x(99)00082-7
10414488 466724 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL61532 466724 0 None None None Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1016/s0960-894x(99)00082-7
10414488 466724 0 None None None Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL61532 466724 0 None None None Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL3349022 484266 0 None -3 2 Human 8.7 pKi = 8.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL3349022 484266 0 None -3 2 Human 8.7 pKi = 8.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
10555187 236804 0 None None None Human 8.7 pKi = 8.7 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 576 10 1 6 6.4 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC2CCNCC2)c2ccccc12 10.1021/jm970512x
CHEMBL340369 236804 0 None None None Human 8.7 pKi = 8.7 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 576 10 1 6 6.4 O=C(CN1CCC(N2CCCCC2)CC1)c1c(COc2ccc(Cl)cc2)n(CCC2CCNCC2)c2ccccc12 10.1021/jm970512x
45273656 391922 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 529 6 1 3 6.0 Cc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL558133 391922 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 529 6 1 3 6.0 Cc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL125807 41434 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 560 9 3 7 5.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3ccccc3)CC2)c1 10.1016/s0960-894x(01)00761-2
44409242 278599 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
CHEMBL383763 278599 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
ChEMBL 538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCN(C)C[C@@H]3F)C2=O)CC1 10.1016/j.bmcl.2005.11.104
54582376 125872 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1657 47 12 12 10.8 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
91932453 125872 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1657 47 12 12 10.8 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789739 125872 0 None None None Human 7.0 pKi = 7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1657 47 12 12 10.8 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10577912 473342 0 None None None Human 7.0 pKi = 7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cccc(F)c3F)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL87548 473342 0 None None None Human 7.0 pKi = 7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cccc(F)c3F)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL4277697 478133 0 None -25 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
73351127 202629 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 899 27 12 9 -0.8 NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040737 202629 0 None None None Human 6.0 pKi = 6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 899 27 12 9 -0.8 NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL4281120 478155 0 None -39 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4020 127 61 56 -17.0 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 478168 0 None -5011 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4135 130 62 56 -15.2 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290488 478204 0 None -19 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4048 129 60 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
162661557 367041 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 821 18 6 5 6.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803258 367041 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 821 18 6 5 6.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL338296 235765 0 None None None Human 7.0 pKi = 7.0 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 605 11 3 9 4.8 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
46879455 19821 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.8 Cc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1076207 19821 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.8 Cc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
46879823 20609 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1cccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)c1 10.1016/j.bmcl.2009.09.048
CHEMBL1081713 20609 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1cccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)c1 10.1016/j.bmcl.2009.09.048
CHEMBL124335 40632 0 None None None Human 7.0 pKi = 7.0 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 591 10 4 9 4.5 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3O)CC2)c1 10.1016/s0960-894x(01)00761-2
21188508 238191 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 487 9 0 4 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL344952 238191 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 487 9 0 4 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
44362830 239887 0 None None None Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 516 9 0 5 6.0 COCc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL357914 239887 0 None None None Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 516 9 0 5 6.0 COCc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
44362352 238143 0 None None None Human 8.0 pKi = 8.0 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 467 10 0 4 7.1 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCC(C)C)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL344530 238143 0 None None None Human 8.0 pKi = 8.0 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 467 10 0 4 7.1 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCC(C)C)CC1 10.1016/s0960-894x(98)00048-1
49865805 40039 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 861 21 6 15 2.0 CC(=O)OC[C@@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](OC(C)=O)C(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1223993 40039 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 861 21 6 15 2.0 CC(=O)OC[C@@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](OC(C)=O)C(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL2440916 477832 0 None 4 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1757 54 17 18 4.7 CCC(=O)NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040674 477832 0 None 4 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1757 54 17 18 4.7 CCC(=O)NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
45270992 393267 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccc([C@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL563052 393267 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccc([C@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
44362822 77886 0 None None None Human 5.0 pKi = 5.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 371 5 0 3 6.1 Clc1ccc(OCc2sc3ccccc3c2CN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
CHEMBL142796 77886 0 None None None Human 5.0 pKi = 5.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 371 5 0 3 6.1 Clc1ccc(OCc2sc3ccccc3c2CN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
46879457 20238 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 372 5 2 6 4.6 Fc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079610 20238 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 372 5 2 6 4.6 Fc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
15383697 201884 0 None None None Human 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 359 4 1 7 2.6 COc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
CHEMBL299965 201884 0 None None None Human 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 359 4 1 7 2.6 COc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
CHEMBL196546 143940 0 None None None Human 5.9 pKi = 5.9 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 633 10 3 9 5.6 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC(C)(C)C)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL269267 486290 0 None -13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cellsDisplacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cells
ChEMBL 1930 62 29 26 -8.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
19426761 387221 0 None None None Human 6.9 pKi = 6.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 343 3 1 6 2.9 Cc1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
CHEMBL53657 387221 0 None None None Human 6.9 pKi = 6.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 343 3 1 6 2.9 Cc1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
44563341 353152 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 515 11 5 4 2.6 CC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL472901 353152 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 515 11 5 4 2.6 CC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL124152 40508 0 None None None Human 7.9 pKi = 7.9 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 591 10 3 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL4287140 478188 0 None -8 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4017 125 59 55 -15.0 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
155565033 349537 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2407 58 36 30 -5.2 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4578617 349537 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2407 58 36 30 -5.2 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
44362411 77632 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 550 7 0 4 6.6 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142584 77632 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 550 7 0 4 6.6 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44362410 330151 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 422 7 0 4 5.7 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C)c1 10.1016/s0960-894x(99)00019-0
CHEMBL423012 330151 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 422 7 0 4 5.7 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C)c1 10.1016/s0960-894x(99)00019-0
CHEMBL2371910 477716 0 None -31 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1709 54 26 20 -4.2 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
45270142 390098 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 530 7 1 6 5.8 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4nnc(C)o4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL551608 390098 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 530 7 1 6 5.8 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4nnc(C)o4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
73354094 202616 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 971 30 13 10 -1.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
73357158 202616 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 971 30 13 10 -1.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040672 202616 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 971 30 13 10 -1.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040757 202616 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 971 30 13 10 -1.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
10720203 473357 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 5 3 4 5.7 CC(C)(C)OC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL87667 473357 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 5 3 4 5.7 CC(C)(C)OC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
44362998 239689 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 490 7 0 4 7.1 CN(C)C1CCN(CCc2c(C(C)(C)Oc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL357010 239689 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 490 7 0 4 7.1 CN(C)C1CCN(CCc2c(C(C)(C)Oc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10815605 473750 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 8 1 4 5.4 Clc1ccc(OCc2nc3ccccc3n2CCCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL90369 473750 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 8 1 4 5.4 Clc1ccc(OCc2nc3ccccc3n2CCCCC2CCCNC2)cc1 10.1021/jm9706630
46879822 20608 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1081712 20608 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
46879521 20397 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 388 5 2 6 5.1 Clc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1080617 20397 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 388 5 2 6 5.1 Clc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
44362921 329825 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 458 6 0 3 6.9 CN(C)C1CCN(CCc2c(/C=C/c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL422294 329825 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 458 6 0 3 6.9 CN(C)C1CCN(CCc2c(/C=C/c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44296729 201690 0 None None None Human 5.9 pKi = 5.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 328 3 2 6 2.5 Nc1ccc([S+]([O-])c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
CHEMBL298542 201690 0 None None None Human 5.9 pKi = 5.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 328 3 2 6 2.5 Nc1ccc([S+]([O-])c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
46879606 20290 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 398 6 2 7 4.9 COc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079917 20290 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 398 6 2 7 4.9 COc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL4289021 478196 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4034 128 61 56 -16.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294418 478222 0 None -1000 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2261 50 36 30 -6.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
44362626 80565 0 None None None Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 394 7 0 4 5.0 CN(C)C1CCN(CCc2c(COc3ccccc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145248 80565 0 None None None Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 394 7 0 4 5.0 CN(C)C1CCN(CCc2c(COc3ccccc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10692519 40352 0 None None None Human 5.9 pKi = 5.9 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 402 5 0 3 6.1 Cn1c(COc2ccc(Cl)cc2Cl)c(CN2CCCCC2)c2ccccc21 10.1021/jm970512x
CHEMBL123410 40352 0 None None None Human 5.9 pKi = 5.9 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 402 5 0 3 6.1 Cn1c(COc2ccc(Cl)cc2Cl)c(CN2CCCCC2)c2ccccc21 10.1021/jm970512x
44362766 238002 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 459 6 0 4 6.5 CN(C)C1CCN(CCc2c(/C=N/c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL343413 238002 0 None None None Human 4.9 pKi = 4.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 459 6 0 4 6.5 CN(C)C1CCN(CCc2c(/C=N/c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL592149 489310 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1221 38 18 15 -0.5 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2009.12.068
11799055 474124 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.7 Clc1ccc(OCc2nc3ccccc3n2CCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL92685 474124 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.7 Clc1ccc(OCc2nc3ccccc3n2CCC2CCCNC2)cc1 10.1021/jm9706630
19426753 372890 0 None None None Human 6.9 pKi = 6.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 357 4 1 6 3.1 CCc1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
CHEMBL51611 372890 0 None None None Human 6.9 pKi = 6.9 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 357 4 1 6 3.1 CCc1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
44324723 159892 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 794 14 2 8 10.7 Cc1ccc2c(c1)nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1.Cc1ccc2nc(COc3ccc(Cl)cc3)n(CCCC3CCCNC3)c2c1 10.1021/jm9706630
CHEMBL210900 159892 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 794 14 2 8 10.7 Cc1ccc2c(c1)nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1.Cc1ccc2nc(COc3ccc(Cl)cc3)n(CCCC3CCCNC3)c2c1 10.1021/jm9706630
21336507 372810 0 None -1288 2 Human 4.9 pKi = 4.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
CHEMBL51542 372810 0 None -1288 2 Human 4.9 pKi = 4.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
44363000 80180 0 None None None Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 497 7 0 5 5.7 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C#N)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL144935 80180 0 None None None Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 497 7 0 5 5.7 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C#N)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL4287140 478188 0 None -8 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4017 125 59 55 -15.0 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
54583330 125887 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 906 21 5 7 6.0 Cc1ccc(/C=C/c2cc3c4c(c2)CCCN4CCC3)c(C)[n+]1CCOCCOCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789823 125887 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 906 21 5 7 6.0 Cc1ccc(/C=C/c2cc3c4c(c2)CCCN4CCC3)c(C)[n+]1CCOCCOCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
11800628 221826 0 None None None Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 541 6 4 4 6.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4sccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL329366 221826 0 None None None Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 541 6 4 4 6.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4sccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
54585271 125839 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1098 29 6 8 9.1 Cc1cc(/C=C\C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789354 125839 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1098 29 6 8 9.1 Cc1cc(/C=C\C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
54583332 125863 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1070 27 6 8 8.3 Cc1cc(/C=C/C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789557 125863 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1070 27 6 8 8.3 Cc1cc(/C=C/C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
49865812 40046 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 699 21 8 7 3.1 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(N)=O 10.1016/j.bmc.2010.07.028
CHEMBL1224000 40046 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 699 21 8 7 3.1 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(N)=O 10.1016/j.bmc.2010.07.028
72205486 202617 0 None 29 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 689 20 9 7 1.2 N=C(N)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040689 202617 0 None 29 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 689 20 9 7 1.2 N=C(N)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL2370633 485599 0 None -426 2 Human 6.9 pKi = 6.9 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2198 56 33 31 -11.5 CC[C@H](C)[C@H](NC(=O)[C@@H]1CNC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL4289021 478196 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4034 128 61 56 -16.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294418 478222 0 None -1000 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2261 50 36 30 -6.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
44362637 80799 0 None None None Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 522 9 0 5 6.1 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CC(=O)N2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL145438 80799 0 None None None Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 522 9 0 5 6.1 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CC(=O)N2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL3349038 484267 0 None -6 2 Human 7.9 pKi = 7.9 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
72205671 202618 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 657 19 9 6 1.5 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CN)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040694 202618 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 657 19 9 6 1.5 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CN)cc1 10.1016/j.bmc.2013.08.065
3474 7886 30 None 2 3 Human 7.8 pKi = 7.8 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(01)00761-2
5311023 7886 30 None 2 3 Human 7.8 pKi = 7.8 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(01)00761-2
CHEMBL332347 7886 30 None 2 3 Human 7.8 pKi = 7.8 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/s0960-894x(01)00761-2
44362574 77464 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 7 0 4 6.4 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142427 77464 0 None None None Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 7 0 4 6.4 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL2371909 477715 0 None -33 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1695 53 26 20 -4.6 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
CHEMBL2371910 477716 0 None -31 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1709 54 26 20 -4.2 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
54587223 125877 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 875 18 6 5 7.0 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789787 125877 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 875 18 6 5 7.0 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10529375 473493 0 None None None Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 5 4 3 5.3 CC(C)(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88576 473493 0 None None None Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 5 4 3 5.3 CC(C)(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
11800499 473539 0 None None None Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 536 6 4 4 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cnc4ccccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88871 473539 0 None None None Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 536 6 4 4 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cnc4ccccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
155561620 349642 0 None -117 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4581256 349642 0 None -117 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
10696695 216395 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 7 4 3 5.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(CNC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314425 216395 0 None None None Human 5.9 pKi = 5.9 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 7 4 3 5.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(CNC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
54583519 124406 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 491 7 2 7 5.3 COc1cc(Cl)c(-c2c(C)nn3c(NCC(C)(C)NC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771263 124406 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 491 7 2 7 5.3 COc1cc(Cl)c(-c2c(C)nn3c(NCC(C)(C)NC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL2110196 485074 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2683 79 36 30 0.3 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
21336503 374142 0 None -549 2 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2cccc3ccccc23)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
CHEMBL51874 374142 0 None -549 2 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2cccc3ccccc23)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
10458754 80330 0 None None None Human 7.8 pKi = 7.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145056 80330 0 None None None Human 7.8 pKi = 7.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL3349022 484266 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
45269317 393048 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 519 7 1 4 5.2 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N(C)C)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL562000 393048 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 519 7 1 4 5.2 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N(C)C)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
70686176 157265 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 486 13 5 4 3.9 N=C(N)NCCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)CCc1ccc(O)cc1 10.1021/ml200265m
CHEMBL2046865 157265 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
ChEMBL 486 13 5 4 3.9 N=C(N)NCCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)CCc1ccc(O)cc1 10.1021/ml200265m
10625155 222050 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 498 6 4 3 4.8 C/N=C(/Nc1ccccc1)NC1CCc2ccccc2N(Cc2cccc(NC(=O)NC(C)C)c2)C1=O 10.1021/jm990044m
CHEMBL330095 222050 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 498 6 4 3 4.8 C/N=C(/Nc1ccccc1)NC1CCc2ccccc2N(Cc2cccc(NC(=O)NC(C)C)c2)C1=O 10.1021/jm990044m
45270153 390317 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 559 7 1 4 6.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL552762 390317 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 559 7 1 4 6.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
54582348 125876 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 849 20 6 5 6.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789785 125876 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 849 20 6 5 6.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10624998 473785 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 493 6 4 6 3.7 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nncs3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL90560 473785 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 493 6 4 6 3.7 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nncs3)CCc3ccccc32)c1 10.1021/jm990044m
49865799 40033 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 830 29 6 5 10.2 CCCCCCCCCCCCC#CC#CCCCCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1223986 40033 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 830 29 6 5 10.2 CCCCCCCCCCCCC#CC#CCCCCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
10842778 221121 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCCC4CCNCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL328460 221121 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCCC4CCNCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
46879650 20616 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 6 2 6 5.2 CC[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1081733 20616 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 6 2 6 5.2 CC[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL4294277 478221 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283846 478172 0 None -39 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4034 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CO)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10605125 474233 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.4 Clc1ccc(OCc2nc3c(OCCCC4CCCCN4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL93535 474233 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.4 Clc1ccc(OCc2nc3c(OCCCC4CCCCN4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
16132350 484239 20 None -13 2 Human 7.8 pKi = 7.8 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.0c00027
CHEMBL267633 484239 20 None -13 2 Human 7.8 pKi = 7.8 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.0c00027
44362801 79415 0 None None None Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 472 7 0 4 5.8 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL144262 79415 0 None None None Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 472 7 0 4 5.8 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL3349022 484266 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL4294277 478221 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
45267593 393793 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 515 6 1 3 5.7 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccccc1 10.1016/j.bmcl.2009.06.050
CHEMBL564810 393793 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 515 6 1 3 5.7 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccccc1 10.1016/j.bmcl.2009.06.050
10505296 473476 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 492 6 4 5 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nccs3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88450 473476 0 None None None Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 492 6 4 5 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nccs3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL266730 486205 0 None -51 2 Human 6.8 pKi = 6.8 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2261 70 32 31 -9.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL4283846 478172 0 None -39 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4034 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CO)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
155547323 347717 0 None -144 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4533775 347717 0 None -144 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
9982218 201875 5 None -2041 6 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL299879 201875 5 None -2041 6 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
21188477 81581 0 None None None Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 483 11 1 5 5.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(=O)O)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL146116 81581 0 None None None Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 483 11 1 5 5.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(=O)O)CC1 10.1016/s0960-894x(98)00048-1
46879456 20237 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.5 COc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079609 20237 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.5 COc1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
10625949 216214 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 526 6 4 5 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ocnc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314123 216214 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 526 6 4 5 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ocnc4c3)CCc3ccccc32)c1 10.1021/jm990044m
10649777 473175 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 4 3 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)CCC4)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL86433 473175 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 4 3 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)CCC4)CCc3ccccc32)c1 10.1021/jm990044m
10509290 473066 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@@H]4CCCNC4)cccc3n2CCC[C@H]2CCCNC2)cc1 10.1021/jm9706630
CHEMBL90717 473066 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@@H]4CCCNC4)cccc3n2CCC[C@H]2CCCNC2)cc1 10.1021/jm9706630
44362838 80875 0 None None None Human 5.8 pKi = 5.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 461 7 1 4 6.4 CN(C)C1CCN(CCc2c(CNc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145501 80875 0 None None None Human 5.8 pKi = 5.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 461 7 1 4 6.4 CN(C)C1CCN(CCc2c(CNc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44362997 240572 0 None None None Human 5.8 pKi = 5.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.9 CC(Oc1ccc(Cl)cc1Cl)c1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL359207 240572 0 None None None Human 5.8 pKi = 5.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.9 CC(Oc1ccc(Cl)cc1Cl)c1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
21336489 160983 0 None -1737 2 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 441 8 3 4 3.7 Nc1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL2113711 160983 0 None -1737 2 Human 4.8 pKi = 4.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 441 8 3 4 3.7 Nc1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
44362506 80352 0 None None None Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 515 8 1 5 4.9 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C(N)=O)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145078 80352 0 None None None Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 515 8 1 5 4.9 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C(N)=O)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
46879693 20292 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 430 6 2 6 6.2 c1ccc([C@@H]2CSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1079927 20292 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 430 6 2 6 6.2 c1ccc([C@@H]2CSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
15383696 387276 0 None None None Human 5.8 pKi = 5.8 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2ccc(Cl)cc2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL53876 387276 0 None None None Human 5.8 pKi = 5.8 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2ccc(Cl)cc2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
45269306 392838 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 6.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCCC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL561392 392838 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 6.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCCC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
10626335 222037 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 543 6 4 5 4.7 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)OCCO4)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL329997 222037 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 543 6 4 5 4.7 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)OCCO4)CCc3ccccc32)c1 10.1021/jm990044m
10577995 332830 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 524 6 5 3 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4[nH]ccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL432766 332830 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 524 6 5 3 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4[nH]ccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
10795082 474214 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 5.8 Clc1ccc(OCc2nc3c(OCCC4CCCNC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL93375 474214 0 None None None Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 5.8 Clc1ccc(OCc2nc3c(OCCC4CCCNC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
44351121 314845 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 91 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929374 314845 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 91 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL409634 314845 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 91 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
2317 139928 3 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to NPY1 receptorBinding affinity to NPY1 receptor
ChEMBL 590 27 4 8 6.3 COc1ccccc1CNCCCCCCNCCSSCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmcl.2011.06.124
CHEMBL19060 139928 3 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to NPY1 receptorBinding affinity to NPY1 receptor
ChEMBL 590 27 4 8 6.3 COc1ccccc1CNCCCCCCNCCSSCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmcl.2011.06.124
CHEMBL340824 236975 0 None None None Human 6.7 pKi = 6.7 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 636 10 3 7 7.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3cccc(-c4ccccc4)c3)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL3349022 484266 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
54587217 124717 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 586 16 6 5 3.1 NCCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1774205 124717 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 586 16 6 5 3.1 NCCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
44362862 237998 0 None None None Human 6.7 pKi = 6.7 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(CO)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL343399 237998 0 None None None Human 6.7 pKi = 6.7 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 502 8 1 5 5.3 CN(C)C1CCN(CCc2c(COc3ccc(CO)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44362821 78234 0 None None None Human 5.7 pKi = 5.7 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 385 6 0 3 6.2 Clc1ccc(OCc2sc3ccccc3c2CCN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
CHEMBL143068 78234 0 None None None Human 5.7 pKi = 5.7 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 385 6 0 3 6.2 Clc1ccc(OCc2sc3ccccc3c2CCN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
46879779 20348 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 472 8 2 6 6.9 c1ccc(CCC2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1080301 20348 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 472 8 2 6 6.9 c1ccc(CCC2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL4283705 478170 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282216 478164 0 None -316 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4032 124 59 56 -16.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CN(C(=N)N)C[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
16132350 484239 20 None -13 2 Human 8.7 pKi = 8.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL267633 484239 20 None -13 2 Human 8.7 pKi = 8.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL3349022 484266 0 None -3 2 Human 8.7 pKi = 8.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
10414488 466724 0 None None None Human 8.7 pKi = 8.7 Binding
Binding affinity at cloned Neuropeptide Y receptor type 1 expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y receptor type 1 expressed in AV-12 cells is evaluated.
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1016/s0960-894x(98)00048-1
CHEMBL61532 466724 0 None None None Human 8.7 pKi = 8.7 Binding
Binding affinity at cloned Neuropeptide Y receptor type 1 expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y receptor type 1 expressed in AV-12 cells is evaluated.
ChEMBL 524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1016/s0960-894x(98)00048-1
3474 7886 30 None 2 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
5311023 7886 30 None 2 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
CHEMBL332347 7886 30 None 2 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm801018u
CHEMBL441396 484356 0 None -6 2 Human 8.7 pKi = 8.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 4252 131 59 59 -18.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
44283143 317234 0 None 28 4 Human 8.6 pKi = 8.6 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
91931648 317234 0 None 28 4 Human 8.6 pKi = 8.6 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
CHEMBL413455 317234 0 None 28 4 Human 8.6 pKi = 8.6 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
155563387 349327 0 None 269 2 Human 8.6 pKi = 8.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2259 56 35 29 -7.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4573545 349327 0 None 269 2 Human 8.6 pKi = 8.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2259 56 35 29 -7.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL126618 41929 0 None None None Human 8.6 pKi = 8.6 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 576 9 4 8 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3cccc(O)c3)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL437863 488684 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4265 131 59 59 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
10767712 221096 0 None None None Human 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 6 5 4 4.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(\N)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL328288 221096 0 None None None Human 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 6 5 4 4.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(\N)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL4283705 478170 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
72205482 202614 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 671 19 8 5 2.7 NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040670 202614 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 671 19 8 5 2.7 NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL2440898 477834 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1625 54 21 16 1.5 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CNC(=O)CCC(=O)NCCN(CCN)CCNC(=O)CCC(=O)NCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040691 477834 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1625 54 21 16 1.5 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CNC(=O)CCC(=O)NCCN(CCN)CCNC(=O)CCC(=O)NCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
10625207 473527 0 None None None Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 6 5 4 4.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(N)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88805 473527 0 None None None Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 6 5 4 4.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(N)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL4282216 478164 0 None -316 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4032 124 59 56 -16.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CN(C(=N)N)C[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
21188661 80746 0 None None None Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 550 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(=O)N2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL145396 80746 0 None None None Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 550 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(=O)N2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
171357542 386647 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 628 12 3 11 3.9 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(Nc2c(NCCCN3CCC(c4cccc(OC)c4)CC3)c(=O)c2=O)c1 10.1039/D1MD00058F
CHEMBL5282574 386647 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 628 12 3 11 3.9 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(Nc2c(NCCCN3CCC(c4cccc(OC)c4)CC3)c(=O)c2=O)c1 10.1039/D1MD00058F
9908496 124399 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 391 6 2 5 4.9 Cc1cc(C)c(-c2c(C)nn3c(NCCNC4CCCC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771256 124399 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 391 6 2 5 4.9 Cc1cc(C)c(-c2c(C)nn3c(NCCNC4CCCC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.12.116
16200926 484354 10 None -52 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cellsDisplacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cells
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
CHEMBL439904 484354 10 None -52 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cellsDisplacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cells
ChEMBL 4047 129 61 56 -16.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
CHEMBL3349022 484266 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL428017 488501 20 None -41 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to NPYY1 receptor (unknown origin)Binding affinity to NPYY1 receptor (unknown origin)
ChEMBL 1786 58 29 23 -5.8 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1016/j.bmcl.2013.11.061
CHEMBL428017 488501 20 None -41 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human NPY1 receptor in SK-N-MC cellsDisplacement of [125I]PYY from human NPY1 receptor in SK-N-MC cells
ChEMBL 1786 58 29 23 -5.8 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1016/j.bmcl.2007.01.045
45268477 393170 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1cccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)c1 10.1016/j.bmcl.2009.06.050
CHEMBL562532 393170 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1cccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)c1 10.1016/j.bmcl.2009.06.050
CHEMBL2440911 477841 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040758 477841 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL411979 488196 0 None -83 2 Human 6.7 pKi = 6.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3339 89 46 47 -13.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@H](C)CC 10.1021/jm00055a010
11799136 216220 0 None None None Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 4.9 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Oc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314169 216220 0 None None None Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 4.9 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Oc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
162651028 366985 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802711 366985 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44362526 238168 0 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 455 9 1 5 5.2 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CC(=O)O)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL344722 238168 0 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 455 9 1 5 5.2 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CC(=O)O)CC1 10.1016/s0960-894x(98)00048-1
54587431 124408 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 425 8 2 6 4.3 COc1cc(Cl)c(-c2c(C)nn3c(NCCNCCF)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771265 124408 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 425 8 2 6 4.3 COc1cc(Cl)c(-c2c(C)nn3c(NCCNCCF)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
44517723 387839 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 581 8 1 4 6.0 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)F)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL540466 387839 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 581 8 1 4 6.0 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)F)cc1 10.1016/j.bmcl.2009.06.050
52953218 125870 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 918 20 6 6 6.3 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789734 125870 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 918 20 6 6 6.3 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
52953218 125870 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometryDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometry
ChEMBL 918 20 6 6 6.3 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789734 125870 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometryDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometry
ChEMBL 918 20 6 6 6.3 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
127041328 274546 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 559 13 7 5 1.7 NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747821 274546 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 559 13 7 5 1.7 NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
44351120 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
44351146 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929372 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929377 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL437671 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL440824 333455 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL408891 488038 0 None -41 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1538 47 23 17 -2.7 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
CHEMBL2370624 477666 0 None -95 2 Human 6.7 pKi = 6.7 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2157 56 33 30 -9.9 CC[C@H](C)[C@H](NC(=O)[C@@H]1CNC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
46879560 20684 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.9 c1ccc2sc(NCCc3ccc(NC4=NCCCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1082083 20684 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.9 c1ccc2sc(NCCc3ccc(NC4=NCCCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
54587219 125871 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 931 21 6 5 7.0 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789738 125871 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 931 21 6 5 7.0 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL2440899 477840 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1963 55 17 21 5.8 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040747 477840 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1963 55 17 21 5.8 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL2440911 477841 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040758 477841 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL2370634 485600 0 None -208 2 Human 6.6 pKi = 6.6 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2212 56 33 31 -11.1 CC[C@H](C)[C@H](NC(=O)[C@@H]1CNC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
44363007 80564 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 475 6 1 4 6.0 CN(C)C1CCN(CCc2c(C(=O)Nc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145243 80564 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 475 6 1 4 6.0 CN(C)C1CCN(CCc2c(C(=O)Nc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
22617869 124397 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 323 4 2 5 3.3 Cc1cc(C)c(-c2c(C)nn3c(NCCN)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771254 124397 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 323 4 2 5 3.3 Cc1cc(C)c(-c2c(C)nn3c(NCCN)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.12.116
10619067 329511 0 None None None Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 368 5 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CN2CCCCC2)c2ccccc21 10.1021/jm9706630
CHEMBL421549 329511 0 None None None Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 368 5 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CN2CCCCC2)c2ccccc21 10.1021/jm9706630
3474 7886 30 None 2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm970512x
5311023 7886 30 None 2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm970512x
CHEMBL332347 7886 30 None 2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm970512x
10619067 329511 0 None None None Human 5.6 pKi = 5.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 368 5 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CN2CCCCC2)c2ccccc21 10.1021/jm970512x
CHEMBL421549 329511 0 None None None Human 5.6 pKi = 5.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 368 5 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CN2CCCCC2)c2ccccc21 10.1021/jm970512x
19426744 387202 0 None None None Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 407 3 1 6 3.3 Nc1cc(S(=O)(=O)c2ccccc2Br)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL53497 387202 0 None None None Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 407 3 1 6 3.3 Nc1cc(S(=O)(=O)c2ccccc2Br)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
21336493 372358 0 None -1698 2 Human 4.6 pKi = 4.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccc3ccccc3n2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL51138 372358 0 None -1698 2 Human 4.6 pKi = 4.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccc3ccccc3n2)CC1 10.1016/s0960-894x(02)00287-1
45271821 122253 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 555 8 1 5 6.6 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccc(OC)nc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL171377 122253 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 555 8 1 5 6.6 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccc(OC)nc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
54584290 125834 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 880 23 5 7 6.0 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCOCCOCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789346 125834 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 880 23 5 7 6.0 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCOCCOCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL2440914 477839 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1701 52 17 18 4.1 NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040731 477839 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1701 52 17 18 4.1 NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
10674056 470788 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4scnc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL84793 470788 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4scnc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL263848 486106 0 None -16 2 Human 7.6 pKi = 7.6 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3339 91 46 47 -13.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
10600984 215704 0 None None None Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccn3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL313292 215704 0 None None None Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccn3)CCc3ccccc32)c1 10.1021/jm990044m
44362444 80611 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 436 7 0 4 6.0 Cc1cc(C)c(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C)c1 10.1016/s0960-894x(99)00019-0
CHEMBL145289 80611 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 436 7 0 4 6.0 Cc1cc(C)c(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C)c1 10.1016/s0960-894x(99)00019-0
44362459 237562 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 529 9 0 5 5.9 CN(C)Cc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL341908 237562 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 529 9 0 5 5.9 CN(C)Cc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
46880224 20562 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 354 5 2 6 4.5 c1ccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1081469 20562 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 354 5 2 6 4.5 c1ccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL2440927 477842 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1605 54 17 18 1.8 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040781 477842 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1605 54 17 18 1.8 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
10816575 473257 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 554 6 5 5 3.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)C(=O)NC4=O)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL86952 473257 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 554 6 5 5 3.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)C(=O)NC4=O)CCc3ccccc32)c1 10.1021/jm990044m
155533017 336340 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2435 58 36 30 -4.4 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4468261 336340 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2435 58 36 30 -4.4 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL438914 488751 12 None 54 4 Human 7.6 pKi = 7.6 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 1221 36 15 16 -2.1 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](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)N[C@@H](Cc1ccc(O)cc1)C(=O)OC)[C@@H](C)CC 10.1021/jm010031k
CHEMBL4290445 478203 0 None -3981 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4135 129 61 56 -15.2 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290615 478205 0 None -12 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 478203 0 None -3981 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4135 129 61 56 -15.2 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290615 478205 0 None -12 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
46879737 20342 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.4 COC1CN=C(Nc2ccc(CCNc3nc4ccccc4s3)cc2)S1 10.1016/j.bmcl.2009.09.048
CHEMBL1080289 20342 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.4 COC1CN=C(Nc2ccc(CCNc3nc4ccccc4s3)cc2)S1 10.1016/j.bmcl.2009.09.048
10672357 40645 0 None None None Human 7.6 pKi = 7.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 479 7 0 5 5.5 Cn1c(COc2ccc(Cl)cc2)c(C(=O)CN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
CHEMBL124343 40645 0 None None None Human 7.6 pKi = 7.6 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 479 7 0 5 5.5 Cn1c(COc2ccc(Cl)cc2)c(C(=O)CN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
52953220 125869 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789732 125869 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
52953220 125869 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometryDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometry
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789732 125869 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometryDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells by flow cytometry
ChEMBL 962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
10554097 216656 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 5 4 4.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4[nH]ncc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL315299 216656 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 5 4 4.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4[nH]ncc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL3349341 484268 0 None -72 2 Human 6.6 pKi = 6.6 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
44362542 239644 0 None None None Human 6.6 pKi = 6.6 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 10 0 5 6.5 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(C(=O)CCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL356585 239644 0 None None None Human 6.6 pKi = 6.6 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 10 0 5 6.5 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(C(=O)CCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
49865807 40040 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 714 21 7 8 3.8 COC(=O)CCNC(=O)CCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1223995 40040 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 714 21 7 8 3.8 COC(=O)CCNC(=O)CCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL2440899 477840 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1963 55 17 21 5.8 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040747 477840 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1963 55 17 21 5.8 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
44362811 329967 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 399 7 0 3 6.6 Clc1ccc(OCc2sc3ccccc3c2CCCN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
CHEMBL422655 329967 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 399 7 0 3 6.6 Clc1ccc(OCc2sc3ccccc3c2CCCN2CCCCC2)cc1 10.1016/s0960-894x(99)00019-0
44350924 333614 0 None -58 4 Human 6.6 pKi = 6.6 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929378 333614 0 None -58 4 Human 6.6 pKi = 6.6 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL439122 333614 0 None -58 4 Human 6.6 pKi = 6.6 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
45271004 390178 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 549 6 1 3 6.4 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL551876 390178 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 549 6 1 3 6.4 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.050
44563342 372769 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 515 13 5 4 3.4 CCC/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL515095 372769 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 515 13 5 4 3.4 CCC/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
10676562 221130 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@H]4CCCNC4)cccc3n2CCC[C@@H]2CCCNC2)cc1 10.1021/jm9706630
CHEMBL328532 221130 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@H]4CCCNC4)cccc3n2CCC[C@@H]2CCCNC2)cc1 10.1021/jm9706630
49865801 40035 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 743 15 6 5 7.7 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCc1ccc2ccc3cccc4ccc1c2c34 10.1016/j.bmc.2010.07.028
CHEMBL1223988 40035 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 743 15 6 5 7.7 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCc1ccc2ccc3cccc4ccc1c2c34 10.1016/j.bmc.2010.07.028
CHEMBL592104 489308 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1650 48 22 23 -4.9 CC[C@H](C)[C@H](NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
44362774 329826 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 422 8 0 5 4.9 CN(C)C1CCN(CCc2c(COc3ccccc3C=O)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL422297 329826 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 422 8 0 5 4.9 CN(C)C1CCN(CCc2c(COc3ccccc3C=O)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10673757 216542 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 529 6 4 5 4.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)OCO4)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314529 216542 0 None None None Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 529 6 4 5 4.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)OCO4)CCc3ccccc32)c1 10.1021/jm990044m
44362627 82183 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 8 0 4 6.4 CN(C)C1CCN(CCc2c(CCOc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL146606 82183 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 8 0 4 6.4 CN(C)C1CCN(CCc2c(CCOc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL2440194 486012 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 1661 53 28 21 -5.7 CCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)[C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm4008505
10472655 387048 0 None None None Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 344 3 2 7 2.1 Nc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
CHEMBL53016 387048 0 None None None Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 344 3 2 7 2.1 Nc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
44362868 66935 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 464 7 0 4 6.7 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C(C)(C)C)c1 10.1016/s0960-894x(99)00019-0
CHEMBL141879 66935 0 None None None Human 5.6 pKi = 5.6 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 464 7 0 4 6.7 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(C(C)(C)C)c1 10.1016/s0960-894x(99)00019-0
44362387 81153 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 439 9 0 4 6.5 CCCN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL145761 81153 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 439 9 0 4 6.5 CCCN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
21188602 329671 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 501 10 0 4 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL421770 329671 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 501 10 0 4 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
21188717 330204 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 511 12 0 6 6.4 CCOC(=O)CCCN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL423383 330204 0 None None None Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 511 12 0 6 6.4 CCOC(=O)CCCN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL2440183 477809 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to Y1 receptor (unknown origin)Binding affinity to Y1 receptor (unknown origin)
ChEMBL 1686 52 27 23 -6.2 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)[C@H]1C(=O)OC)[C@@H](C)O)[C@@H](C)CC 10.1021/jm4008505
9868731 124398 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 457 9 2 6 5.2 COc1ccc(CCNCCNc2cc(C)nc3c(-c4c(C)cc(C)cc4C)c(C)nn23)cc1 10.1016/j.bmcl.2010.12.116
CHEMBL1771255 124398 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 457 9 2 6 5.2 COc1ccc(CCNCCNc2cc(C)nc3c(-c4c(C)cc(C)cc4C)c(C)nn23)cc1 10.1016/j.bmcl.2010.12.116
45272692 392097 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 525 7 1 4 6.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4cccnc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL559045 392097 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 525 7 1 4 6.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4cccnc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
54582343 125873 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 875 19 5 5 7.6 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789769 125873 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 875 19 5 5 7.6 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL2440928 477831 0 None 7 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1633 56 17 18 2.6 NCCN(CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040658 477831 0 None 7 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1633 56 17 18 2.6 NCCN(CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
10744091 473775 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 503 6 4 3 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(F)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL90497 473775 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 503 6 4 3 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(F)cc3)CCc3ccccc32)c1 10.1021/jm990044m
10700181 474122 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 6.0 Clc1ccc(OCc2nc3c(OCCC4CCCCN4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL92679 474122 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 6.0 Clc1ccc(OCc2nc3c(OCCC4CCCCN4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
155543070 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
155549336 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
172472665 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4522438 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4549208 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL5499142 347296 0 None -158 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL414051 488318 0 None -323 2 Human 6.5 pKi = 6.5 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2275 70 32 31 -8.6 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
162648914 366975 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802592 366975 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
162662291 367047 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803298 367047 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
15383694 372292 0 None None None Human 6.5 pKi = 6.5 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 329 3 1 6 2.6 Nc1cc(S(=O)(=O)c2ccccc2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL51065 372292 0 None None None Human 6.5 pKi = 6.5 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 329 3 1 6 2.6 Nc1cc(S(=O)(=O)c2ccccc2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
9869677 124403 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 477 8 2 7 4.9 CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771260 124403 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 477 8 2 7 4.9 CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
49865808 40041 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 640 16 7 9 2.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCn1cc(CO)nn1 10.1016/j.bmc.2010.07.028
CHEMBL1223996 40041 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 640 16 7 9 2.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCn1cc(CO)nn1 10.1016/j.bmc.2010.07.028
CHEMBL604165 489324 0 None -8 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 3111 92 44 45 -13.6 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.12.068
127041325 274543 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 714 15 6 8 4.4 [N-]=[N+]=Nc1cccc(-n2cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)c1 10.1021/acs.jmedchem.5b00925
CHEMBL3747818 274543 0 None None None Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 714 15 6 8 4.4 [N-]=[N+]=Nc1cccc(-n2cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)c1 10.1021/acs.jmedchem.5b00925
14160 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1039/D1MD00058F
9960164 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1039/D1MD00058F
CHEMBL2046866 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1039/D1MD00058F
CHEMBL324554 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1039/D1MD00058F
14160 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00761-2
9960164 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00761-2
CHEMBL2046866 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00761-2
CHEMBL324554 1380 35 None None None Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 10.1016/s0960-894x(01)00761-2
9869041 124402 12 None -3 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125]sauvagin from rat recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125]sauvagin from rat recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771259 124402 12 None -3 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125]sauvagin from rat recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125]sauvagin from rat recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL4290048 478201 0 None -25 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4005 126 59 55 -15.2 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL413871 488306 0 None -7 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 2298 71 34 25 -3.7 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
11640844 20346 0 None 199 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1080298 20346 0 None 199 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL2440924 477820 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1285 38 13 12 3.9 NCCN(CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
10605127 221131 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCCC4CCCNC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL328541 221131 0 None None None Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCCC4CCCNC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
45269310 392905 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 531 7 1 4 6.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCCC4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL561594 392905 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 531 7 1 4 6.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCCC4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
162661307 367040 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803242 367040 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
72205289 202609 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 703 21 8 7 1.2 NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040662 202609 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 703 21 8 7 1.2 NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
155564444 349269 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2181 50 30 28 -5.3 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4572358 349269 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2181 50 30 28 -5.3 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
44362820 78167 0 None None None Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 428 7 0 4 5.7 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL143014 78167 0 None None None Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 428 7 0 4 5.7 CN(C)C1CCN(CCc2c(COc3ccc(Cl)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL2440912 477837 0 None -10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040729 477837 0 None -10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1717 58 19 18 0.7 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
46879646 19832 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 436 5 2 6 6.2 Clc1cc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2cc1Cl 10.1016/j.bmcl.2009.09.048
CHEMBL1076268 19832 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 436 5 2 6 6.2 Clc1cc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2cc1Cl 10.1016/j.bmcl.2009.09.048
46879607 20314 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 386 5 2 6 5.0 Fc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1080100 20314 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 386 5 2 6 5.0 Fc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
45270136 390030 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 559 7 1 4 7.2 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccc(Cl)nc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL551206 390030 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 559 7 1 4 7.2 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccc(Cl)nc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL340208 236642 0 None None None Human 6.5 pKi = 6.5 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 609 10 3 8 5.5 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/s0960-894x(01)00761-2
10791454 222048 0 None None None Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.2 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCCCN2)cc1 10.1021/jm9706630
CHEMBL330066 222048 0 None None None Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.2 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCCCN2)cc1 10.1021/jm9706630
21336500 201790 0 None -190 2 Human 5.5 pKi = 5.5 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 500 10 3 4 4.8 O=S(=O)(NC[C@H]1CC[C@H](CNC(CO)Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL299295 201790 0 None -190 2 Human 5.5 pKi = 5.5 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 500 10 3 4 4.8 O=S(=O)(NC[C@H]1CC[C@H](CNC(CO)Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
15338882 352997 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 531 11 5 5 2.8 COC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL471710 352997 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 531 11 5 5 2.8 COC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
45269300 392629 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 8 1 6 7.4 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(c4ccccc4)(c4nnc(C)s4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL560795 392629 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 8 1 6 7.4 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(c4ccccc4)(c4nnc(C)s4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL2440917 477829 0 None 9 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1539 52 19 14 4.0 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CCCC(=O)NCCN(CCN)CCNC(=O)CCCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040656 477829 0 None 9 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1539 52 19 14 4.0 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CCCC(=O)NCCN(CCN)CCNC(=O)CCCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
46879609 20316 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 413 6 2 8 4.8 O=[N+]([O-])c1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1080102 20316 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 413 6 2 8 4.8 O=[N+]([O-])c1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
46879780 20349 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 450 6 2 6 6.8 c1ccc2sc(NCCc3ccc(NC4=NC(C5CCCCC5)CCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1080302 20349 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 450 6 2 6 6.8 c1ccc2sc(NCCc3ccc(NC4=NC(C5CCCCC5)CCS4)cc3)nc2c1 10.1016/j.bmcl.2009.09.048
15421872 238081 0 None None None Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 397 7 1 4 5.4 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCNCC1 10.1016/s0960-894x(98)00048-1
CHEMBL344096 238081 0 None None None Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 397 7 1 4 5.4 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCNCC1 10.1016/s0960-894x(98)00048-1
10820168 197186 0 None 47 4 Human 7.5 pKi = 7.5 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 1192 37 16 15 -2.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC 10.1021/jm010031k
CHEMBL265391 197186 0 None 47 4 Human 7.5 pKi = 7.5 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 1192 37 16 15 -2.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](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)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC 10.1021/jm010031k
CHEMBL438548 488722 0 None -4 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1759 55 26 22 -4.0 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CSSC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
46879608 20315 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 402 5 2 6 5.5 Clc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1080101 20315 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 402 5 2 6 5.5 Clc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
46879453 20206 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.8 Cc1cccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc12 10.1016/j.bmcl.2009.09.048
CHEMBL1079440 20206 0 None None None Human 5.5 pKi = 5.5 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.8 Cc1cccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc12 10.1016/j.bmcl.2009.09.048
21336511 365998 0 None -323 2 Human 5.5 pKi = 5.5 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL51884 365998 0 None -323 2 Human 5.5 pKi = 5.5 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL439307 488778 22 None 57 2 Human 7.4 pKi = 7.4 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2595 85 38 36 -9.0 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
10768859 215652 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 7 5 4 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(/Nc3ccc(O)cc3)NC(C)C)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL313007 215652 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 7 5 4 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(/Nc3ccc(O)cc3)NC(C)C)CCc3ccccc32)c1 10.1021/jm990044m
73354090 202622 0 None 11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 757 21 10 7 0.2 NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
73355613 202622 0 None 11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 757 21 10 7 0.2 NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040709 202622 0 None 11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 757 21 10 7 0.2 NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040756 202622 0 None 11 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 757 21 10 7 0.2 NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
127030359 276535 0 None -257 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787713 276535 0 None -257 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
44362625 238082 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 628 7 0 4 7.3 CN(C)C1CCN(CCc2c(COc3c(Br)cc(Br)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL344101 238082 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 628 7 0 4 7.3 CN(C)C1CCN(CCc2c(COc3c(Br)cc(Br)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
46879524 19827 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 422 5 2 6 5.8 Clc1cc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2cc1Cl 10.1016/j.bmcl.2009.09.048
CHEMBL1076234 19827 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 422 5 2 6 5.8 Clc1cc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2cc1Cl 10.1016/j.bmcl.2009.09.048
44362553 237580 0 None None None Human 7.4 pKi = 7.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 508 10 0 5 6.6 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL342112 237580 0 None None None Human 7.4 pKi = 7.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 508 10 0 5 6.6 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL2440927 477842 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1605 54 17 18 1.8 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040781 477842 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1605 54 17 18 1.8 NCCN(CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL124061 40484 0 None None None Human 7.4 pKi = 7.4 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 591 10 4 9 4.5 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3cccc(O)c3)CC2)c1 10.1016/s0960-894x(01)00761-2
44362784 238114 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 408 7 0 4 5.4 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)cc1 10.1016/s0960-894x(99)00019-0
CHEMBL344338 238114 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 408 7 0 4 5.4 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)cc1 10.1016/s0960-894x(99)00019-0
44362398 80335 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 470 8 0 4 6.7 CN(C)C1CCN(CCc2c(COc3ccc(-c4ccccc4)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145061 80335 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 470 8 0 4 6.7 CN(C)C1CCN(CCc2c(COc3ccc(-c4ccccc4)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
46879649 20615 1 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.9 C[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1081732 20615 1 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 368 5 2 6 4.9 C[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
54580549 124400 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 417 6 2 5 5.3 Cc1cc(NCCNC2CCCC2)n2nc(C)c(-c3c(Cl)cccc3Cl)c2n1 10.1016/j.bmcl.2010.12.116
CHEMBL1771257 124400 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 417 6 2 5 5.3 Cc1cc(NCCNC2CCCC2)n2nc(C)c(-c3c(Cl)cccc3Cl)c2n1 10.1016/j.bmcl.2010.12.116
54584288 124719 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 587 15 7 6 2.7 N=C(N)N(CCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)C(=O)NCCCCN 10.1016/j.bmc.2011.03.045
CHEMBL1774207 124719 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 587 15 7 6 2.7 N=C(N)N(CCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)C(=O)NCCCCN 10.1016/j.bmc.2011.03.045
54587221 125836 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 932 21 6 6 6.7 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789348 125836 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 932 21 6 6 6.7 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
44362861 239959 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 497 7 0 5 5.7 CN(C)C1CCN(CCc2c(COc3ccc(C#N)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL358111 239959 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 497 7 0 5 5.7 CN(C)C1CCN(CCc2c(COc3ccc(C#N)cc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44362989 333297 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 520 7 0 4 5.7 CN(C)C1CCN(CCc2c(COc3ccccc3I)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL436213 333297 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 520 7 0 4 5.7 CN(C)C1CCN(CCc2c(COc3ccccc3I)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
162652708 366994 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802795 366994 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44362895 77669 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 6 1 4 5.9 CN(C)C1CCN(CCc2c(C(O)c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142603 77669 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 6 1 4 5.9 CN(C)C1CCN(CCc2c(C(O)c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10624729 216564 0 None None None Human 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 484 7 3 3 4.4 CC(C)NC(=O)Cc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314662 216564 0 None None None Human 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 484 7 3 3 4.4 CC(C)NC(=O)Cc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
9911304 124409 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 443 8 2 6 4.6 COc1cc(Cl)c(-c2c(C)nn3c(NCCNCC(F)F)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771266 124409 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 443 8 2 6 4.6 COc1cc(Cl)c(-c2c(C)nn3c(NCCNCC(F)F)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL591971 489306 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1207 36 18 15 -1.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2009.12.068
CHEMBL4278700 478140 0 None -398 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4211 131 60 58 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 478215 0 None -100 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4048 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3349022 484266 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL238533 485977 0 None -128 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cellsDisplacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cells
ChEMBL 1888 61 32 26 -8.4 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
44350924 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
91929378 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL439122 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4279794 478144 0 None -1584 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4121 129 62 56 -15.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279133 478143 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4288294 478192 0 None -630 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
46879454 20207 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.5 COc1cccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc12 10.1016/j.bmcl.2009.09.048
CHEMBL1079441 20207 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 384 6 2 7 4.5 COc1cccc2sc(NCCc3ccc(NC4=NCCS4)cc3)nc12 10.1016/j.bmcl.2009.09.048
CHEMBL127282 484596 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4237 130 59 59 -19.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL4290048 478201 0 None -25 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4005 126 59 55 -15.2 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
127041011 274541 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 688 14 7 8 3.1 N/C(=N/C(=O)NCc1cn(-c2ccc(N)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747816 274541 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 688 14 7 8 3.1 N/C(=N/C(=O)NCc1cn(-c2ccc(N)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL31913 217371 0 None None None Human 8.4 pKi = 8.4 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 590 10 3 8 5.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
54582344 124718 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 587 15 7 5 2.5 NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1774206 124718 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 587 15 7 5 2.5 NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
44362660 81095 0 None None None Human 8.4 pKi = 8.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 522 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCN2CCCCC2)CC1 10.1016/s0960-894x(99)00082-7
CHEMBL145714 81095 0 None None None Human 8.4 pKi = 8.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 522 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCN2CCCCC2)CC1 10.1016/s0960-894x(99)00082-7
44373216 197222 17 None None None Human 8.4 pKi = 8.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 490 12 1 6 5.7 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCNCC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL265752 197222 17 None None None Human 8.4 pKi = 8.4 Binding
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 490 12 1 6 5.7 c1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCNCC2)cc1 10.1016/s0960-894x(99)00082-7
CHEMBL3349039 486808 0 None -4 2 Human 8.4 pKi = 8.4 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4265 131 59 59 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
44362660 81095 0 None None None Human 8.4 pKi = 8.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 522 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL145714 81095 0 None None None Human 8.4 pKi = 8.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 522 11 0 5 6.9 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
127041307 274469 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 714 15 6 8 4.4 [N-]=[N+]=Nc1ccc(-n2cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746796 274469 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 714 15 6 8 4.4 [N-]=[N+]=Nc1ccc(-n2cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)cc1 10.1021/acs.jmedchem.5b00925
10076108 352857 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 545 12 5 5 3.2 CCOC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
CHEMBL470496 352857 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells
ChEMBL 545 12 5 5 3.2 CCOC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/jm801018u
10524003 39422 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 382 6 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CCN2CCCCC2)c2ccccc21 10.1021/jm970512x
CHEMBL121799 39422 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 382 6 0 3 5.4 Cn1c(COc2ccc(Cl)cc2)c(CCN2CCCCC2)c2ccccc21 10.1021/jm970512x
1485 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
21129772 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
5311023 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
9869458 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
CHEMBL2440929 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
CHEMBL332347 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
CHEMBL44246 1304 7 None 2 4 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm9706630
CHEMBL413426 488280 0 None 20 4 Human 8.3 pKi = 8.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 2419 73 30 34 -5.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)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)N[C@@H](Cc1ccc(O)cc1)C(=O)OC)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)N[C@@H](Cc1ccc(O)cc1)C(=O)OC 10.1021/jm010031k
CHEMBL4278700 478140 0 None -398 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4211 131 60 58 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 478215 0 None -100 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4048 129 61 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
49865804 40037 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 790 23 7 8 5.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(=O)OCc1ccccc1 10.1016/j.bmc.2010.07.028
CHEMBL1223991 40037 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 790 23 7 8 5.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(=O)OCc1ccccc1 10.1016/j.bmc.2010.07.028
CHEMBL2440925 477833 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1541 50 17 14 4.9 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040675 477833 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1541 50 17 14 4.9 NCCN(CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCC(=O)NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
44350924 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
91929378 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL439122 333614 0 None -58 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4279794 478144 0 None -1584 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4121 129 62 56 -15.6 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
53359565 274460 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from NPY1R (unknown origin)Displacement of [3H]UR-MK114 from NPY1R (unknown origin)
ChEMBL 860 18 6 12 4.1 CN(Cc1cn(-c2ccc(-n3cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)c1ccncc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746696 274460 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from NPY1R (unknown origin)Displacement of [3H]UR-MK114 from NPY1R (unknown origin)
ChEMBL 860 18 6 12 4.1 CN(Cc1cn(-c2ccc(-n3cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)c1ccncc1 10.1021/acs.jmedchem.5b00925
155543070 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
155549336 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
172472665 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4522438 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4549208 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL5499142 347296 0 None -158 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
10673317 221904 0 None None None Human 6.4 pKi = 6.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 7 1 4 5.4 Cc1cccc2nc(COc3ccc(Cl)cc3)n(CCCC3CCCNC3)c12 10.1021/jm9706630
CHEMBL329786 221904 0 None None None Human 6.4 pKi = 6.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 7 1 4 5.4 Cc1cccc2nc(COc3ccc(Cl)cc3)n(CCCC3CCCNC3)c12 10.1021/jm9706630
44362810 81220 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.5 COC(c1ccc(Cl)cc1Cl)c1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145808 81220 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.5 COC(c1ccc(Cl)cc1Cl)c1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL4279133 478143 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4288294 478192 0 None -630 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL124150 40506 0 None None None Human 6.4 pKi = 6.4 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 605 11 3 9 4.8 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccc(OC)cc3)CC2)c1 10.1016/s0960-894x(01)00761-2
49865810 40043 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 735 16 10 12 -0.1 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCC(=O)OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2010.07.028
CHEMBL1223998 40043 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 735 16 10 12 -0.1 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCC(=O)OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2010.07.028
127041326 274544 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 687 14 5 7 3.8 CN(Cc1cn(-c2ccccc2)nn1)C(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747819 274544 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 687 14 5 7 3.8 CN(Cc1cn(-c2ccccc2)nn1)C(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
72205667 202633 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 600 17 8 5 2.4 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCN)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040753 202633 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 600 17 8 5 2.4 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCN)cc1 10.1016/j.bmc.2013.08.065
10818866 473077 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@H]4CCCNC4)cccc3n2CCC[C@H]2CCCNC2)cc1 10.1021/jm9706630
CHEMBL92148 473077 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@H]4CCCNC4)cccc3n2CCC[C@H]2CCCNC2)cc1 10.1021/jm9706630
127031281 276534 0 None -301 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1789 59 29 21 -2.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN/C(N)=N/C(=O)NCCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787712 276534 0 None -301 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1789 59 29 21 -2.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN/C(N)=N/C(=O)NCCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL410007 488092 0 None -1023 2 Human 6.4 pKi = 6.4 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3384 82 49 47 -14.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
10815247 216539 0 None None None Human 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 7 3 4 5.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(COC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314520 216539 0 None None None Human 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 500 7 3 4 5.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(COC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL2311081 484214 0 None -58 2 Human 7.4 pKi = 7.4 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
45268459 392796 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 547 7 1 5 5.9 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCOC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL561332 392796 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 547 7 1 5 5.9 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCOC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
54580353 125883 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1004 26 7 8 6.7 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789807 125883 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1004 26 7 8 6.7 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2011.03.045
CHEMBL2440926 477830 0 None 13 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1541 50 17 14 4.9 NCCN(CCNC(=O)CCCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040657 477830 0 None 13 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1541 50 17 14 4.9 NCCN(CCNC(=O)CCCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
44362777 77615 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 408 7 0 4 5.4 Cc1ccccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142561 77615 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 408 7 0 4 5.4 Cc1ccccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
44362832 81076 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 486 7 0 4 6.1 Cc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145693 81076 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 486 7 0 4 6.1 Cc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
44362723 239712 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 446 6 0 3 6.4 CN(C)C1CCN(CCc2c(Cc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL357184 239712 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 446 6 0 3 6.4 CN(C)C1CCN(CCc2c(Cc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
136216703 155158 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using [125I]PYYBinding affinity against Neuropeptide Y receptor type 1 using [125I]PYY
ChEMBL 482 2 4 7 4.0 N[C@H]1CCCC[C@@H]1NC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL2112936 155158 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Binding affinity against Neuropeptide Y receptor type 1 using [125I]PYYBinding affinity against Neuropeptide Y receptor type 1 using [125I]PYY
ChEMBL 482 2 4 7 4.0 N[C@H]1CCCC[C@@H]1NC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
44362610 81048 0 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 483 10 0 6 5.6 CCOC(=O)CN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL145663 81048 0 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 483 10 0 6 5.6 CCOC(=O)CN1CCC(CCCn2c(COc3ccc(Cl)cc3)nc3c(C)cccc32)CC1 10.1016/s0960-894x(98)00048-1
25147723 26947 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1295 32 10 14 6.9 N/C(=N/C(=O)CCCn1cc(-c2ccc(-c3cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
25147724 26947 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1295 32 10 14 6.9 N/C(=N/C(=O)CCCn1cc(-c2ccc(-c3cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
91934897 26947 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1295 32 10 14 6.9 N/C(=N/C(=O)CCCn1cc(-c2ccc(-c3cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
CHEMBL1187385 26947 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1295 32 10 14 6.9 N/C(=N/C(=O)CCCn1cc(-c2ccc(-c3cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c4ccccc4)c4ccccc4)C(=O)NCc4ccc(O)cc4)nn3)cc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
45268483 387255 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 599 7 1 4 6.3 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)(F)F)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL538380 387255 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 599 7 1 4 6.3 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)(F)F)cc1 10.1016/j.bmcl.2009.06.050
10624769 473519 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 485 6 4 3 4.9 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88742 473519 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 485 6 4 3 4.9 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
10722606 474362 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 1 6 5.9 Clc1ccc(OCc2nc3c(OCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL94292 474362 0 None None None Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 1 6 5.9 Clc1ccc(OCc2nc3c(OCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL2440917 477829 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1539 52 19 14 4.0 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CCCC(=O)NCCN(CCN)CCNC(=O)CCCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040656 477829 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1539 52 19 14 4.0 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)CCCC(=O)NCCN(CCN)CCNC(=O)CCCC(=O)NCCCCNC(=O)NCc2ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c3ccccc3)c3ccccc3)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL265426 486162 0 None 77 2 Human 7.4 pKi = 7.4 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2765 87 38 34 -4.3 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
45271861 389726 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 533 6 1 3 5.9 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccc(F)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL549917 389726 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 533 6 1 3 5.9 C[C@@H](N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1)c1ccc(F)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL3349022 484266 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
10625004 222527 1 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 493 6 0 5 5.1 Cn1c(COc2ccc(Cl)cc2)c(C(=O)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
CHEMBL331202 222527 1 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 493 6 0 5 5.1 Cn1c(COc2ccc(Cl)cc2)c(C(=O)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
CHEMBL2440192 477814 0 None -831 3 Human 6.4 pKi = 6.4 Binding
Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry
ChEMBL 4151 126 58 57 -15.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](N)Cc1ccc(O)cc1 10.1021/jm4008505
131886627 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
155524657 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
85472343 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4456247 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4475071 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4577373 335533 0 None -457 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
24868176 484361 19 None -2089 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 4179 127 58 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
CHEMBL4540843 484361 19 None -2089 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 4179 127 58 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
24868176 484361 19 None -2089 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 4179 127 58 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
CHEMBL4540843 484361 19 None -2089 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 4179 127 58 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
45271838 390194 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 546 7 2 4 5.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCNC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL551933 390194 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 546 7 2 4 5.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(N4CCCNC4=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
162655171 367007 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802928 367007 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44362773 66432 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 424 8 1 5 4.5 CN(C)C1CCN(CCc2c(COc3ccccc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL141442 66432 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 424 8 1 5 4.5 CN(C)C1CCN(CCc2c(COc3ccccc3CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
44362764 81114 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 472 7 0 4 5.8 CN(C)C1CCN(CCc2c(COc3ccccc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145726 81114 0 None None None Human 6.4 pKi = 6.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 472 7 0 4 5.8 CN(C)C1CCN(CCc2c(COc3ccccc3Br)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10552954 216560 0 None None None Human 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 5.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(OC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314637 216560 0 None None None Human 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 5.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(OC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
44362765 80738 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 474 7 1 5 6.2 CN(C)C1CCN(CCc2c(/C=N/Nc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145392 80738 0 None None None Human 5.4 pKi = 5.4 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 474 7 1 5 6.2 CN(C)C1CCN(CCc2c(/C=N/Nc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
46231126 408345 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 2031 71 25 26 -0.7 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
91937010 408345 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 2031 71 25 26 -0.7 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
CHEMBL577447 408345 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 2031 71 25 26 -0.7 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CCN(CC(=O)NCCCCCCCC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
164616390 368573 0 None -234 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 1093 27 20 14 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
CHEMBL4858915 368573 0 None -234 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 1093 27 20 14 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
CHEMBL438548 488722 0 None -4 2 Human 7.3 pKi = 7.3 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 1759 55 26 22 -4.0 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CSSC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
49865800 40034 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 711 25 6 5 8.2 CCCCCCCCCCCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1223987 40034 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 711 25 6 5 8.2 CCCCCCCCCCCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
1507 5870 0 None -346 7 Human 6.3 pKi = 6.3 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
44351001 5870 0 None -346 7 Human 6.3 pKi = 6.3 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL265849 5870 0 None -346 7 Human 6.3 pKi = 6.3 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
46879876 20401 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1080655 20401 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
45273649 391893 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 531 7 1 4 5.2 COc1ccc(CN[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL557932 391893 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 531 7 1 4 5.2 COc1ccc(CN[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
10601025 221839 0 None None None Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 487 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)COc3ccccc32)c1 10.1021/jm990044m
CHEMBL329425 221839 0 None None None Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 487 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)COc3ccccc32)c1 10.1021/jm990044m
9820766 330142 28 None None None Human 7.3 pKi = 7.3 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 371 4 1 6 3.7 CC(C)c1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
CHEMBL422942 330142 28 None None None Human 7.3 pKi = 7.3 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 371 4 1 6 3.7 CC(C)c1ccccc1S(=O)(=O)c1cc(N)c2ncccc2c1[N+](=O)[O-] 10.1016/0960-894X(96)00319-8
45273630 391453 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 504 8 2 4 6.3 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(NC(C)=O)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL556915 391453 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 504 8 2 4 6.3 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(NC(C)=O)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL2440914 477839 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1701 52 17 18 4.1 NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040731 477839 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1701 52 17 18 4.1 NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
46879690 20445 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 396 7 2 6 5.6 CCCC1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1080826 20445 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 396 7 2 6 5.6 CCCC1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
21336495 202125 0 None -1737 2 Human 4.3 pKi = 4.3 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccnc3ccccc23)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL301747 202125 0 None -1737 2 Human 4.3 pKi = 4.3 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccnc3ccccc23)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL3349022 484266 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL429071 488537 0 None 81 2 Human 7.3 pKi = 7.3 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2367 77 34 32 -5.7 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
44588507 26731 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 686 16 5 7 4.3 N/C(=N/C(=O)CCCn1cc(-c2ccccc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
CHEMBL1186145 26731 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 686 16 5 7 4.3 N/C(=N/C(=O)CCCn1cc(-c2ccccc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
45269305 392686 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 518 8 1 4 6.7 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(c4ccccc4)(N(C)C(C)=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL561193 392686 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 518 8 1 4 6.7 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)C3CCC(c4ccccc4)(N(C)C(C)=O)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL386823 487705 14 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for cloned Y1 receptor using [125I]PYY as radioligandAffinity for cloned Y1 receptor using [125I]PYY as radioligand
ChEMBL 1206 36 16 15 -2.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](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)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC 10.1021/jm010031k
54583518 124405 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 477 7 2 7 4.9 COc1cc(Cl)c(-c2c(C)nn3c(NCC(C)NC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771262 124405 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 477 7 2 7 4.9 COc1cc(Cl)c(-c2c(C)nn3c(NCC(C)NC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
9956814 124407 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 479 7 2 6 5.6 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCCCC4F)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771264 124407 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 479 7 2 6 5.6 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCCCC4F)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL591971 489306 0 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1207 36 18 15 -1.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2009.12.068
171351388 386915 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 600 10 3 9 4.0 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(N/C(=N/C#N)NCCCN2CCC(c3cccc(OC)c3)CC2)c1 10.1039/D1MD00058F
CHEMBL5288617 386915 0 None None None Human 8.3 pKi = 8.3 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 600 10 3 9 4.0 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(N/C(=N/C#N)NCCCN2CCC(c3cccc(OC)c3)CC2)c1 10.1039/D1MD00058F
3474 7886 30 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cellsDisplacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
5311023 7886 30 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cellsDisplacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
CHEMBL332347 7886 30 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cellsDisplacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1016/j.bmc.2011.03.045
9807379 473571 0 None None None Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ncsc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL89078 473571 0 None None None Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ncsc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL437656 488676 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3339 89 46 47 -13.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@H](C)CC 10.1021/jm00055a010
CHEMBL3349022 484266 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL3349022 484266 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
21188533 332958 0 None None None Human 8.2 pKi = 8.2 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 12 0 5 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL433734 332958 0 None None None Human 8.2 pKi = 8.2 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 12 0 5 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL3349022 484266 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL2440182 477808 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Y1 receptor (unknown origin)Binding affinity to Y1 receptor (unknown origin)
ChEMBL 1769 54 29 25 -8.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]2[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)[C@H]2C(=O)OC)[C@H]1C(=O)OC 10.1021/jm4008505
CHEMBL4276961 478127 0 None -5011 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4180 127 58 57 -15.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
11560009 20343 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 5 2 6 5.2 CC1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1080291 20343 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 5 2 6 5.2 CC1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
54581331 125862 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 848 21 5 5 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789555 125862 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 848 21 5 5 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL2440928 477831 0 None 7 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1633 56 17 18 2.6 NCCN(CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040658 477831 0 None 7 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human MCF7 cells
ChEMBL 1633 56 17 18 2.6 NCCN(CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCC(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL4276961 478127 0 None -5011 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4180 127 58 57 -15.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 478149 0 None -389 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 478154 0 None -251 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2249 50 37 31 -8.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4282616 478166 0 None -100 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4048 129 60 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291016 478211 0 None -50 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 478149 0 None -389 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 478154 0 None -251 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2249 50 37 31 -8.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4282616 478166 0 None -100 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4048 129 60 56 -16.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291016 478211 0 None -50 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 129 60 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL124151 40507 0 None None None Human 6.3 pKi = 6.3 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 589 10 3 8 5.1 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1016/s0960-894x(01)00761-2
49865813 40047 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 628 17 9 6 2.8 N=C(N)NCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
CHEMBL1224001 40047 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 628 17 9 6 2.8 N=C(N)NCCCCCC(=O)NC(=N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2010.07.028
21188533 332958 0 None None None Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 12 0 5 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL433734 332958 0 None None None Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 536 12 0 5 7.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCCN2CCCCC2)CC1 10.1016/s0960-894x(98)00048-1
21188571 333997 0 None None None Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 411 7 0 4 5.7 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(C)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL442412 333997 0 None None None Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 411 7 0 4 5.7 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(C)CC1 10.1016/s0960-894x(98)00048-1
162654570 367003 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4802896 367003 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
46879610 20197 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 446 6 2 8 4.3 CS(=O)(=O)c1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079388 20197 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 446 6 2 8 4.3 CS(=O)(=O)c1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL337939 235706 0 None None None Human 6.3 pKi = 6.3 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 484 8 3 7 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCCCC2)c1 10.1016/s0960-894x(01)00761-2
46879522 20255 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 399 6 2 8 4.4 O=[N+]([O-])c1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079729 20255 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 399 6 2 8 4.4 O=[N+]([O-])c1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
11654472 20344 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 6 2 6 5.9 CC(C)C1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1080292 20344 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 6 2 6 5.9 CC(C)C1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL2440913 477838 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1581 44 17 14 5.6 NCCN(CCNC(=O)c1ccc(C(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040730 477838 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1581 44 17 14 5.6 NCCN(CCNC(=O)c1ccc(C(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
10839529 328774 0 None None None Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 399 7 2 5 4.8 Oc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1 10.1021/jm9706630
CHEMBL420613 328774 0 None None None Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 399 7 2 5 4.8 Oc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1 10.1021/jm9706630
46879781 20402 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1080660 20402 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
11670084 20607 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 474 7 2 7 6.6 COc1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1081711 20607 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 474 7 2 7 6.6 COc1ccc(C2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
10601682 328621 0 None None None Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 506 7 3 4 4.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NS(=O)(=O)c3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL420426 328621 0 None None None Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 506 7 3 4 4.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NS(=O)(=O)c3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
9806472 317491 0 None -257 2 Human 5.3 pKi = 5.3 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
CHEMBL415926 317491 0 None -257 2 Human 5.3 pKi = 5.3 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
10671331 40353 0 None None None Human 6.3 pKi = 6.3 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 451 6 0 4 5.9 Cn1c(COc2ccc(Cl)cc2)c(CN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
CHEMBL123413 40353 0 None None None Human 6.3 pKi = 6.3 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 451 6 0 4 5.9 Cn1c(COc2ccc(Cl)cc2)c(CN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
54586222 125838 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1743 49 14 14 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
91932454 125838 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1743 49 14 14 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789351 125838 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1743 49 14 14 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCNC(=O)CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10816198 215619 0 None None None Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 536 6 4 4 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ncccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL312841 215619 0 None None None Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 536 6 4 4 5.4 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ncccc4c3)CCc3ccccc32)c1 10.1021/jm990044m
10625178 216608 0 None None None Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 6 4 3 5.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314961 216608 0 None None None Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 6 4 3 5.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCCc3ccccc32)c1 10.1021/jm990044m
162670721 367085 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
CHEMBL4803781 367085 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
ChEMBL 663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1039/c9md00538b
44363018 240564 0 None None None Human 5.3 pKi = 5.3 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 460 6 0 4 6.0 CN(C)C1CCN(CCc2c(C(=O)c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL359174 240564 0 None None None Human 5.3 pKi = 5.3 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 460 6 0 4 6.0 CN(C)C1CCN(CCc2c(C(=O)c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
21188733 238195 0 None None None Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 515 11 0 4 7.7 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL344971 238195 0 None None None Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 515 11 0 4 7.7 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCc2ccccc2)CC1 10.1016/s0960-894x(98)00048-1
19426762 385953 0 None None None Human 7.2 pKi = 7.2 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 347 3 1 6 2.7 Nc1cc(S(=O)(=O)c2ccccc2F)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL52643 385953 0 None None None Human 7.2 pKi = 7.2 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 347 3 1 6 2.7 Nc1cc(S(=O)(=O)c2ccccc2F)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
44588503 26973 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1439 46 10 19 5.3 N/C(=N/C(=O)CCCn1cc(COCCOCCOCCOCCOCc2cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
49797584 26973 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1439 46 10 19 5.3 N/C(=N/C(=O)CCCn1cc(COCCOCCOCCOCCOCc2cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
CHEMBL1187587 26973 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1439 46 10 19 5.3 N/C(=N/C(=O)CCCn1cc(COCCOCCOCCOCCOCc2cn(CCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c3ccccc3)c3ccccc3)C(=O)NCc3ccc(O)cc3)nn2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
44362628 81069 0 None None None Human 5.2 pKi = 5.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 538 8 0 4 7.9 CN(C)C1CCN(CCc2c(C(Oc3ccc(Cl)cc3Cl)c3ccccc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145686 81069 0 None None None Human 5.2 pKi = 5.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 538 8 0 4 7.9 CN(C)C1CCN(CCc2c(C(Oc3ccc(Cl)cc3Cl)c3ccccc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
49865803 40036 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 949 25 8 10 4.2 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)COCCOCCOCC(=O)NCCNC(=O)C1=C2C=Cc3cccc4c3C2C(=CC4)C=C1 10.1016/j.bmc.2010.07.028
CHEMBL1223990 40036 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 949 25 8 10 4.2 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)COCCOCCOCC(=O)NCCNC(=O)C1=C2C=Cc3cccc4c3C2C(=CC4)C=C1 10.1016/j.bmc.2010.07.028
46879523 20256 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 432 6 2 8 3.9 CS(=O)(=O)c1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1079730 20256 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 432 6 2 8 3.9 CS(=O)(=O)c1ccc2nc(NCCc3ccc(NC4=NCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
15383698 372281 0 None None None Human 6.2 pKi = 6.2 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 343 3 1 6 2.9 Cc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
CHEMBL51048 372281 0 None None None Human 6.2 pKi = 6.2 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 343 3 1 6 2.9 Cc1ccc(S(=O)(=O)c2cc(N)c3ncccc3c2[N+](=O)[O-])cc1 10.1016/0960-894X(96)00319-8
10747659 222086 0 None None None Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@@H]4CCCNC4)cccc3n2CCC[C@@H]2CCCNC2)cc1 10.1021/jm9706630
CHEMBL330223 222086 0 None None None Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 524 12 2 6 6.2 Clc1ccc(OCc2nc3c(OCCC[C@@H]4CCCNC4)cccc3n2CCC[C@@H]2CCCNC2)cc1 10.1021/jm9706630
44588505 26725 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1133 32 10 11 4.1 N/C(=N/C(=O)COCCOCCOCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
CHEMBL1186104 26725 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cellsDisplacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells
ChEMBL 1133 32 10 11 4.1 N/C(=N/C(=O)COCCOCCOCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2008.09.033
CHEMBL3349022 484266 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL3349022 484266 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
49865809 40042 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 639 16 7 9 2.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCn1cc(CN)nn1 10.1016/j.bmc.2010.07.028
CHEMBL1223997 40042 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 639 16 7 9 2.3 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCn1cc(CN)nn1 10.1016/j.bmc.2010.07.028
127041012 274542 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 673 14 6 7 3.5 N/C(=N/C(=O)NCc1cn(-c2ccccc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747817 274542 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK114 from NPY1R in human SK-N-MC cells by radioligand binding assay
ChEMBL 673 14 6 7 3.5 N/C(=N/C(=O)NCc1cn(-c2ccccc2)nn1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL429159 488538 0 None -100 2 Human 7.2 pKi = 7.2 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3339 89 46 47 -13.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@H](C)CC 10.1021/jm00055a010
54584307 125835 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1601 43 12 12 9.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
91932452 125835 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1601 43 12 12 9.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789347 125835 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1601 43 12 12 9.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN(CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)CCNC(=O)CCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10554910 215833 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 561 7 4 3 6.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(-c4ccccc4)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL313612 215833 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 561 7 4 3 6.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(-c4ccccc4)cc3)CCc3ccccc32)c1 10.1021/jm990044m
46879563 20509 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 5 2 6 5.2 Cc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
CHEMBL1081181 20509 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 382 5 2 6 5.2 Cc1ccc2nc(NCCc3ccc(NC4=NCCCS4)cc3)sc2c1 10.1016/j.bmcl.2009.09.048
11669044 20347 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 424 7 2 6 6.3 CC(C)CC1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1080300 20347 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 424 7 2 6 6.3 CC(C)CC1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL592100 489307 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1608 47 22 23 -5.1 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
CHEMBL2440923 477819 0 None 31 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1085 29 10 8 6.4 N/C(=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL4277590 478130 0 None -1258 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4050 129 60 55 -15.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277676 478132 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277590 478130 0 None -1258 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4050 129 60 55 -15.8 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277676 478132 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 478187 0 None -2511 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290891 478210 0 None -199 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 478187 0 None -2511 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290891 478210 0 None -199 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 4062 130 61 56 -15.9 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL2440916 477832 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1757 54 17 18 4.7 CCC(=O)NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040674 477832 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 1757 54 17 18 4.7 CCC(=O)NCCN(CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1)CCNC(=O)c1ccc(C(=O)NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1 10.1016/j.bmc.2013.08.065
10554549 470841 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 544 8 6 5 3.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(\NCCO)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL85297 470841 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 544 8 6 5 3.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(/N=C(\NCCO)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
44362878 240569 0 None None None Human 5.2 pKi = 5.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 432 5 0 3 6.4 CN(C)C1CCN(CCc2c(-c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL359192 240569 0 None None None Human 5.2 pKi = 5.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 432 5 0 3 6.4 CN(C)C1CCN(CCc2c(-c3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10649849 332740 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 528 7 4 4 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(N(C)C)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL431990 332740 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 528 7 4 4 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(N(C)C)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL124275 40572 0 None None None Human 7.2 pKi = 7.2 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 575 10 3 8 4.8 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(01)00761-2
44362460 77549 0 None None None Human 6.2 pKi = 6.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 515 9 1 5 5.5 CNCc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142495 77549 0 None None None Human 6.2 pKi = 6.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 515 9 1 5 5.5 CNCc1cc(Br)ccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL3349022 484266 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL340209 236643 0 None None None Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 643 10 3 8 6.1 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL124953 40754 0 None None None Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 558 9 3 8 4.8 CO/C(O)=C1\C(C)=NC(C)=C(C#N)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
46879691 20446 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 8 2 6 6.0 CCCCC1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1080827 20446 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 8 2 6 6.0 CCCCC1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
44362815 237986 0 None None None Human 6.2 pKi = 6.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.9 CC(CN1CCC(N(C)C)CC1)c1c(COc2ccc(Cl)cc2Cl)sc2ccccc12 10.1016/s0960-894x(99)00019-0
CHEMBL343313 237986 0 None None None Human 6.2 pKi = 6.2 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 476 7 0 4 6.9 CC(CN1CCC(N(C)C)CC1)c1c(COc2ccc(Cl)cc2Cl)sc2ccccc12 10.1016/s0960-894x(99)00019-0
10578417 332741 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nc4ccccc4s3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL431994 332741 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 542 6 4 5 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3nc4ccccc4s3)CCc3ccccc32)c1 10.1021/jm990044m
10838640 470773 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 5.3 CC(C)OC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL84632 470773 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 3 4 5.3 CC(C)OC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
9932616 124401 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 433 6 2 6 4.5 Cc1cc(NCCNC2CCOCC2)n2nc(C)c(-c3c(Cl)cccc3Cl)c2n1 10.1016/j.bmcl.2010.12.116
CHEMBL1771258 124401 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 433 6 2 6 4.5 Cc1cc(NCCNC2CCOCC2)n2nc(C)c(-c3c(Cl)cccc3Cl)c2n1 10.1016/j.bmcl.2010.12.116
CHEMBL592121 489309 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 minsDisplacement of [125I]NPY from human neuropeptide Y1 receptor expressed in human MCF7 cells after 40 mins
ChEMBL 1222 38 19 16 -2.7 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1016/j.bmcl.2009.12.068
10747569 473938 0 None None None Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 5.8 Clc1ccc(OCc2nc3c(OCCC4CCNCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL91462 473938 0 None None None Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 510 11 2 6 5.8 Clc1ccc(OCc2nc3c(OCCC4CCNCC4)cccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
45269316 393047 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL561999 393047 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
72205287 202610 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 647 19 7 7 1.7 NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040665 202610 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 647 19 7 7 1.7 NCCOCCOCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
9806521 196883 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 514 6 5 4 4.5 C/N=C(/Nc1ccc(O)cc1)NC1CCc2ccccc2N(Cc2cccc(NC(=O)NC(C)C)c2)C1=O 10.1021/jm990044m
CHEMBL262904 196883 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 514 6 5 4 4.5 C/N=C(/Nc1ccc(O)cc1)NC1CCc2ccccc2N(Cc2cccc(NC(=O)NC(C)C)c2)C1=O 10.1021/jm990044m
45270973 389640 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 524 7 1 3 7.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL549851 389640 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 524 7 1 3 7.1 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4ccccc4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL2371908 477714 0 None -151 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1707 55 26 22 -3.7 CC(C)C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)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)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050907d
10601584 216811 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 503 6 4 3 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3F)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL316366 216811 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 503 6 4 3 5.0 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3F)CCc3ccccc32)c1 10.1021/jm990044m
10768834 216563 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 541 6 4 4 6.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ccsc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314656 216563 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 541 6 4 4 6.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ccsc4c3)CCc3ccccc32)c1 10.1021/jm990044m
10768322 391897 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(F)cc3F)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL557948 391897 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(F)cc3F)CCc3ccccc32)c1 10.1021/jm990044m
10649770 473246 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 4 4 5.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ccoc4c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL86898 473246 0 None None None Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 525 6 4 4 5.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4ccoc4c3)CCc3ccccc32)c1 10.1021/jm990044m
10601376 473984 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.0 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
CHEMBL91738 473984 0 None None None Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.0 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCCNC2)cc1 10.1021/jm9706630
10741628 473625 0 None None None Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 437 6 4 3 3.9 CC(C)NC(=O)Nc1cccc(CN2CCCCC(NC(=O)Nc3ccccc3)C2=O)c1 10.1021/jm990044m
CHEMBL89460 473625 0 None None None Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 437 6 4 3 3.9 CC(C)NC(=O)Nc1cccc(CN2CCCCC(NC(=O)Nc3ccccc3)C2=O)c1 10.1021/jm990044m
10786219 216800 0 None None None Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 0 4 5.1 Clc1ccc(OCc2nc3ccccc3n2CCCN2CCCCC2)cc1 10.1021/jm9706630
CHEMBL316291 216800 0 None None None Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 0 4 5.1 Clc1ccc(OCc2nc3ccccc3n2CCCN2CCCCC2)cc1 10.1021/jm9706630
73354088 202632 0 None 52 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 903 31 10 10 0.6 NCCCOCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
73355615 202632 0 None 52 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 903 31 10 10 0.6 NCCCOCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040752 202632 0 None 52 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 903 31 10 10 0.6 NCCCOCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040785 202632 0 None 52 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 903 31 10 10 0.6 NCCCOCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
10744516 473390 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 519 6 4 3 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL87896 473390 0 None None None Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 519 6 4 3 5.5 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)CCc3ccccc32)c1 10.1021/jm990044m
46879692 19834 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 7 2 6 5.9 CC(C)C[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1076276 19834 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 410 7 2 6 5.9 CC(C)C[C@@H]1CSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
44362831 237898 0 None None None Human 6.1 pKi = 6.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 540 7 0 4 6.8 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C(F)(F)F)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL342751 237898 0 None None None Human 6.1 pKi = 6.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 540 7 0 4 6.8 CN(C)C1CCN(CCc2c(COc3ccc(Br)cc3C(F)(F)F)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
127029975 276542 0 None -144 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1675 55 28 20 -1.9 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787766 276542 0 None -144 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1675 55 28 20 -1.9 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
49865811 40044 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 700 21 8 7 3.7 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(=O)O 10.1016/j.bmc.2010.07.028
CHEMBL1223999 40044 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells
ChEMBL 700 21 8 7 3.7 N=C(NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1)NC(=O)CCCCCCC(=O)NCCC(=O)O 10.1016/j.bmc.2010.07.028
72205853 202612 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 713 21 9 6 2.1 CCC(=O)NCC(=O)NCCCCNC(=O)NCc1ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040669 202612 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 713 21 9 6 2.1 CCC(=O)NCC(=O)NCCCCNC(=O)NCc1ccc(CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)C(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmc.2013.08.065
10599930 221044 0 None None None Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 457 5 4 3 4.1 CNC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL328000 221044 0 None None None Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 457 5 4 3 4.1 CNC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
44294942 369793 0 None -58 2 Human 5.1 pKi = 5.1 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 446 11 2 3 5.6 O=S(=O)(NCCCCCCNCc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
CHEMBL48777 369793 0 None -58 2 Human 5.1 pKi = 5.1 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 1
ChEMBL 446 11 2 3 5.6 O=S(=O)(NCCCCCCNCc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
44362412 80887 0 None None None Human 6.1 pKi = 6.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 7 0 4 6.1 CN(C)C1CCN(CCc2c(COc3ccc(C(F)(F)F)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145510 80887 0 None None None Human 6.1 pKi = 6.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 462 7 0 4 6.1 CN(C)C1CCN(CCc2c(COc3ccc(C(F)(F)F)cc3)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
10720174 473429 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 7 4 3 5.1 CC(C)CNC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL88141 473429 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 499 7 4 3 5.1 CC(C)CNC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL3104112 477874 0 None -83 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to NPYY1 receptor (unknown origin)Binding affinity to NPYY1 receptor (unknown origin)
ChEMBL 4057 159 50 64 -11.5 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)c1cccnc1SCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2013.11.061
164616390 368573 0 None -234 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 1093 27 20 14 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
CHEMBL4858915 368573 0 None -234 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]UR-MK299 from human neuropeptide Y Y1 receptor in human SK-N-MC cells measured after 90 mins by scintillation counting analysis
ChEMBL 1093 27 20 14 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
73349570 202619 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 845 27 10 9 0.2 NCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
73352596 202619 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 845 27 10 9 0.2 NCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040698 202619 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 845 27 10 9 0.2 NCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040699 202619 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 845 27 10 9 0.2 NCCOCCOCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
44362863 80517 0 None None None Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 486 7 0 4 6.1 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(Br)c1 10.1016/s0960-894x(99)00019-0
CHEMBL145205 80517 0 None None None Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 486 7 0 4 6.1 Cc1ccc(OCc2sc3ccccc3c2CCN2CCC(N(C)C)CC2)c(Br)c1 10.1016/s0960-894x(99)00019-0
10531064 216666 0 None None None Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 568 6 4 5 4.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)C(=O)N(C)C4=O)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL315378 216666 0 None None None Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 568 6 4 5 4.1 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc4c(c3)C(=O)N(C)C4=O)CCc3ccccc32)c1 10.1021/jm990044m
10719643 222281 0 None None None Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.8 Clc1ccc(OCc2nc3ccccc3n2CCC2CCCCN2)cc1 10.1021/jm9706630
CHEMBL330703 222281 0 None None None Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.8 Clc1ccc(OCc2nc3ccccc3n2CCC2CCCCN2)cc1 10.1021/jm9706630
45270156 389580 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccccc1[C@@H](C)N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1 10.1016/j.bmcl.2009.06.050
CHEMBL549377 389580 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 545 7 1 4 5.7 COc1ccccc1[C@@H](C)N[C@@H]1CC[C@@H](C(=O)N2CCC(C(=O)N3CCCC3)(c3ccccc3)CC2)C(C)(C)C1 10.1016/j.bmcl.2009.06.050
44362704 80450 0 None None None Human 5.1 pKi = 5.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 456 4 0 3 6.2 CN(C)C1CCN(CCc2c(C#Cc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL145161 80450 0 None None None Human 5.1 pKi = 5.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 456 4 0 3 6.2 CN(C)C1CCN(CCc2c(C#Cc3ccc(Cl)cc3Cl)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL4282168 478163 0 None -2511 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 1737 54 29 23 -5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282168 478163 0 None -2511 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 1737 54 29 23 -5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
9805674 124404 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 491 9 2 7 5.3 CCCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
CHEMBL1771261 124404 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cellsDisplacement of [125I]-PYY from human recombinant NPY Y1 receptor overexpressed in membrane of Sf9 cells
ChEMBL 491 9 2 7 5.3 CCCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1 10.1016/j.bmcl.2010.12.116
155546907 347725 0 None 19 2 Human 8.1 pKi = 8.1 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2379 58 36 30 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL4534028 347725 0 None 19 2 Human 8.1 pKi = 8.1 Binding
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assayDisplacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
ChEMBL 2379 58 36 30 -6.0 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c00027
CHEMBL2371911 477717 0 None -29 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1723 55 26 20 -3.8 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
10577766 222258 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 515 7 4 4 4.9 COc1ccc(NC(=O)NC2CCc3ccccc3N(Cc3cccc(NC(=O)NC(C)C)c3)C2=O)cc1 10.1021/jm990044m
CHEMBL330574 222258 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 515 7 4 4 4.9 COc1ccc(NC(=O)NC2CCc3ccccc3N(Cc3cccc(NC(=O)NC(C)C)c3)C2=O)cc1 10.1021/jm990044m
10696766 332769 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 501 6 5 4 4.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL432188 332769 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 501 6 5 4 4.6 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc(O)cc3)CCc3ccccc32)c1 10.1021/jm990044m
10838641 473228 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccncc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL86775 473228 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 486 6 4 4 4.3 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccncc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL271525 198032 0 None None None Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 574 10 3 7 5.6 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL3349022 484266 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
73349568 202620 0 None 38 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 828 24 11 8 -0.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
73354092 202620 0 None 38 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 828 24 11 8 -0.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040703 202620 0 None 38 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 828 24 11 8 -0.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040743 202620 0 None 38 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 828 24 11 8 -0.3 NCCC(=O)NCCNC(=O)CCC(=O)NCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1 10.1016/j.bmc.2013.08.065
10554007 333568 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cc(F)cc(F)c3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL438777 333568 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 521 6 4 3 5.2 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3cc(F)cc(F)c3)CCc3ccccc32)c1 10.1021/jm990044m
44351120 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
44351146 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929372 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
91929377 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL437671 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
CHEMBL440824 333455 0 None -7 2 Human 7.1 pKi = 7.1 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3255 89 45 45 -10.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCCCCCCCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
21188674 77812 0 None None None Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 482 11 1 5 5.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(N)=O)CC1 10.1016/s0960-894x(98)00048-1
CHEMBL142720 77812 0 None None None Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.Binding affinity at cloned Neuropeptide Y-1 receptor expressed in AV-12 cells is evaluated.
ChEMBL 482 11 1 5 5.3 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCN(CCCC(N)=O)CC1 10.1016/s0960-894x(98)00048-1
10673787 216602 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 530 7 4 5 4.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc([N+](=O)[O-])cc3)CCc3ccccc32)c1 10.1021/jm990044m
CHEMBL314926 216602 0 None None None Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 530 7 4 5 4.8 CC(C)NC(=O)Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccc([N+](=O)[O-])cc3)CCc3ccccc32)c1 10.1021/jm990044m
44362839 67423 0 None None None Human 4.1 pKi = 4.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 318 5 1 4 3.0 CN(C)C1CCN(CCc2c(CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL142292 67423 0 None None None Human 4.1 pKi = 4.1 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 318 5 1 4 3.0 CN(C)C1CCN(CCc2c(CO)sc3ccccc23)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL341329 237274 0 None None None Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 574 10 3 7 5.9 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3ccccc3)CC2)c1 10.1016/s0960-894x(01)00761-2
45271828 390020 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 516 7 1 6 5.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4nnco4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
CHEMBL551132 390020 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation countingDisplacement of [125I]PYY from human recombinant neuropeptide Y1 receptor expressed in CHO (NFAT-bla) cells by scintillation counting
ChEMBL 516 7 1 6 5.5 COc1ccc([C@@H](C)N[C@@H]2CC[C@@H](C(=O)N3CCC(c4ccccc4)(c4nnco4)CC3)C(C)(C)C2)cc1 10.1016/j.bmcl.2009.06.050
72205669 202631 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 686 20 10 6 1.7 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)NCCN)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040749 202631 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 686 20 10 6 1.7 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(=O)NCCCCNC(=O)NCCN)cc1 10.1016/j.bmc.2013.08.065
19426755 202046 0 None None None Human 6.1 pKi = 6.1 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2cccc(Cl)c2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL301150 202046 0 None None None Human 6.1 pKi = 6.1 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2cccc(Cl)c2)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL3349022 484266 0 None -3 2 Human 8.0 pKi = 8.0 Binding
Affinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cellsAffinity against Neuropeptide Y1 receptor on SK-N-MC human neuroblastoma cells
ChEMBL 4251 131 63 59 -17.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00076a007
CHEMBL420514 328691 0 None None None Human 8.0 pKi = 8.0 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 566 9 3 7 5.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(C3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00761-2
72205291 202628 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 615 17 7 5 3.2 NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL3040736 202628 0 None None None Human 8.0 pKi = 8 Binding
Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells
ChEMBL 615 17 7 5 3.2 NCCCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2013.08.065
CHEMBL2371911 477717 0 None -29 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]NPY from human NPY1 receptor expressed in CHO cellsDisplacement of [125I]NPY from human NPY1 receptor expressed in CHO cells
ChEMBL 1723 55 26 20 -3.8 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm050907d
10743445 220933 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 483 6 4 3 4.6 O=C(Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1)NC1CC1 10.1021/jm990044m
CHEMBL327410 220933 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cellsIn vitro binding affinity towards Neuropeptide Y receptor type 1 was determined as potency to displace [125I]-peptide YY binding to human neuroblastoma SK-N-MC cells
ChEMBL 483 6 4 3 4.6 O=C(Nc1cccc(CN2C(=O)C(NC(=O)Nc3ccccc3)CCc3ccccc32)c1)NC1CC1 10.1021/jm990044m
11798404 40223 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 465 7 0 4 5.9 Cn1c(COc2ccc(Cl)cc2)c(CCN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
CHEMBL122841 40223 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 465 7 0 4 5.9 Cn1c(COc2ccc(Cl)cc2)c(CCN2CCC(N3CCCCC3)CC2)c2ccccc21 10.1021/jm970512x
19426760 201804 0 None None None Human 7.0 pKi = 7.0 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2ccccc2Cl)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL299384 201804 0 None None None Human 7.0 pKi = 7.0 Binding
Compound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligandCompound was tested for binding affinity against neuropeptide Y1 (NPY1) receptor from SK-N-MC membranes using [125I]PYY as radioligand
ChEMBL 363 3 1 6 3.2 Nc1cc(S(=O)(=O)c2ccccc2Cl)c([N+](=O)[O-])c2cccnc12 10.1016/0960-894X(96)00319-8
CHEMBL410780 488137 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2683 79 36 30 0.3 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
131886627 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
155524657 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
85472343 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4456247 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4475071 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4577373 335533 0 None -457 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation countingDisplacement of [3H]UR-MK136 from human NPY Y1 receptor expressed in human MCF7 cells by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
10791009 473789 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.7 Clc1ccc(OCc2nc3ccccc3n2CCC2CCNCC2)cc1 10.1021/jm9706630
CHEMBL90574 473789 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 369 6 1 4 4.7 Clc1ccc(OCc2nc3ccccc3n2CCC2CCNCC2)cc1 10.1021/jm9706630
CHEMBL441204 488825 0 None 10 2 Human 7.0 pKi = 7.0 Binding
Compound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cellsCompound was tested for the displacement of [125I]-PYY (SK-N-MC) from Neuropeptide Y receptor type 1 in the membranes prepared from cells
ChEMBL 2537 79 34 30 -1.0 CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm950811r
46879824 20648 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1ccccc1C1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
CHEMBL1081890 20648 0 None None None Human 6.0 pKi = 6.0 Binding
Displacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 478 6 2 6 7.3 Clc1ccccc1C1CCSC(Nc2ccc(CCNc3nc4ccccc4s3)cc2)=N1 10.1016/j.bmcl.2009.09.048
54582350 125886 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1056 26 6 8 7.9 Cc1cc(/C=C/C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789821 125886 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 1056 26 6 8 7.9 Cc1cc(/C=C/C=C2\N(C)c3ccc4ccccc4c3C2(C)C)cc(C)[n+]1CCOCCOCCNC(=O)CCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL127962 42682 0 None None None Human 7.0 pKi = 7.0 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 589 10 3 8 5.1 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3C)CC2)c1 10.1016/s0960-894x(01)00761-2
CHEMBL427966 488498 0 None -25 2 Human 7.0 pKi = 7.0 Binding
Tested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cellsTested against neuropeptide Y1 receptors using SK-N-MC human neuroblastoma cells
ChEMBL 3317 91 46 45 -13.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/jm00055a010
54586208 125878 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 965 25 5 8 6.5 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCOCCOCCOCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
CHEMBL1789790 125878 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cellsDisplacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells
ChEMBL 965 25 5 8 6.5 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCOCCOCCOCCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/j.bmc.2011.03.045
10625562 221803 0 None None None Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 7 1 4 5.4 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1 10.1021/jm9706630
CHEMBL329224 221803 0 None None None Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 397 7 1 4 5.4 Cc1cccc2c1nc(COc1ccc(Cl)cc1)n2CCCC1CCCNC1 10.1021/jm9706630
10554658 39395 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 548 9 0 5 6.8 Clc1ccc(OCc2c(CN3CCC(N4CCCCC4)CC3)c3ccccc3n2CCN2CCCCC2)cc1 10.1021/jm970512x
CHEMBL121636 39395 0 None None None Human 7.0 pKi = 7.0 Binding
Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cellsBinding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells
ChEMBL 548 9 0 5 6.8 Clc1ccc(OCc2c(CN3CCC(N4CCCCC4)CC3)c3ccccc3n2CCN2CCCCC2)cc1 10.1021/jm970512x
44362999 239570 0 None None None Human 6.0 pKi = 6.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 434 9 0 4 5.8 C=CCc1ccccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
CHEMBL356118 239570 0 None None None Human 6.0 pKi = 6.0 Binding
Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.Ability to displace [125I]pPYY from AV12 cell line stably transfected with cloned human neuropeptide Y receptor type 1.
ChEMBL 434 9 0 4 5.8 C=CCc1ccccc1OCc1sc2ccccc2c1CCN1CCC(N(C)C)CC1 10.1016/s0960-894x(99)00019-0
10601378 473790 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.0 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCNCC2)cc1 10.1021/jm9706630
CHEMBL90605 473790 0 None None None Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YYIn vitro binding affinity towards human neuropeptide Y receptor type 1, determined by measuring its ability to displace [125]peptide YY
ChEMBL 383 7 1 4 5.0 Clc1ccc(OCc2nc3ccccc3n2CCCC2CCNCC2)cc1 10.1021/jm9706630
171351517 386904 0 None None None Human 7.0 pKi = 7 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 573 9 2 11 4.4 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(Nc2nnc(CN3CCC(c4cccc(OC)c4)CC3)o2)c1 10.1039/D1MD00058F
CHEMBL5288434 386904 0 None None None Human 7.0 pKi = 7 Binding
Displacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assayDisplacement of 125I-PYY from human neuropeptide Y Y1 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 1 hrs by competitive binding assay
ChEMBL 573 9 2 11 4.4 COC(=O)C1=CNC(C)=C(C(=O)OC)C1c1cccc(Nc2nnc(CN3CCC(c4cccc(OC)c4)CC3)o2)c1 10.1039/D1MD00058F
CHEMBL339255 235939 0 None None None Human 6.0 pKi = 6 Binding
Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membraneInhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane
ChEMBL 633 13 3 9 5.6 CCCCO/C(O)=C1\C(C)=NC(C)=C(C(=O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/s0960-894x(01)00761-2
14160 1380 35 None None None Human 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 18573246
9960164 1380 35 None None None Human 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 18573246
CHEMBL2046866 1380 35 None None None Human 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 18573246
CHEMBL324554 1380 35 None None None Human 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 10 3 8 4.7 CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC(=CC=C2)NC(=O)NCCCN3CCC(CC3)C4=CC(=CC=C4)OC)C(=O)OC 18573246
3474 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O None
5311023 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O None
CHEMBL332347 7886 30 None 10 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O None
118705601 7751 0 None -1 2 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4238 131 59 59 -18.2 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 1317848
1520 7751 0 None -1 2 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4238 131 59 59 -18.2 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 1317848
1531 7675 0 None 2 2 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 2351 58 38 30 8.8 CC[C@@H]([C@@H](C(=N[C@@H]1CCC(=NC[C@@H](N=C(O)[C@@H]2CCCN2C(=O)[C@H](CCC(=NC[C@H](N=C([C@H]2N(C1=O)CCC2)O)C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N)O)Cc1ccc(cc1)O)O)CCCNC(=N)N)O)CC(C)C)O)CCCNC(=N)N)O)Cc1ccc(cc1)O)O)O)N=C([C@H]([C@H](CC)C)N)O)C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N)O)Cc1ccc(cc1)O)O)CCCNC(=N)N)O)CC(C)C)O)CCCNC(=N)N)O)Cc1ccc(cc1)O)O)O)O)N)C 10694200
56947140 7675 0 None 2 2 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 2351 58 38 30 8.8 CC[C@@H]([C@@H](C(=N[C@@H]1CCC(=NC[C@@H](N=C(O)[C@@H]2CCCN2C(=O)[C@H](CCC(=NC[C@H](N=C([C@H]2N(C1=O)CCC2)O)C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N)O)Cc1ccc(cc1)O)O)CCCNC(=N)N)O)CC(C)C)O)CCCNC(=N)N)O)Cc1ccc(cc1)O)O)O)N=C([C@H]([C@H](CC)C)N)O)C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N[C@H](C(=N)O)Cc1ccc(cc1)O)O)CCCNC(=N)N)O)CC(C)C)O)CCCNC(=N)N)O)Cc1ccc(cc1)O)O)O)O)N)C 10694200
118705601 7751 0 None -1 2 Human 10.2 pKd None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4238 131 59 59 -18.2 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 16097949
1520 7751 0 None -1 2 Human 10.2 pKd None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4238 131 59 59 -18.2 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 16097949
1521 8011 0 None None None Mouse 8.8 pKd None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 7623780
44288922 8011 0 None None None Mouse 8.8 pKd None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 7623780
1518 7729 0 None -1 2 Rat 9.2 pKd None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 1316999
44288922 7729 0 None -1 2 Rat 9.2 pKd None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC 1316999
1504 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
44288922 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
CHEMBL438945 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
P01303 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
P07808 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
P57774 5725 8 None 6 9 Rat 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4269 132 59 60 -19.0 NCCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N)Cc1ccc(cc1)O)CCCN=C(N)N)CCC(=O)N)CCCN=C(N)N)[C@H](O)C)[C@H](CC)C)CC(C)C)CC(=O)N)[C@H](CC)C)Cc1ccc(cc1)O)Cc1c[nH]cn1)CCCN=C(N)N)CC(C)C)C)CO)Cc1ccc(cc1)O)Cc1ccc(cc1)O)CCCN=C(N)N)C)CCSC)CC(=O)O)CCC(=O)O)C)C)CC(=O)O)CCC(=O)O)CC(=O)N)CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(cc1)O)N)CO 9145427
1485 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
1485 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
1485 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
21129772 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
21129772 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
21129772 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
5311023 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
5311023 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
5311023 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
9869458 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
9869458 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
9869458 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
CHEMBL2440929 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL2440929 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
CHEMBL2440929 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
CHEMBL332347 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL332347 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
CHEMBL332347 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
CHEMBL44246 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL44246 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 8886416
CHEMBL44246 1304 7 None -2 4 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 9145427
1485 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
1485 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
21129772 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
21129772 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
5311023 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
5311023 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
9869458 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
9869458 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
CHEMBL2440929 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL2440929 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
CHEMBL332347 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL332347 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
CHEMBL44246 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562541
CHEMBL44246 1304 7 None 2 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 7562543
1549 5880 0 None 1 5 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4107 129 58 58 -18.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
155817422 5880 0 None 1 5 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4107 129 58 58 -18.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
1505 5866 0 None 1 4 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P01304 5866 0 None 1 4 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1527 4691 0 None 1 5 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1515 6213 0 None 1 6 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P10631 6213 0 None 1 6 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P68005 6213 0 None 1 6 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
Q9EPS2 6213 0 None 1 6 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1545 4687 0 None 50 4 Rat 10.6 pKi None 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1529 3787 0 None 1 5 Rat 10.9 pKi None 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1513 6116 0 None -5011 6 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P06303 6116 0 None -5011 6 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1517 6598 0 None -112 3 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P10082 6598 0 None -112 3 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1516 6596 0 None -39 5 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 3014 96 45 42 -12.9 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 9145427
57339564 6596 0 None -39 5 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 3014 96 45 42 -12.9 CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 9145427
1510 5886 0 None -31 6 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 3992 126 57 56 -18.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
155817418 5886 0 None -31 6 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 3992 126 57 56 -18.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
1507 5870 0 None -12 7 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
44351001 5870 0 None -12 7 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
CHEMBL265849 5870 0 None -12 7 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 2982 95 44 40 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 9145427
1511 6110 0 None -354 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P01302 6110 0 None -354 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1512 6112 0 None -630 6 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
P01298 6112 0 None -630 6 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145427
1530 7444 0 None None None Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 750 15 3 6 5.2 CN(C[C@@H]1CC[C@@H](CC1)C/N=C(/c1ccc(cc1)C[C@H](C(=O)N1CCCC1)NC(=O)[C@H](NS(=O)(=O)c1ccc2c(c1)cccc2)Cc1ccccc1)\N)C 16097949
5312150 7444 0 None None None Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 750 15 3 6 5.2 CN(C[C@@H]1CC[C@@H](CC1)C/N=C(/c1ccc(cc1)C[C@H](C(=O)N1CCCC1)NC(=O)[C@H](NS(=O)(=O)c1ccc2c(c1)cccc2)Cc1ccccc1)\N)C 16097949
1505 5866 0 None -1 4 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16097949
P01304 5866 0 None -1 4 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16097949