Ligand source activities (1 row/activity)



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

 Species

 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
155550061 173988 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 862 21 12 7 2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4539775 173988 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 862 21 12 7 2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152055 211757 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155547823 173691 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 795 19 11 7 1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4533110 173691 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 795 19 11 7 1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155529648 171532 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 759 19 11 7 0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4462883 171532 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 759 19 11 7 0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152060 211762 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155545453 173501 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4528114 173501 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152056 211758 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
71454755 80784 None 0 Human Functional pEC50 = 10.4 10.4 9 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80784 None 0 Human Functional pEC50 = 10.4 10.4 9 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2187 None 32 Human Functional pEC50 = 10.3 10.3 1 4
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2187 None 32 Human Functional pEC50 = 10.3 10.3 1 4
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2187 None 32 Human Functional pEC50 = 10.3 10.3 1 4
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2187 None 32 Human Functional pEC50 = 10.3 10.3 1 4
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
71461938 80787 None 0 Human Functional pEC50 = 10.3 10.3 -2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80787 None 0 Human Functional pEC50 = 10.3 10.3 -2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL3085809 213454 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155522287 170742 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 761 19 11 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4451244 170742 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 761 19 11 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2151642 211748 None 0 Human Functional pEC50 = 10.2 10.2 -3 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2187 None 32 Human Functional pEC50 = 10.2 10.2 1 4
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
1283 2187 None 32 Human Functional pEC50 = 10.2 10.2 1 4
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
25240297 2187 None 32 Human Functional pEC50 = 10.2 10.2 1 4
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL376756 2187 None 32 Human Functional pEC50 = 10.2 10.2 1 4
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL2152058 211760 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155551159 174055 None 0 Human Functional pEC50 = 10.2 10.2 17 2
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4541289 174055 None 0 Human Functional pEC50 = 10.2 10.2 17 2
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
90324535 118937 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
CHEMBL3422408 118937 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
CHEMBL3422407 214124 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
71461940 80795 None 0 Human Functional pEC50 = 10.1 10.1 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80795 None 0 Human Functional pEC50 = 10.1 10.1 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
25084920 149966 None 0 Human Functional pEC50 = 10.1 10.1 16 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949159 149966 None 0 Human Functional pEC50 = 10.1 10.1 16 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3422414 214127 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
1281 2187 None 32 Human Functional pEC50 = 10.1 10.1 1 4
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
1283 2187 None 32 Human Functional pEC50 = 10.1 10.1 1 4
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
25240297 2187 None 32 Human Functional pEC50 = 10.1 10.1 1 4
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
CHEMBL376756 2187 None 32 Human Functional pEC50 = 10.1 10.1 1 4
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
71460220 80794 None 0 Human Functional pEC50 = 10.0 10.0 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80794 None 0 Human Functional pEC50 = 10.0 10.0 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460219 80791 None 0 Human Functional pEC50 = 10 10.0 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80791 None 0 Human Functional pEC50 = 10 10.0 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL3422413 214126 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
71451197 80793 None 0 Human Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80793 None 0 Human Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155536247 172246 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 11 8 1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4473151 172246 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 11 8 1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155565826 175913 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 801 19 11 7 1.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4584512 175913 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 801 19 11 7 1.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
71460218 80790 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80790 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155527587 171322 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1025 28 15 11 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4459547 171322 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1025 28 15 11 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155559289 174975 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 747 19 11 7 0.6 CCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4563528 174975 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 747 19 11 7 0.6 CCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152061 211763 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152062 211764 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155548337 173845 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4536531 173845 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155514052 169909 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 986 28 14 11 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4439387 169909 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 986 28 14 11 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155534639 172086 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 784 19 12 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4470916 172086 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 784 19 12 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
1281 2187 None 32 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
1283 2187 None 32 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
25240297 2187 None 32 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2187 None 32 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
71449398 80789 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80789 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80792 None 0 Human Functional pEC50 = 9.6 9.6 2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80792 None 0 Human Functional pEC50 = 9.6 9.6 2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155549139 173914 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 12 8 0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4538305 173914 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 12 8 0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155533419 171922 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 809 20 11 7 1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4468499 171922 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 809 20 11 7 1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL3086284 213461 None 6 Human Functional pEC50 = 9.6 9.6 -1 2
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152052 211754 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152054 211756 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
25138123 179353 None 0 Human Functional pEC50 = 9.5 9.5 3388 3
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL472833 179353 None 0 Human Functional pEC50 = 9.5 9.5 3388 3
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
118707492 113189 None 0 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 113189 None 0 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707486 113183 None 0 Human Functional pEC50 = 9.5 9.5 7 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 113183 None 0 Human Functional pEC50 = 9.5 9.5 7 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152057 211759 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None C/N=C(/NC)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155554573 174701 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 694 18 10 7 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4557192 174701 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 694 18 10 7 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
49787129 113190 None 7 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 113190 None 7 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 113190 None 7 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 113190 None 7 Human Functional pEC50 = 9.5 9.5 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152064 211766 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152063 211765 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
25138131 173974 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL453956 173974 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL2152059 211761 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCCNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
24996490 149974 None 0 Human Functional pEC50 = 9.4 9.4 16 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949224 149974 None 0 Human Functional pEC50 = 9.4 9.4 16 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707495 113193 None 0 Human Functional pEC50 = 9.4 9.4 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 113193 None 0 Human Functional pEC50 = 9.4 9.4 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3315315 213838 None 0 Human Functional pEC50 = 9.4 9.4 2 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16735569 142421 None 0 Human Functional pEC50 = 9.4 9.4 263 3
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL388586 142421 None 0 Human Functional pEC50 = 9.4 9.4 263 3
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
25075973 153311 None 0 Human Functional pEC50 = 9.3 9.3 42 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977314 153311 None 0 Human Functional pEC50 = 9.3 9.3 42 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134132372 145187 None 0 Human Functional pEC50 = 9.3 9.3 19 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3911692 145187 None 0 Human Functional pEC50 = 9.3 9.3 19 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134150351 151807 None 0 Human Functional pEC50 = 9.3 9.3 14 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964403 151807 None 0 Human Functional pEC50 = 9.3 9.3 14 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707489 113186 None 0 Human Functional pEC50 = 9.3 9.3 13 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](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(N)=O 10.1021/jm5005489
CHEMBL3314220 113186 None 0 Human Functional pEC50 = 9.3 9.3 13 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](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(N)=O 10.1021/jm5005489
118707484 113181 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 113181 None 0 Human Functional pEC50 = 9.3 9.3 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075960 146444 None 0 Human Functional pEC50 = 9.3 9.3 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3921327 146444 None 0 Human Functional pEC50 = 9.3 9.3 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
71449399 80796 None 0 Human Functional pEC50 = 9.2 9.2 -1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80796 None 0 Human Functional pEC50 = 9.2 9.2 -1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
118707481 113178 None 0 Human Functional pEC50 = 9.2 9.2 12 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314212 113178 None 0 Human Functional pEC50 = 9.2 9.2 12 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155538456 172492 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 756 19 10 7 1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4476438 172492 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 756 19 10 7 1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118735592 118938 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(CC(=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)nn1 10.1021/jm5019675
CHEMBL3422409 118938 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(CC(=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)nn1 10.1021/jm5019675
134157013 154200 None 0 Human Functional pEC50 = 9.2 9.2 7 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985112 154200 None 0 Human Functional pEC50 = 9.2 9.2 7 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
71456524 80785 None 0 Human Functional pEC50 = 9.2 9.2 2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80785 None 0 Human Functional pEC50 = 9.2 9.2 2 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155529496 171562 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 823 21 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4463349 171562 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 823 21 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118707490 113187 None 0 Human Functional pEC50 = 9.2 9.2 20 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314221 113187 None 0 Human Functional pEC50 = 9.2 9.2 20 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707491 113188 None 0 Human Functional pEC50 = 9.2 9.2 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 113188 None 0 Human Functional pEC50 = 9.2 9.2 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075963 147330 None 0 Human Functional pEC50 = 9.2 9.2 2 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3928465 147330 None 0 Human Functional pEC50 = 9.2 9.2 2 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16735569 142421 None 0 Human Functional pEC50 = 9.2 9.2 263 3
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388586 142421 None 0 Human Functional pEC50 = 9.2 9.2 263 3
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707487 113184 None 0 Human Functional pEC50 = 9.2 9.2 13 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 113184 None 0 Human Functional pEC50 = 9.2 9.2 13 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71456525 80788 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80788 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
57653049 152203 None 0 Human Functional pEC50 = 9.1 9.1 11 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967782 152203 None 0 Human Functional pEC50 = 9.1 9.1 11 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707496 113194 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 113194 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16735730 97279 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268579 97279 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707493 113191 None 0 Human Functional pEC50 = 9.1 9.1 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 113191 None 0 Human Functional pEC50 = 9.1 9.1 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
118707494 113192 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 113192 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707476 113173 None 0 Human Functional pEC50 = 9.1 9.1 6 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 113173 None 0 Human Functional pEC50 = 9.1 9.1 6 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155518633 170424 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 781 20 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4446920 170424 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 781 20 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL3422412 214125 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
118707497 113195 None 0 Human Functional pEC50 = 9.0 9.0 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 113195 None 0 Human Functional pEC50 = 9.0 9.0 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
71461937 80786 None 0 Human Functional pEC50 = 9.0 9.0 4 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80786 None 0 Human Functional pEC50 = 9.0 9.0 4 2
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2187 None 32 Human Functional pEC50 = 9.0 9.0 1 4
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
16737378 85506 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 780 21 10 7 1.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226757 85506 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 780 21 10 7 1.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735542 169259 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 11 8 0.8 CC(=O)NCc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
CHEMBL440431 169259 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 11 8 0.8 CC(=O)NCc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
16735568 142182 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 825 22 10 9 1.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388146 142182 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 825 22 10 9 1.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707485 113182 None 0 Human Functional pEC50 = 9 9.0 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 113182 None 0 Human Functional pEC50 = 9 9.0 4 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996809 148704 None 0 Human Functional pEC50 = 9.0 9.0 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3939287 148704 None 0 Human Functional pEC50 = 9.0 9.0 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707492 113189 None 0 Rat Functional pEC50 = 9.0 9.0 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 113189 None 0 Rat Functional pEC50 = 9.0 9.0 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16736193 84842 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 10 8 1.1 COc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
CHEMBL223390 84842 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 10 8 1.1 COc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
16735543 85472 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(O)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226566 85472 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(O)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24995518 145660 None 0 Human Functional pEC50 = 8.9 8.9 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3915251 145660 None 0 Human Functional pEC50 = 8.9 8.9 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24992020 152317 None 0 Human Functional pEC50 = 8.9 8.9 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3968824 152317 None 0 Human Functional pEC50 = 8.9 8.9 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707482 113179 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 113179 None 0 Human Functional pEC50 = 8.9 8.9 10 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25084920 149966 None 0 Rat Functional pEC50 = 8.9 8.9 -16 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949159 149966 None 0 Rat Functional pEC50 = 8.9 8.9 -16 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16735779 142420 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 814 21 10 7 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388585 142420 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 814 21 10 7 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707488 113185 None 0 Human Functional pEC50 = 8.9 8.9 24 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314219 113185 None 0 Human Functional pEC50 = 8.9 8.9 24 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
49787129 113190 None 7 Rat Functional pEC50 = 8.9 8.9 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 113190 None 7 Rat Functional pEC50 = 8.9 8.9 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 113190 None 7 Rat Functional pEC50 = 8.9 8.9 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 113190 None 7 Rat Functional pEC50 = 8.9 8.9 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3315315 213838 None 0 Rat Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
10328205 85851 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 13 8 0.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229621 85851 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 13 8 0.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
155535993 172213 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 750 22 10 7 1.3 CCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4472672 172213 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 750 22 10 7 1.3 CCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
25075965 147554 None 0 Human Functional pEC50 = 8.9 8.9 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3930297 147554 None 0 Human Functional pEC50 = 8.9 8.9 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152048 211750 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152066 211768 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155541282 173116 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 987 28 14 12 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4518378 173116 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 987 28 14 12 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118707480 113177 None 0 Human Functional pEC50 = 8.8 8.8 14 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314211 113177 None 0 Human Functional pEC50 = 8.8 8.8 14 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152049 211751 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
16735508 85485 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226633 85485 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24996486 150849 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956437 150849 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707477 113174 None 0 Human Functional pEC50 = 8.8 8.8 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 113174 None 0 Human Functional pEC50 = 8.8 8.8 3 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118735685 118951 None 0 Human Functional pEC50 = 8.8 8.8 141 2
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL3422516 118951 None 0 Human Functional pEC50 = 8.8 8.8 141 2
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
16736170 85533 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 837 22 13 8 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL227165 85533 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 837 22 13 8 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735729 97288 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268659 97288 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16738337 97289 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 770 21 11 8 -0.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268660 97289 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 770 21 11 8 -0.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707495 113193 None 0 Rat Functional pEC50 = 8.8 8.8 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 113193 None 0 Rat Functional pEC50 = 8.8 8.8 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24994272 153296 None 0 Human Functional pEC50 = 8.7 8.7 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977235 153296 None 0 Human Functional pEC50 = 8.7 8.7 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707478 113175 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 113175 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075963 147330 None 0 Rat Functional pEC50 = 8.7 8.7 -2 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3928465 147330 None 0 Rat Functional pEC50 = 8.7 8.7 -2 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134154824 151022 None 0 Human Functional pEC50 = 8.7 8.7 2 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3957784 151022 None 0 Human Functional pEC50 = 8.7 8.7 2 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993970 152113 None 0 Human Functional pEC50 = 8.7 8.7 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967058 152113 None 0 Human Functional pEC50 = 8.7 8.7 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152067 211769 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CNC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL3086284 213461 None 6 Rat Functional pEC50 = 8 8.0 1 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL221141 211882 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL262316 212996 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373854 214652 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374748 214666 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL410741 215295 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL426552 215807 None 0 Human Functional pEC50 = 5 5.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL375006 214670 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374260 214657 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cccnc1)C(N)=O 10.1021/jm0609824
101134421 2189 None 12 Human Functional pEC50 = 6.0 6.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Functional pEC50 = 6.0 6.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Functional pEC50 = 6.0 6.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Functional pEC50 = 6.0 6.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL386958 214862 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
25084922 151109 None 0 Rat Functional pEC50 = 8.0 8.0 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3958495 151109 None 0 Rat Functional pEC50 = 8.0 8.0 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993005 154218 None 0 Rat Functional pEC50 = 8.0 8.0 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985323 154218 None 0 Rat Functional pEC50 = 8.0 8.0 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL221602 211883 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL435315 216124 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cccnc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL439094 216282 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134150893 152003 None 0 Rat Functional pEC50 = 7.0 7.0 -19 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3966187 152003 None 0 Rat Functional pEC50 = 7.0 7.0 -19 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707479 113176 None 0 Rat Functional pEC50 = 7.0 7.0 -25 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314210 113176 None 0 Rat Functional pEC50 = 7.0 7.0 -25 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
134151953 153160 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3976038 153160 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707478 113175 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 113175 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
90324512 118939 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1408 39 18 21 -2.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(Cc2cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)nn2)nn1 10.1021/jm5019675
CHEMBL3422410 118939 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1408 39 18 21 -2.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(Cc2cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)nn2)nn1 10.1021/jm5019675
118707482 113179 None 0 Rat Functional pEC50 = 7.9 7.9 -10 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 113179 None 0 Rat Functional pEC50 = 7.9 7.9 -10 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707490 113187 None 0 Rat Functional pEC50 = 7.9 7.9 -20 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314221 113187 None 0 Rat Functional pEC50 = 7.9 7.9 -20 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3422510 214130 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
155547611 173809 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 652 17 10 7 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4535825 173809 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 652 17 10 7 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
24996155 147754 None 0 Rat Functional pEC50 = 7.8 7.8 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3931718 147754 None 0 Rat Functional pEC50 = 7.8 7.8 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134135834 144350 None 0 Rat Functional pEC50 = 7.8 7.8 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3904889 144350 None 0 Rat Functional pEC50 = 7.8 7.8 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993970 152113 None 0 Rat Functional pEC50 = 7.8 7.8 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967058 152113 None 0 Rat Functional pEC50 = 7.8 7.8 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995205 143129 None 0 Rat Functional pEC50 = 7.8 7.8 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3894943 143129 None 0 Rat Functional pEC50 = 7.8 7.8 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996810 151865 None 0 Rat Functional pEC50 = 7.8 7.8 -7 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964945 151865 None 0 Rat Functional pEC50 = 7.8 7.8 -7 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
1281 2187 None 32 Human Functional pEC50 = 7.8 7.8 1 4
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1283 2187 None 32 Human Functional pEC50 = 7.8 7.8 1 4
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
25240297 2187 None 32 Human Functional pEC50 = 7.8 7.8 1 4
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2187 None 32 Human Functional pEC50 = 7.8 7.8 1 4
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220855 211881 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134143614 145530 None 0 Rat Functional pEC50 = 7.8 7.8 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3914238 145530 None 0 Rat Functional pEC50 = 7.8 7.8 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118735681 118948 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1612 56 20 17 2.8 CCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
CHEMBL3422512 118948 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1612 56 20 17 2.8 CCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
16735731 85487 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 769 21 11 7 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226635 85487 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 769 21 11 7 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134151953 153160 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3976038 153160 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16736192 143387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL389708 143387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
155550676 174387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1082 29 16 12 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4549804 174387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1082 29 16 12 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152151 211770 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CNC(=O)CNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
118707486 113183 None 0 Rat Functional pEC50 = 8.7 8.7 -7 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 113183 None 0 Rat Functional pEC50 = 8.7 8.7 -7 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996155 147754 None 0 Human Functional pEC50 = 8.6 8.6 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3931718 147754 None 0 Human Functional pEC50 = 8.6 8.6 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
57653056 150796 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956072 150796 None 0 Human Functional pEC50 = 8.6 8.6 10 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707484 113181 None 0 Rat Functional pEC50 = 8.6 8.6 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 113181 None 0 Rat Functional pEC50 = 8.6 8.6 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996810 151865 None 0 Human Functional pEC50 = 8.6 8.6 7 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964945 151865 None 0 Human Functional pEC50 = 8.6 8.6 7 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25138124 170409 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444664 170409 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL3422406 214123 None 21 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
CHEMBL3086284 213461 None 6 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
16735781 85853 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 900 25 11 9 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229656 85853 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 900 25 11 9 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134135834 144350 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3904889 144350 None 0 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995205 143129 None 0 Human Functional pEC50 = 8.6 8.6 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3894943 143129 None 0 Human Functional pEC50 = 8.6 8.6 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25084922 151109 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3958495 151109 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707483 113180 None 0 Human Functional pEC50 = 8.6 8.6 33 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314214 113180 None 0 Human Functional pEC50 = 8.6 8.6 33 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075960 146444 None 0 Rat Functional pEC50 = 8.6 8.6 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3921327 146444 None 0 Rat Functional pEC50 = 8.6 8.6 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707491 113188 None 0 Rat Functional pEC50 = 8.6 8.6 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 113188 None 0 Rat Functional pEC50 = 8.6 8.6 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118735683 118949 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1741 61 22 19 2.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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)O 10.1021/jm5019675
CHEMBL3422514 118949 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1741 61 22 19 2.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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)O 10.1021/jm5019675
24996487 150871 None 0 Rat Functional pEC50 = 7.7 7.7 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956626 150871 None 0 Rat Functional pEC50 = 7.7 7.7 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075973 153311 None 0 Rat Functional pEC50 = 7.7 7.7 -42 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977314 153311 None 0 Rat Functional pEC50 = 7.7 7.7 -42 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL221817 211887 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0609824
CHEMBL221764 211885 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374246 214656 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118735686 118952 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1693 61 21 22 0.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL3422517 118952 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1693 61 21 22 0.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
134157281 154093 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3984058 154093 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707480 113177 None 0 Rat Functional pEC50 = 7.7 7.7 -14 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314211 113177 None 0 Rat Functional pEC50 = 7.7 7.7 -14 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL221761 211884 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)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](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2189 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
57653056 150796 None 0 Rat Functional pEC50 = 7.6 7.6 -10 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956072 150796 None 0 Rat Functional pEC50 = 7.6 7.6 -10 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118735684 118950 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1669 61 22 20 -0.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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)O 10.1021/jm5019675
CHEMBL3422515 118950 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1669 61 22 20 -0.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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)O 10.1021/jm5019675
CHEMBL434382 216116 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220759 211880 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375983 214695 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375982 214694 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374077 214653 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL441935 216364 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
16735544 142146 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 916 23 11 10 2.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1OC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387875 142146 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 916 23 11 10 2.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1OC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735511 143127 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL389493 143127 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16736191 161968 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CO)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL415004 161968 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CO)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735509 85486 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226634 85486 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
44425065 137044 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 809 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL374398 137044 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 809 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
9919540 85852 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 992 27 10 10 3.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN(Cc2ccccn2)Cc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229655 85852 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 992 27 10 10 3.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN(Cc2ccccn2)Cc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16736169 142117 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 899 25 11 8 2.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387648 142117 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 899 25 11 8 2.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24993005 154218 None 0 Human Functional pEC50 = 8.5 8.5 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985323 154218 None 0 Human Functional pEC50 = 8.5 8.5 3 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134143614 145530 None 0 Human Functional pEC50 = 8.4 8.4 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3914238 145530 None 0 Human Functional pEC50 = 8.4 8.4 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707493 113191 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 113191 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL2152065 211767 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
118707497 113195 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 113195 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL375450 214682 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707488 113185 None 0 Rat Functional pEC50 = 7.5 7.5 -24 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314219 113185 None 0 Rat Functional pEC50 = 7.5 7.5 -24 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
101134421 2189 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 213001 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0609824
CHEMBL373714 214651 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
10222 3740 None 12 Rat Functional pEC50 = 7.4 7.4 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3740 None 12 Rat Functional pEC50 = 7.4 7.4 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3740 None 12 Rat Functional pEC50 = 7.4 7.4 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3740 None 12 Rat Functional pEC50 = 7.4 7.4 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL221816 211886 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm0609824
CHEMBL373676 214650 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 215567 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm0609824
118707485 113182 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 113182 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707496 113194 None 0 Rat Functional pEC50 = 8.4 8.4 -5 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 113194 None 0 Rat Functional pEC50 = 8.4 8.4 -5 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
1281 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2187 None 32 Rat Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
118707494 113192 None 0 Rat Functional pEC50 = 8.4 8.4 -5 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 113192 None 0 Rat Functional pEC50 = 8.4 8.4 -5 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25138129 188740 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL503052 188740 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
24994895 149813 None 0 Human Functional pEC50 = 8.4 8.4 9 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3947975 149813 None 0 Human Functional pEC50 = 8.4 8.4 9 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707479 113176 None 0 Human Functional pEC50 = 8.4 8.4 25 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314210 113176 None 0 Human Functional pEC50 = 8.4 8.4 25 2
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16736392 142150 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387923 142150 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134154824 151022 None 0 Rat Functional pEC50 = 8.3 8.3 -2 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3957784 151022 None 0 Rat Functional pEC50 = 8.3 8.3 -2 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075965 147554 None 0 Rat Functional pEC50 = 8.3 8.3 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3930297 147554 None 0 Rat Functional pEC50 = 8.3 8.3 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157013 154200 None 0 Rat Functional pEC50 = 8.3 8.3 -7 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985112 154200 None 0 Rat Functional pEC50 = 8.3 8.3 -7 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996487 150871 None 0 Human Functional pEC50 = 8.3 8.3 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956626 150871 None 0 Human Functional pEC50 = 8.3 8.3 4 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157281 154093 None 0 Rat Functional pEC50 = 7.4 7.4 -1 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3984058 154093 None 0 Rat Functional pEC50 = 7.4 7.4 -1 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24994895 149813 None 0 Rat Functional pEC50 = 7.4 7.4 -9 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3947975 149813 None 0 Rat Functional pEC50 = 7.4 7.4 -9 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157735 153930 None 0 Rat Functional pEC50 = 7.4 7.4 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3982675 153930 None 0 Rat Functional pEC50 = 7.4 7.4 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995519 143322 None 0 Rat Functional pEC50 = 7.3 7.3 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3896533 143322 None 0 Rat Functional pEC50 = 7.3 7.3 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL414073 215567 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm0609824
25075978 148640 None 0 Rat Functional pEC50 = 7.3 7.3 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3938759 148640 None 0 Rat Functional pEC50 = 7.3 7.3 -8 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16737730 97290 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268661 97290 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
10222 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
24995519 143322 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3896533 143322 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075978 148640 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3938759 148640 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25138125 188457 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL501043 188457 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
134157735 153930 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3982675 153930 None 0 Human Functional pEC50 = 8.3 8.3 8 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707477 113174 None 0 Rat Functional pEC50 = 8.2 8.2 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 113174 None 0 Rat Functional pEC50 = 8.2 8.2 -3 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
134150893 152003 None 0 Human Functional pEC50 = 8.2 8.2 19 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3966187 152003 None 0 Human Functional pEC50 = 8.2 8.2 19 2
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152050 211752 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
24995518 145660 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3915251 145660 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707476 113173 None 0 Rat Functional pEC50 = 8.2 8.2 -6 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 113173 None 0 Rat Functional pEC50 = 8.2 8.2 -6 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996486 150849 None 0 Rat Functional pEC50 = 8.2 8.2 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956437 150849 None 0 Rat Functional pEC50 = 8.2 8.2 -4 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707489 113186 None 0 Rat Functional pEC50 = 8.2 8.2 -13 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](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(N)=O 10.1021/jm5005489
CHEMBL3314220 113186 None 0 Rat Functional pEC50 = 8.2 8.2 -13 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](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(N)=O 10.1021/jm5005489
CHEMBL374295 214659 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375432 214680 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134150351 151807 None 0 Rat Functional pEC50 = 8.2 8.2 -14 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964403 151807 None 0 Rat Functional pEC50 = 8.2 8.2 -14 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24992020 152317 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3968824 152317 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996490 149974 None 0 Rat Functional pEC50 = 8.2 8.2 -16 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949224 149974 None 0 Rat Functional pEC50 = 8.2 8.2 -16 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152051 211753 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL3422511 214131 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm5019675
24994272 153296 None 0 Rat Functional pEC50 = 8.1 8.1 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977235 153296 None 0 Rat Functional pEC50 = 8.1 8.1 -3 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996809 148704 None 0 Rat Functional pEC50 = 8.1 8.1 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3939287 148704 None 0 Rat Functional pEC50 = 8.1 8.1 -6 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707481 113178 None 0 Rat Functional pEC50 = 8.1 8.1 -12 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314212 113178 None 0 Rat Functional pEC50 = 8.1 8.1 -12 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155534572 172048 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1040 28 16 12 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4470482 172048 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1040 28 16 12 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL434379 216114 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL2152053 211755 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL414811 215618 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
155559308 174950 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 910 24 13 9 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4562955 174950 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 910 24 13 9 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
57653049 152203 None 0 Rat Functional pEC50 = 8.1 8.1 -11 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967782 152203 None 0 Rat Functional pEC50 = 8.1 8.1 -11 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL435922 216135 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL385105 214802 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134132372 145187 None 0 Rat Functional pEC50 = 8.0 8.0 -19 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3911692 145187 None 0 Rat Functional pEC50 = 8.0 8.0 -19 2
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707487 113184 None 0 Rat Functional pEC50 = 8.0 8.0 -13 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 113184 None 0 Rat Functional pEC50 = 8.0 8.0 -13 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL375395 214679 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/jm0609824
118707483 113180 None 0 Rat Functional pEC50 = 7.0 7.0 -33 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314214 113180 None 0 Rat Functional pEC50 = 7.0 7.0 -33 2
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
135936864 10472 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164674 10472 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016360 10477 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164939 10477 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016359 10455 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1164153 10455 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
136016412 10491 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165432 10491 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016444 10497 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165783 10497 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016380 10484 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165222 10484 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016381 10448 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163896 10448 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
135936875 10445 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163809 10445 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016362 10479 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165100 10479 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016382 10449 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163897 10449 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016407 10441 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163736 10441 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL3086284 213461 None 6 Human Functional pIC50 = 8.1 8.1 -1 2
Affinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1RAffinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.6019/CHEMBL5209897
136016389 10447 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163888 10447 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
135401501 10999 None 2 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilizationAntagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilization
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10999 None 2 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilizationAntagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilization
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
10222 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
46700761 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
CHEMBL3924151 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
DB11975 3740 None 12 Human Functional pEC50 = 8.3 8.3 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
1287 2192 None 0 Human Functional pEC50 = 8.8 8.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
155817402 2192 None 0 Human Functional pEC50 = 8.8 8.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
4014 117 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18302161
4015 1520 None 0 Mouse Functional pIC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19934405


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL3086284 213461 None 6 Rat Binding pEC50 = 9.8 9.8 -1 3
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155551159 174055 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4541289 174055 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
1281 2187 None 32 Human Binding pIC50 = 10.2 10.2 1 2
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1283 2187 None 32 Human Binding pIC50 = 10.2 10.2 1 2
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
25240297 2187 None 32 Human Binding pIC50 = 10.2 10.2 1 2
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2187 None 32 Human Binding pIC50 = 10.2 10.2 1 2
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1281 2187 None 32 Human Binding pIC50 = 10.1 10.1 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2187 None 32 Human Binding pIC50 = 10.1 10.1 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2187 None 32 Human Binding pIC50 = 10.1 10.1 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2187 None 32 Human Binding pIC50 = 10.1 10.1 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL2151642 211748 None 0 Human Binding pIC50 = 10.0 10.0 2 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2187 None 32 Rat Binding pIC50 = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2187 None 32 Rat Binding pIC50 = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2187 None 32 Rat Binding pIC50 = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2187 None 32 Rat Binding pIC50 = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
58143625 125458 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.0 CNC/C=C/[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645499 125458 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.0 CNC/C=C/[C@@H](CC(C)C)C(C)=O nan
1281 2187 None 32 Human Binding pIC50 = 9.9 9.9 1 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
1283 2187 None 32 Human Binding pIC50 = 9.9 9.9 1 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25240297 2187 None 32 Human Binding pIC50 = 9.9 9.9 1 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
CHEMBL376756 2187 None 32 Human Binding pIC50 = 9.9 9.9 1 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25138123 179353 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL472833 179353 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
25138123 179353 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL472833 179353 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71460220 80794 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80794 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461938 80787 None 0 Human Binding pIC50 = 9.8 9.8 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80787 None 0 Human Binding pIC50 = 9.8 9.8 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461938 80787 None 0 Rat Binding pIC50 = 9.8 9.8 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80787 None 0 Rat Binding pIC50 = 9.8 9.8 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460219 80791 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80791 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461940 80795 None 0 Human Binding pIC50 = 9.7 9.7 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80795 None 0 Human Binding pIC50 = 9.7 9.7 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460220 80794 None 0 Rat Binding pIC50 = 9.7 9.7 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80794 None 0 Rat Binding pIC50 = 9.7 9.7 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461940 80795 None 0 Rat Binding pIC50 = 9.7 9.7 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80795 None 0 Rat Binding pIC50 = 9.7 9.7 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
58143618 125463 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645504 125463 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
71460219 80791 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80791 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
25138131 173974 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL453956 173974 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL2151642 211748 None 0 Rat Binding pIC50 = 9.6 9.6 -2 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449399 80796 None 0 Human Binding pIC50 = 9.6 9.6 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80796 None 0 Human Binding pIC50 = 9.6 9.6 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71451197 80793 None 0 Rat Binding pIC50 = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80793 None 0 Rat Binding pIC50 = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449399 80796 None 0 Rat Binding pIC50 = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80796 None 0 Rat Binding pIC50 = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71451197 80793 None 0 Human Binding pIC50 = 9.5 9.5 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80793 None 0 Human Binding pIC50 = 9.5 9.5 1 2
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460218 80790 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80790 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456525 80788 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80788 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460218 80790 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80790 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456525 80788 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80788 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461937 80786 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80786 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456524 80785 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80785 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80792 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80792 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
59002736 125457 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645498 125457 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@@H](CC(C)C)C(C)=O nan
16735569 142421 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL388586 142421 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
16735569 142421 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL388586 142421 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71449398 80789 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80789 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449398 80789 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80789 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80792 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80792 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
58143621 125459 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 185 7 1 2 2.2 CNCCC[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645500 125459 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 185 7 1 2 2.2 CNCCC[C@@H](CC(C)C)C(C)=O nan
25138124 170409 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444664 170409 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71456524 80785 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80785 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
136016473 10588 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169902 10588 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016474 10661 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 3 7 5.3 CCN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170468 10661 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 3 7 5.3 CCN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016476 10688 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170685 10688 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
135410889 10721 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170904 10721 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016519 10933 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173008 10933 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016412 10491 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165432 10491 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016490 10813 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171977 10813 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016389 10447 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163888 10447 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
136016372 10438 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccc(C(=O)NCCN)cc2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163732 10438 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccc(C(=O)NCCN)cc2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016390 10452 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 4.5 COc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3ccccc3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163972 10452 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 4.5 COc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3ccccc3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
136016413 10442 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 7 4 7 4.4 Cc1c(-c2ccccc2O)nc(NC(=O)c2ccco2)c(C#N)c1-c1cccc(NC(=O)CCN)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163739 10442 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 7 4 7 4.4 Cc1c(-c2ccccc2O)nc(NC(=O)c2ccco2)c(C#N)c1-c1cccc(NC(=O)CCN)c1 10.1016/j.bmc.2010.04.036
136016490 10813 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171977 10813 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016484 10752 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CC3CCCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171294 10752 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CC3CCCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016391 10485 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 7 4 7 3.5 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1165223 10485 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 7 4 7 3.5 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016492 10753 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 N#Cc1c(-c2cccc(NC(=O)CN3CCCCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171296 10753 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 N#Cc1c(-c2cccc(NC(=O)CN3CCCCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016518 10929 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 2 7 4.7 CN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1172940 10929 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 2 7 4.7 CN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
135401501 10999 None 2 Rat Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10999 None 2 Rat Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016398 10440 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 495 7 4 7 4.3 CC(C)(CN)NC(=O)c1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163735 10440 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 495 7 4 7 4.3 CC(C)(CN)NC(=O)c1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016436 10457 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 427 5 3 6 4.8 N#Cc1c(-c2cccc(CO)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164235 10457 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 427 5 3 6 4.8 N#Cc1c(-c2cccc(CO)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016475 10687 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 3 7 5.6 CCN(CC)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170684 10687 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 3 7 5.6 CCN(CC)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016489 10741 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171102 10741 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1672381 211290 None 5 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None CN(C)c1cccc2c(S(=O)(=O)N3CCC[C@H]3C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cccc12 10.1021/ml1002053
136016478 10717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 555 10 3 7 6.0 CCN(CC)C(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170895 10717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 555 10 3 7 6.0 CCN(CC)C(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016477 10716 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 8 3 7 5.3 CC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(C)C 10.1016/j.bmc.2010.05.061
CHEMBL1170894 10716 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 8 3 7 5.3 CC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(C)C 10.1016/j.bmc.2010.05.061
136016483 10740 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 CN1CCC[C@H]1CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171097 10740 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 CN1CCC[C@H]1CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016522 10982 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 4.7 CN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173438 10982 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 4.7 CN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
71451197 80793 None 0 Human Binding pIC50 = 7.7 7.7 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80793 None 0 Human Binding pIC50 = 7.7 7.7 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016471 10582 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 7 3 7 4.8 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3cccs3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169893 10582 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 7 3 7 4.8 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3cccs3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016382 10449 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163897 10449 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
71454755 80784 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80784 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461937 80786 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80786 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
136016523 10990 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 2 7 5.1 CCN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173512 10990 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 2 7 5.1 CCN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016486 14355 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171483 14355 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1200097 14355 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016472 10587 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169901 10587 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
135936864 10472 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164674 10472 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
135528869 10467 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 4 3 6 4.9 N#Cc1c(-c2cccc(N)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164603 10467 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 4 3 6 4.9 N#Cc1c(-c2cccc(N)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016480 10798 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 569 11 3 7 6.4 CCC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(CC)CC 10.1016/j.bmc.2010.05.061
CHEMBL1171797 10798 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 569 11 3 7 6.4 CCC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(CC)CC 10.1016/j.bmc.2010.05.061
25138132 189025 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL507796 189025 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
135410892 14385 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1200240 14385 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL3216935 14385 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016482 10720 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170903 10720 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016488 10722 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170911 10722 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
71454755 80784 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80784 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
135401501 10999 None 2 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10999 None 2 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
135936875 10445 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1163809 10445 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
135936875 10445 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163809 10445 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016491 10742 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(CC)C(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171104 10742 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(CC)C(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016493 10784 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 2 7 5.0 CN(C)CCN(C)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171663 10784 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 2 7 5.0 CN(C)CCN(C)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016362 10479 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165100 10479 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016397 10439 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NCCN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
CHEMBL1163734 10439 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NCCN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
58143614 125461 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@H](O)/C=C(\CC(C)C)C(C)=O nan
CHEMBL3645502 125461 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@H](O)/C=C(\CC(C)C)C(C)=O nan
58143618 125463 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645504 125463 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
25138126 172573 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL448207 172573 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
25138130 172855 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL450923 172855 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016399 10444 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NC(C)(C)CN)c2)c1C#N 10.1016/j.bmc.2010.04.036
CHEMBL1163808 10444 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NC(C)(C)CN)c2)c1C#N 10.1016/j.bmc.2010.04.036
136016406 10492 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NC(C)(C)CN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
CHEMBL1165467 10492 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NC(C)(C)CN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
136016361 10456 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccccc2C(=O)NCCN)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164154 10456 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccccc2C(=O)NCCN)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016360 10477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164939 10477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
88978455 125464 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@H](CC(C)C)C(C)=O nan
CHEMBL3645505 125464 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@H](CC(C)C)C(C)=O nan
135410889 10721 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170904 10721 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
58143615 125462 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645503 125462 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
25138128 182106 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL478053 182106 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016487 10765 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 471 6 4 7 3.9 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171484 10765 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 471 6 4 7 3.9 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
122196636 125460 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.2 CNCC/C=C(/CC(C)C)C(C)=O nan
CHEMBL3645501 125460 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.2 CNCC/C=C(/CC(C)C)C(C)=O nan
25138125 188457 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL501043 188457 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016472 10587 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169901 10587 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL3087931 213473 None 0 Human Binding pIC50 = 7.4 7.4 -1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016392 10486 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NCCN)c2)c1C#N 10.1016/j.bmc.2010.04.036
CHEMBL1165224 10486 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NCCN)c2)c1C#N 10.1016/j.bmc.2010.04.036
58143616 125465 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@@H](O)/C=C(\CC(C)C)C(C)=O nan
CHEMBL3645506 125465 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@@H](O)/C=C(\CC(C)C)C(C)=O nan
25138127 170308 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444522 170308 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016473 10588 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169902 10588 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016519 10933 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173008 10933 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016379 10480 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 513 8 4 8 4.6 COc1ccc(O)c(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165103 10480 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 513 8 4 8 4.6 COc1ccc(O)c(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c1 10.1016/j.bmc.2010.04.036
136016373 10478 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2cc(Cl)ccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164988 10478 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2cc(Cl)ccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
58143615 125462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645503 125462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
25138129 188740 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL503052 188740 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016359 10455 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1164153 10455 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
136016444 10497 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165783 10497 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016443 10471 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 3 6 4.8 N#Cc1c(-c2cccc(CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164673 10471 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 3 6 4.8 N#Cc1c(-c2cccc(CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016517 11000 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 3 7 4.8 N#Cc1c(-c2cccc(N3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173644 11000 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 3 7 4.8 N#Cc1c(-c2cccc(N3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016380 10484 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.05.061
CHEMBL1165222 10484 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.05.061
136016380 10484 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165222 10484 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016482 10720 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170903 10720 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016479 10718 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 4 7 5.7 CCNC(CC)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170896 10718 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 4 7 5.7 CCNC(CC)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016407 10441 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163736 10441 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016488 10722 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170911 10722 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL3086284 213461 None 6 Human Binding pIC50 = 8.1 8.1 1 3
Cellular activity assay: GPR54 expressing cell growthCellular activity assay: GPR54 expressing cell growth
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.6019/CHEMBL4507306
CHEMBL3086284 213461 None 6 Human Binding pIC50 = 8.1 8.1 1 3
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1486 3323 None 25 Human Binding pIC50 = 6.1 6.1 - 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
53320361 3323 None 25 Human Binding pIC50 = 6.1 6.1 - 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
CHEMBL1672380 3323 None 25 Human Binding pIC50 = 6.1 6.1 - 2
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
1281 2187 None 32 Human Binding pIC50 = 5.1 5.1 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
1283 2187 None 32 Human Binding pIC50 = 5.1 5.1 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
25240297 2187 None 32 Human Binding pIC50 = 5.1 5.1 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2187 None 32 Human Binding pIC50 = 5.1 5.1 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL2151642 211748 None 0 Human Binding pIC50 = 7.1 7.1 2 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
46906647 10490 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 476 7 4 6 4.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2N)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1165431 10490 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 476 7 4 6 4.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2N)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
71461938 80787 None 0 Human Binding pIC50 = 8.0 8.0 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80787 None 0 Human Binding pIC50 = 8.0 8.0 1 2
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016481 10694 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 9 4 7 5.7 CC(C)NC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170692 10694 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 9 4 7 5.7 CC(C)NC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016521 14331 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170870 14331 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1200013 14331 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016381 10448 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163896 10448 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016437 10458 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 441 5 3 6 5.0 N#Cc1c(-c2cccc(C(=O)O)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164236 10458 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 441 5 3 6 5.0 N#Cc1c(-c2cccc(C(=O)O)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL3315315 213838 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707495 113193 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 113193 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707486 113183 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 113183 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086282 213459 None 0 Human Binding pKi = 10.5 10.5 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087927 213469 None 0 Human Binding pKi = 10.5 10.5 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1cnc[nH]1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707494 113192 None 0 Human Binding pKi = 10.5 10.5 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 113192 None 0 Human Binding pKi = 10.5 10.5 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
1281 2187 None 32 Human Binding pKi = 10.5 10.5 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2187 None 32 Human Binding pKi = 10.5 10.5 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2187 None 32 Human Binding pKi = 10.5 10.5 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2187 None 32 Human Binding pKi = 10.5 10.5 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
118707485 113182 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 113182 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
49787129 113190 None 7 Human Binding pKi = 10.4 10.4 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 113190 None 7 Human Binding pKi = 10.4 10.4 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707484 113181 None 0 Human Binding pKi = 10.4 10.4 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 113181 None 0 Human Binding pKi = 10.4 10.4 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707497 113195 None 0 Human Binding pKi = 10.4 10.4 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 113195 None 0 Human Binding pKi = 10.4 10.4 2 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
1281 2187 None 32 Human Binding pKi = 10.4 10.4 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
1283 2187 None 32 Human Binding pKi = 10.4 10.4 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
25240297 2187 None 32 Human Binding pKi = 10.4 10.4 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2187 None 32 Human Binding pKi = 10.4 10.4 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
118707492 113189 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 113189 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087793 213466 None 0 Rat Binding pKi = 10.4 10.4 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CC(C)C[C@H](NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087925 213467 None 0 Rat Binding pKi = 10.4 10.4 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087927 213469 None 0 Rat Binding pKi = 10.4 10.4 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1cnc[nH]1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085809 213454 None 0 Human Binding pKi = 10.4 10.4 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087793 213466 None 0 Human Binding pKi = 10.4 10.4 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151642 211748 None 0 Human Binding pKi = 10.3 10.3 2 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71461938 80787 None 0 Human Binding pKi = 10.3 10.3 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80787 None 0 Human Binding pKi = 10.3 10.3 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086282 213459 None 0 Rat Binding pKi = 10.3 10.3 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085804 213449 None 0 Human Binding pKi = 10.3 10.3 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707478 113175 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 113175 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087929 213471 None 0 Human Binding pKi = 10.3 10.3 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1281 2187 None 32 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
1283 2187 None 32 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
25240297 2187 None 32 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2187 None 32 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL3085809 213454 None 0 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087925 213467 None 0 Human Binding pKi = 10.2 10.2 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1281 2187 None 32 Human Binding pKi = 10.2 10.2 1 2
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
1283 2187 None 32 Human Binding pKi = 10.2 10.2 1 2
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
25240297 2187 None 32 Human Binding pKi = 10.2 10.2 1 2
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL376756 2187 None 32 Human Binding pKi = 10.2 10.2 1 2
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL3086283 213460 None 0 Human Binding pKi = 10.2 10.2 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71461938 80787 None 0 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80787 None 0 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
49787129 113190 None 7 Rat Binding pKi = 10.2 10.2 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 113190 None 7 Rat Binding pKi = 10.2 10.2 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085804 213449 None 0 Rat Binding pKi = 10.2 10.2 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707476 113173 None 0 Human Binding pKi = 10.1 10.1 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 113173 None 0 Human Binding pKi = 10.1 10.1 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087929 213471 None 0 Rat Binding pKi = 10.1 10.1 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707484 113181 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 113181 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71461940 80795 None 0 Human Binding pKi = 10.1 10.1 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151654 80795 None 0 Human Binding pKi = 10.1 10.1 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086281 213458 None 0 Human Binding pKi = 10.1 10.1 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087926 213468 None 0 Human Binding pKi = 10.1 10.1 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707477 113174 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 113174 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707494 113192 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 113192 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707497 113195 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 113195 None 0 Rat Binding pKi = 10.1 10.1 -2 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
1281 2187 None 32 Rat Binding pKi = 10.1 10.1 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2187 None 32 Rat Binding pKi = 10.1 10.1 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2187 None 32 Rat Binding pKi = 10.1 10.1 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2187 None 32 Rat Binding pKi = 10.1 10.1 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL3086284 213461 None 6 Human Binding pKi = 10.1 10.1 1 3
Affinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1RAffinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.6019/CHEMBL5210307
CHEMBL3086284 213461 None 6 Human Binding pKi = 10.1 10.1 1 3
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086284 213461 None 6 Human Binding pKi = 10.1 10.1 1 3
Cell free activity assay: Binding to human GPR54Cell free activity assay: Binding to human GPR54
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.6019/CHEMBL4507306
118707496 113194 None 0 Human Binding pKi = 10.1 10.1 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 113194 None 0 Human Binding pKi = 10.1 10.1 1 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71461940 80795 None 0 Rat Binding pKi = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151654 80795 None 0 Rat Binding pKi = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087926 213468 None 0 Rat Binding pKi = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087931 213473 None 0 Rat Binding pKi = 10.0 10.0 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707482 113179 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 113179 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086284 213461 None 6 Rat Binding pKi = 10 10.0 -1 3
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086286 213463 None 0 Human Binding pKi = 10.0 10.0 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087931 213473 None 0 Human Binding pKi = 10.0 10.0 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151642 211748 None 0 Rat Binding pKi = 10.0 10.0 -2 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086283 213460 None 0 Rat Binding pKi = 10.0 10.0 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086284 213461 None 6 Human Binding pKi = 10.0 10.0 1 3
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
118707493 113191 None 0 Rat Binding pKi = 10.0 10.0 - 1
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 113191 None 0 Rat Binding pKi = 10.0 10.0 - 1
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1326 35 19 14 -0.2 CCCC(=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](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
71451197 80793 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80793 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71449399 80796 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151655 80796 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085806 213451 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086280 213457 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087928 213470 None 0 Human Binding pKi = 9.9 9.9 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71451197 80793 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80793 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71449399 80796 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151655 80796 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087928 213470 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707491 113188 None 0 Human Binding pKi = 9.9 9.9 6 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 113188 None 0 Human Binding pKi = 9.9 9.9 6 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086280 213457 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086286 213463 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707476 113173 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 113173 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085806 213451 None 0 Rat Binding pKi = 9.9 9.9 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086284 213461 None 6 Rat Binding pKi = 9.9 9.9 -1 3
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3086281 213458 None 0 Rat Binding pKi = 9.8 9.8 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085808 213453 None 0 Rat Binding pKi = 9.8 9.8 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707496 113194 None 0 Rat Binding pKi = 9.8 9.8 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 113194 None 0 Rat Binding pKi = 9.8 9.8 -1 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085807 213452 None 0 Rat Binding pKi = 9.7 9.7 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085807 213452 None 0 Human Binding pKi = 9.7 9.7 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085811 213456 None 0 Human Binding pKi = 9.7 9.7 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086285 213462 None 0 Human Binding pKi = 9.7 9.7 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707487 113184 None 0 Human Binding pKi = 9.7 9.7 18 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 113184 None 0 Human Binding pKi = 9.7 9.7 18 2
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085808 213453 None 0 Human Binding pKi = 9.7 9.7 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085810 213455 None 0 Human Binding pKi = 9.7 9.7 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085811 213456 None 0 Rat Binding pKi = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087930 213472 None 0 Rat Binding pKi = 9.6 9.6 1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086285 213462 None 0 Rat Binding pKi = 9.6 9.6 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087930 213472 None 0 Human Binding pKi = 9.5 9.5 -1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085810 213455 None 0 Rat Binding pKi = 9.5 9.5 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085805 213450 None 0 Human Binding pKi = 9.3 9.3 1 2
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085805 213450 None 0 Rat Binding pKi = 9.3 9.3 -1 2
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL375982 214694 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707491 113188 None 0 Rat Binding pKi = 9.1 9.1 -6 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 113188 None 0 Rat Binding pKi = 9.1 9.1 -6 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
101134421 2189 None 12 Human Binding pKi = 9.0 9.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Binding pKi = 9.0 9.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Binding pKi = 9.0 9.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Binding pKi = 9.0 9.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1281 2187 None 32 Human Binding pKi = 8.9 8.9 1 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1283 2187 None 32 Human Binding pKi = 8.9 8.9 1 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
25240297 2187 None 32 Human Binding pKi = 8.9 8.9 1 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2187 None 32 Human Binding pKi = 8.9 8.9 1 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 213001 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0609824
CHEMBL221602 211883 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2189 None 12 Human Binding pKi = 8.0 8.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Binding pKi = 8.0 8.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Binding pKi = 8.0 8.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Binding pKi = 8.0 8.0 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL221141 211882 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL262316 212996 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373854 214652 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374295 214659 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374748 214666 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL410741 215295 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL426552 215807 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL375006 214670 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375395 214679 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/jm0609824
CHEMBL441935 216364 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220759 211880 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL434379 216114 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221816 211886 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm0609824
CHEMBL435922 216135 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375983 214695 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220855 211881 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 215567 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm0609824
CHEMBL375450 214682 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373714 214651 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL386958 214862 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374246 214656 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707487 113184 None 0 Rat Binding pKi = 8.4 8.4 -18 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 113184 None 0 Rat Binding pKi = 8.4 8.4 -18 2
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL373676 214650 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
2335 11852 None 18 Human Binding pKi = 5.4 5.4 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
8478 11852 None 18 Human Binding pKi = 5.4 5.4 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL1182210 11852 None 18 Human Binding pKi = 5.4 5.4 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL221753 11852 None 18 Human Binding pKi = 5.4 5.4 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL435315 216124 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cccnc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221817 211887 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0609824
CHEMBL221761 211884 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)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](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL439094 216282 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2189 None 12 Human Binding pKi = 6.3 6.3 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2189 None 12 Human Binding pKi = 6.3 6.3 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2189 None 12 Human Binding pKi = 6.3 6.3 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2189 None 12 Human Binding pKi = 6.3 6.3 -6 2
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL434382 216116 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
10301495 83271 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 517 6 2 7 5.1 NCCCn1nc(C2=C(c3cn(-c4csc5ccccc45)c4ccccc34)C(=O)NC2=O)c2ccccc21 10.1021/jm0609824
CHEMBL218690 83271 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 517 6 2 7 5.1 NCCCn1nc(C2=C(c3cn(-c4csc5ccccc45)c4ccccc34)C(=O)NC2=O)c2ccccc21 10.1021/jm0609824
CHEMBL414811 215618 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 215567 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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/jm0609824
CHEMBL385105 214802 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221764 211885 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374260 214657 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cccnc1)C(N)=O 10.1021/jm0609824
CHEMBL375432 214680 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374077 214653 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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](Cc1ccccc1)C(N)=O 10.1021/jm0609824
1281 2187 None 32 Human Binding pKd = 8.7 8.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2187 None 32 Human Binding pKd = 8.7 8.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2187 None 32 Human Binding pKd = 8.7 8.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2187 None 32 Human Binding pKd = 8.7 8.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
2335 11852 None 18 Human Binding pKi = 8.3 8.3 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 11852 None 18 Human Binding pKi = 8.3 8.3 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 11852 None 18 Human Binding pKi = 8.3 8.3 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 11852 None 18 Human Binding pKi = 8.3 8.3 -8 12
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
1286 2191 None 0 Human Binding pKi = 10 10.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817401 2191 None 0 Human Binding pKi = 10 10.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1289 2196 None 0 Human Binding pKi = 7 7.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817403 2196 None 0 Human Binding pKi = 7 7.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
101134421 2189 None 12 Human Binding pKi = 8.4 8.4 -6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2189 None 12 Human Binding pKi = 8.4 8.4 -6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2189 None 12 Human Binding pKi = 8.4 8.4 -6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2189 None 12 Human Binding pKi = 8.4 8.4 -6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
101134421 2189 None 12 Rat Binding pKi = 8.7 8.7 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2189 None 12 Rat Binding pKi = 8.7 8.7 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2189 None 12 Rat Binding pKi = 8.7 8.7 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2189 None 12 Rat Binding pKi = 8.7 8.7 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2190 None 0 Rat Binding pKi = 8.7 8.7 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2195 None 0 Rat Binding pKi = 8.7 8.7 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2187 None 32 Rat Binding pKi = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2187 None 32 Rat Binding pKi = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2187 None 32 Rat Binding pKi = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2187 None 32 Rat Binding pKi = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2190 None 0 Human Binding pKi = 8.8 8.8 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2195 None 0 Human Binding pKi = 9.2 9.2 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1288 2195 None 0 Human Binding pKi = 9.2 9.2 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1281 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1283 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
25240297 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
CHEMBL376756 2187 None 32 Human Binding pKi = 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843