Ligand source activities (1 row/activity)
| 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
| |
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
| |
| 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 | ||
Showing 1 to 50 of 545 entries
| 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
| |
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 | ||
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