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
| |
| 11467753 | 174300 | None | 0 | Human | Functional | pEC50 | = | 10.8 | 10.8 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP production |
ChEMBL | 626 | 6 | 3 | 5 | 4.5 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2013.01.011 | ||
| CHEMBL454791 | 174300 | None | 0 | Human | Functional | pEC50 | = | 10.8 | 10.8 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP production |
ChEMBL | 626 | 6 | 3 | 5 | 4.5 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2013.01.011 | ||
| 44593666 | 172833 | None | 8 | Human | Functional | pEC50 | = | 10.5 | 10.5 | - | 1 | Antagonist activity at human CGRP receptor in SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor in SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 644 | 6 | 3 | 5 | 4.6 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1021/jm800546t | ||
| CHEMBL450668 | 172833 | None | 8 | Human | Functional | pEC50 | = | 10.5 | 10.5 | - | 1 | Antagonist activity at human CGRP receptor in SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor in SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 644 | 6 | 3 | 5 | 4.6 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1021/jm800546t | ||
| 51049968 | 82592 | None | 40 | Human | Functional | pEC50 | = | 9.9 | 9.9 | 22387 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay |
ChEMBL | 534 | 3 | 2 | 7 | 4.5 | N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F | 10.1021/jm3013147 | ||
| 51049968.0 | 82592 | None | 40 | Human | Functional | pEC50 | = | 9.9 | 9.9 | 22387 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay |
ChEMBL | 534 | 3 | 2 | 7 | 4.5 | N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F | 10.1021/jm3013147 | ||
| CHEMBL2178422 | 82592 | None | 40 | Human | Functional | pEC50 | = | 9.9 | 9.9 | 22387 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay |
ChEMBL | 534 | 3 | 2 | 7 | 4.5 | N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F | 10.1021/jm3013147 | ||
| DB12457 | 82592 | None | 40 | Human | Functional | pEC50 | = | 9.9 | 9.9 | 22387 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay |
ChEMBL | 534 | 3 | 2 | 7 | 4.5 | N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F | 10.1021/jm3013147 | ||
| CHEMBL412994 | 215499 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Agonist activity at human CGRP1 expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human CGRP1 expressed in HEK293 cells assessed as cAMP accumulation |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C | 10.1021/jm061343w | ||||
| 24756611 | 76530 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 5.4 | O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059896 | 76530 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 5.4 | O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1 | 10.1016/j.bmcl.2012.05.118 | ||
| 70694804 | 76534 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 626 | 6 | 2 | 6 | 4.4 | O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059900 | 76534 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 626 | 6 | 2 | 6 | 4.4 | O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O | 10.1016/j.bmcl.2012.05.118 | ||
| 24756612 | 76532 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 4.8 | O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059898 | 76532 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 4.8 | O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21 | 10.1016/j.bmcl.2012.05.118 | ||
| 70694803 | 76531 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 4.7 | O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059897 | 76531 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 613 | 5 | 2 | 5 | 4.7 | O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 | 10.1016/j.bmcl.2012.05.118 | ||
| 62705051 | 76540 | None | 0 | Human | Functional | pEC50 | = | 8.5 | 8.5 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 614 | 5 | 3 | 5 | 5.1 | O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059906 | 76540 | None | 0 | Human | Functional | pEC50 | = | 8.5 | 8.5 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 614 | 5 | 3 | 5 | 5.1 | O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 | 10.1016/j.bmcl.2012.05.118 | ||
| 21102224 | 76539 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 615 | 5 | 2 | 6 | 5.6 | O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL2059905 | 76539 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMPAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated formation of cyclic AMP |
ChEMBL | 615 | 5 | 2 | 6 | 5.6 | O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 | 10.1016/j.bmcl.2012.05.118 | ||
| 11621504 | 173566 | None | 0 | Human | Functional | pIC50 | = | 11 | 11.0 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 627 | 6 | 2 | 6 | 4.9 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL452966 | 173566 | None | 0 | Human | Functional | pIC50 | = | 11 | 11.0 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 627 | 6 | 2 | 6 | 4.9 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 11599913 | 189086 | None | 0 | Human | Functional | pIC50 | = | 11.0 | 11.0 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 645 | 6 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL508453 | 189086 | None | 0 | Human | Functional | pIC50 | = | 11.0 | 11.0 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 645 | 6 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 11685954 | 189062 | None | 0 | Human | Functional | pIC50 | = | 10.8 | 10.8 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 6 | 2 | 6 | 5.1 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL508215 | 189062 | None | 0 | Human | Functional | pIC50 | = | 10.8 | 10.8 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 6 | 2 | 6 | 5.1 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 57404535 | 73824 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018517 | 73824 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 70696075 | 74141 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 607 | 7 | 2 | 6 | 6.2 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022601 | 74141 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 607 | 7 | 2 | 6 | 6.2 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 11498219 | 172232 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 6 | 2 | 6 | 5.1 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL447297 | 172232 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 6 | 2 | 6 | 5.1 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 11549159 | 172869 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 645 | 6 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4ccc(F)cc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL451164 | 172869 | None | 0 | Human | Functional | pIC50 | = | 10.7 | 10.7 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 645 | 6 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4ccc(F)cc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 44593666 | 172833 | None | 8 | Human | Functional | pIC50 | = | 10.6 | 10.6 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 644 | 6 | 3 | 5 | 4.6 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2013.08.031 | ||
| CHEMBL450668 | 172833 | None | 8 | Human | Functional | pIC50 | = | 10.6 | 10.6 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 644 | 6 | 3 | 5 | 4.6 | Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2013.08.031 | ||
| 70696079 | 74146 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 618 | 7 | 2 | 6 | 6.8 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022606 | 74146 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 618 | 7 | 2 | 6 | 6.8 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 11657395 | 188494 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 5 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC3(CCN(C)CC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL501603 | 188494 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 624 | 5 | 2 | 6 | 5.0 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC3(CCN(C)CC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 70687597 | 73814 | None | 0 | Human | Functional | pIC50 | = | 10.3 | 10.3 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 637 | 8 | 2 | 6 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018507 | 73814 | None | 0 | Human | Functional | pIC50 | = | 10.3 | 10.3 | - | 1 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 637 | 8 | 2 | 6 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 11599798 | 188344 | None | 0 | Human | Functional | pIC50 | = | 10.3 | 10.3 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 622 | 6 | 2 | 6 | 4.9 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CC=CCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL499488 | 188344 | None | 0 | Human | Functional | pIC50 | = | 10.3 | 10.3 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 622 | 6 | 2 | 6 | 4.9 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CC=CCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 11520204 | 173444 | None | 0 | Human | Functional | pIC50 | = | 10.2 | 10.2 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 642 | 6 | 2 | 6 | 5.3 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| CHEMBL452686 | 173444 | None | 0 | Human | Functional | pIC50 | = | 10.2 | 10.2 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 642 | 6 | 2 | 6 | 5.3 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
| 164618286 | 184651 | None | 0 | Human | Functional | pIC50 | = | 10.2 | 10.2 | - | 1 | Antagonist activity against human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity against human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 632 | 4 | 2 | 5 | 4.1 | Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 | 10.1016/j.bmcl.2021.128077 | ||
| CHEMBL4848032 | 184651 | None | 0 | Human | Functional | pIC50 | = | 10.2 | 10.2 | - | 1 | Antagonist activity against human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity against human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production |
ChEMBL | 632 | 4 | 2 | 5 | 4.1 | Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 | 10.1016/j.bmcl.2021.128077 | ||
| 11512851 | 189078 | None | 0 | Human | Functional | pIC50 | = | 10.2 | 10.2 | - | 1 | Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production |
ChEMBL | 619 | 6 | 2 | 7 | 4.4 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(c3ccncc3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2009.04.150 | ||
Showing 1 to 50 of 1,189 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
| |
| 6918509 | 77070 | None | 33 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 131 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| CHEMBL207197 | 77070 | None | 33 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 131 | 2 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| 68857312 | 112011 | None | 0 | Human | Binding | pEC50 | = | 9.8 | 9.8 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 881 | 12 | 5 | 10 | 3.2 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| CHEMBL3288288 | 112011 | None | 0 | Human | Binding | pEC50 | = | 9.8 | 9.8 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 881 | 12 | 5 | 10 | 3.2 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| 86298538 | 112013 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 765 | 12 | 4 | 10 | 3.2 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| CHEMBL3288290 | 112013 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 765 | 12 | 4 | 10 | 3.2 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| 86298539 | 112012 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 751 | 12 | 4 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| CHEMBL3288289 | 112012 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay |
ChEMBL | 751 | 12 | 4 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2014.04.033 | ||
| 6918509 | 77070 | None | 33 | Human | Binding | pIC50 | = | 10.7 | 10.7 | 131 | 2 | Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2012.05.118 | ||
| CHEMBL207197 | 77070 | None | 33 | Human | Binding | pIC50 | = | 10.7 | 10.7 | 131 | 2 | Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1016/j.bmcl.2012.05.118 | ||
| 44403861 | 72047 | None | 0 | Human | Binding | pIC50 | = | 10.5 | 10.5 | - | 0 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| CHEMBL197529 | 72047 | None | 0 | Human | Binding | pIC50 | = | 10.5 | 10.5 | - | 0 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| 6918509 | 77070 | None | 33 | Human | Binding | pIC50 | = | 10.5 | 10.5 | 131 | 2 | Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm500364u | ||
| CHEMBL207197 | 77070 | None | 33 | Human | Binding | pIC50 | = | 10.5 | 10.5 | 131 | 2 | Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm500364u | ||
| CHEMBL3883526 | 214876 | None | 0 | Human | Binding | pIC50 | = | 10.5 | 10.5 | - | 0 | Displacement of [125I]hCGRPa from human recombinant CGRP receptor expressed in CHO cells measured after 90 mins by scintillation counting methodDisplacement of [125I]hCGRPa from human recombinant CGRP receptor expressed in CHO cells measured after 90 mins by scintillation counting method |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)[C@@H](C)O)[C@@H](C)O)[C@H](C)O)[C@@H](C)O)C(=O)NCC(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)O)C(C)C | 10.1016/j.bmc.2016.11.014 | ||||
| CHEMBL2369459 | 212076 | None | 0 | Human | Binding | pIC50 | = | 10.4 | 10.4 | - | 1 | Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C | 10.1021/jm8007618 | ||||
| 44403862 | 157987 | None | 0 | Human | Binding | pIC50 | = | 10.3 | 10.3 | - | 0 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 879 | 13 | 5 | 10 | 4.8 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| CHEMBL408415 | 157987 | None | 0 | Human | Binding | pIC50 | = | 10.3 | 10.3 | - | 0 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 879 | 13 | 5 | 10 | 4.8 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| 44403861 | 72047 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| CHEMBL197529 | 72047 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 867 | 12 | 5 | 8 | 4.4 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| 57404535 | 73824 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018517 | 73824 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 57404496 | 74227 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 1 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 602 | 6 | 2 | 8 | 4.4 | Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2023191 | 74227 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 1 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 602 | 6 | 2 | 8 | 4.4 | Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 10416497 | 73811 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018504 | 73811 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 625 | 7 | 2 | 5 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 57404529 | 74225 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 612 | 6 | 2 | 6 | 5.8 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2023189 | 74225 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 612 | 6 | 2 | 6 | 5.8 | Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70683493 | 74226 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 629 | 6 | 2 | 6 | 5.6 | Cc1cc(CC(OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2023190 | 74226 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 629 | 6 | 2 | 6 | 5.6 | Cc1cc(CC(OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70696079 | 74146 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 618 | 7 | 2 | 6 | 6.8 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022606 | 74146 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 618 | 7 | 2 | 6 | 6.8 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70696075 | 74141 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 607 | 7 | 2 | 6 | 6.2 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022601 | 74141 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 607 | 7 | 2 | 6 | 6.2 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70687597 | 73814 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 637 | 8 | 2 | 6 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018507 | 73814 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 637 | 8 | 2 | 6 | 4.9 | Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 70681361 | 74143 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 604 | 7 | 2 | 6 | 6.4 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022603 | 74143 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 604 | 7 | 2 | 6 | 6.4 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 11308219 | 73812 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 643 | 7 | 2 | 5 | 5.1 | Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018505 | 73812 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 643 | 7 | 2 | 5 | 5.1 | Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 44403860 | 141150 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 1 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 853 | 12 | 5 | 10 | 4.3 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| CHEMBL382469 | 141150 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 1 | Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40 |
ChEMBL | 853 | 12 | 5 | 10 | 4.3 | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 | 10.1021/jm0490641 | ||
| 57404534 | 73826 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 643 | 7 | 2 | 5 | 5.1 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| CHEMBL2018519 | 73826 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting |
ChEMBL | 643 | 7 | 2 | 5 | 5.1 | Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.066 | ||
| 11364682 | 74418 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 538 | 6 | 2 | 6 | 5.0 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2024603 | 74418 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 538 | 6 | 2 | 6 | 5.0 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70696077 | 74144 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 590 | 7 | 2 | 6 | 6.0 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022604 | 74144 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 590 | 7 | 2 | 6 | 6.0 | Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCC3)ccn2)cc2cn[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| 70681362 | 74149 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 586 | 6 | 2 | 5 | 6.9 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(-c3ccccc3)n[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
| CHEMBL2022609 | 74149 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting |
ChEMBL | 586 | 6 | 2 | 5 | 6.9 | Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(-c3ccccc3)n[nH]c12 | 10.1016/j.bmcl.2012.02.065 | ||
Showing 1 to 50 of 1,406 entries