Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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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
CHEMBL508349 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
57404529 74225 None 0 Human Functional pIC50 = 10.2 10.2 - 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 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 Functional pIC50 = 10.2 10.2 - 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 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
10416497 73811 None 0 Human Functional pIC50 = 10.2 10.2 - 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(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 Functional pIC50 = 10.2 10.2 - 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(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11592648 188534 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 639 7 2 7 4.9 Cc1cc(C[C@@H](OC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
CHEMBL502243 188534 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 639 7 2 7 4.9 Cc1cc(C[C@@H](OC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
46885183 8340 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092882 8340 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
11422298 92385 None 0 Human Functional pIC50 = 10.1 10.1 - 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 7 3 6 6.0 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)cc(Cl)n1 10.1016/j.bmcl.2013.08.031
CHEMBL2430167 92385 None 0 Human Functional pIC50 = 10.1 10.1 - 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 7 3 6 6.0 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)cc(Cl)n1 10.1016/j.bmcl.2013.08.031
57404534 73826 None 0 Human Functional pIC50 = 10.1 10.1 - 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 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 Functional pIC50 = 10.1 10.1 - 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 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
11308219 73812 None 0 Human Functional pIC50 = 10.1 10.1 - 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 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 Functional pIC50 = 10.1 10.1 - 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 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
164614302 185448 None 0 Human Functional pIC50 = 10.1 10.1 - 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 646 5 2 5 4.5 CCn1c(=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
CHEMBL4859941 185448 None 0 Human Functional pIC50 = 10.1 10.1 - 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 646 5 2 5 4.5 CCn1c(=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
50939479 92530 None 1 Human Functional pIC50 = 10.0 10.0 - 1
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assayAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431248 92530 None 1 Human Functional pIC50 = 10.0 10.0 - 1
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assayAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
11308069 74140 None 0 Human Functional pIC50 = 10 10.0 - 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 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022600 74140 None 0 Human Functional pIC50 = 10 10.0 - 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 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70681361 74143 None 0 Human Functional pIC50 = 10 10.0 - 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 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 Functional pIC50 = 10 10.0 - 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 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
164614208 185310 None 0 Human Functional pIC50 = 9.9 9.9 - 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 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4857649 185310 None 0 Human Functional pIC50 = 9.9 9.9 - 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 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
70681270 73815 None 0 Human Functional pIC50 = 9.9 9.9 - 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 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018508 73815 None 0 Human Functional pIC50 = 9.9 9.9 - 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 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
45485692 201456 None 0 Human Functional pIC50 = 9.9 9.9 - 1
Antagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
CHEMBL585568 201456 None 0 Human Functional pIC50 = 9.9 9.9 - 1
Antagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
11478962 92387 None 0 Human Functional pIC50 = 9.9 9.9 - 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 603 7 3 6 5.3 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)ccn1 10.1016/j.bmcl.2013.08.031
CHEMBL2430169 92387 None 0 Human Functional pIC50 = 9.9 9.9 - 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 603 7 3 6 5.3 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)ccn1 10.1016/j.bmcl.2013.08.031
11599872 189033 None 1 Human Functional pIC50 = 9.9 9.9 - 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 636 6 2 6 5.1 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(c3ccc(F)cc3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
CHEMBL507893 189033 None 1 Human Functional pIC50 = 9.9 9.9 - 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 636 6 2 6 5.1 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(c3ccc(F)cc3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
44583379 188368 None 0 Human Functional pIC50 = 9.7 9.7 - 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 608 6 1 6 5.8 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4cn3)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
CHEMBL499810 188368 None 0 Human Functional pIC50 = 9.7 9.7 - 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 608 6 1 6 5.8 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4cn3)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
11204498 92395 None 0 Human Functional pIC50 = 9.7 9.7 - 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 644 7 3 5 6.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(C(C)(C)C)cc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430177 92395 None 0 Human Functional pIC50 = 9.7 9.7 - 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 644 7 3 5 6.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(C(C)(C)C)cc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54581910 61536 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
CHEMBL1770729 61536 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
46174937 76609 None 8 Human Functional pIC50 = 9.7 9.7 - 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 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
CHEMBL2063115 76609 None 8 Human Functional pIC50 = 9.7 9.7 - 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 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
72191391 92384 None 0 Human Functional pIC50 = 9.7 9.7 - 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 633 6 2 7 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(C2CCCCC2)C3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430166 92384 None 0 Human Functional pIC50 = 9.7 9.7 - 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 633 6 2 7 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(C2CCCCC2)C3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
56944164 75114 None 5 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serumAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serum
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serumAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serum
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
54580850 61531 None 1 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770724 61531 None 1 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54586725 61535 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770728 61535 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
72191392 92383 None 0 Human Functional pIC50 = 9.6 9.6 - 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 641 7 2 7 6.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(Cc2ccccc2)C3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430165 92383 None 0 Human Functional pIC50 = 9.6 9.6 - 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 641 7 2 7 6.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(Cc2ccccc2)C3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
17751102 180045 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4746351 180045 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
11364682 74418 None 0 Human Functional pIC50 = 9.6 9.6 - 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 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 Functional pIC50 = 9.6 9.6 - 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 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
25181509 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
25181509 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
25181509 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
59555187 105236 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114495 105236 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
54585731 61522 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770715 61522 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54583843 61533 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770726 61533 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
70685595 74224 None 0 Human Functional pIC50 = 9.5 9.5 - 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 612 6 2 6 5.8 Cc1cc(CC(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
CHEMBL2023188 74224 None 0 Human Functional pIC50 = 9.5 9.5 - 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 612 6 2 6 5.8 Cc1cc(CC(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
56944164 75114 None 5 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serumAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serum
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serumAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serum
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
11169454 73813 None 0 Human Functional pIC50 = 9.5 9.5 - 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 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018506 73813 None 0 Human Functional pIC50 = 9.5 9.5 - 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 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
54580803 61504 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770557 61504 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
72190778 92392 None 0 Human Functional pIC50 = 9.4 9.4 - 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 620 7 3 5 6.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(C)n2Cc2cccc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430174 92392 None 0 Human Functional pIC50 = 9.4 9.4 - 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 620 7 3 5 6.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(C)n2Cc2cccc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
50939479 92530 None 1 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay in presence of human serumAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay in presence of human serum
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431248 92530 None 1 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay in presence of human serumAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay in presence of human serum
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
72190777 92394 None 0 Human Functional pIC50 = 9.4 9.4 - 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 702 7 3 5 6.7 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)cn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430176 92394 None 0 Human Functional pIC50 = 9.4 9.4 - 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 702 7 3 5 6.7 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)cn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11411030 92396 None 0 Human Functional pIC50 = 9.4 9.4 - 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 624 7 3 5 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430178 92396 None 0 Human Functional pIC50 = 9.4 9.4 - 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 624 7 3 5 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11706981 61527 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770720 61527 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
54586725 61535 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770728 61535 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11238677 92388 None 0 Human Functional pIC50 = 9.4 9.4 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccnc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430170 92388 None 0 Human Functional pIC50 = 9.4 9.4 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccnc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11786642 74410 None 0 Human Functional pIC50 = 9.3 9.3 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024595 74410 None 0 Human Functional pIC50 = 9.3 9.3 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
46885244 7795 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089433 7795 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
59554856 105237 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114496 105237 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
54581909 61530 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770723 61530 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54585731 61522 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770715 61522 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
45267476 198740 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL562069 198740 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11606400 61515 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770568 61515 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
25181509 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
25181509 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
45485605 200110 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
CHEMBL570933 200110 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity at human cloned CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
25181509 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL512773 189474 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
54580838 61521 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770714 61521 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54580850 61531 None 1 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770724 61531 None 1 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11295951 74414 None 0 Human Functional pIC50 = 9.2 9.2 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024599 74414 None 0 Human Functional pIC50 = 9.2 9.2 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11250445 92397 None 0 Human Functional pIC50 = 9.2 9.2 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430179 92397 None 0 Human Functional pIC50 = 9.2 9.2 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccc(F)c2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54583844 61534 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770727 61534 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
46885299 8210 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092208 8210 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
24756690 73810 None 0 Human Functional pIC50 = 9.2 9.2 - 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 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018503 73810 None 0 Human Functional pIC50 = 9.2 9.2 - 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 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
54581910 61536 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
CHEMBL1770729 61536 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
57794685 92403 None 0 Human Functional pIC50 = 9.1 9.1 - 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 588 7 3 5 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430185 92403 None 0 Human Functional pIC50 = 9.1 9.1 - 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 588 7 3 5 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54586710 61526 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770719 61526 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11215446 74409 None 0 Human Functional pIC50 = 9.1 9.1 - 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 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024594 74409 None 0 Human Functional pIC50 = 9.1 9.1 - 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 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
54583842 61529 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770722 61529 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
11478841 92386 None 0 Human Functional pIC50 = 9.1 9.1 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccncc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430168 92386 None 0 Human Functional pIC50 = 9.1 9.1 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccncc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54587762 61532 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770725 61532 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
46885242 8329 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092837 8329 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
44570616 190323 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL517467 190323 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
11456201 92400 None 0 Human Functional pIC50 = 9.1 9.1 - 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 602 8 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2CCc2ccccc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430182 92400 None 0 Human Functional pIC50 = 9.1 9.1 - 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 602 8 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2CCc2ccccc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
46905052 10421 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
CHEMBL1162991 10421 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
44593545 178559 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
71819577 145389 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@@H]1c2cccnc2[C@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
CHEMBL3913150 145389 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@@H]1c2cccnc2[C@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
54587752 61523 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770716 61523 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11341642 74404 None 0 Human Functional pIC50 = 9.0 9.0 - 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 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024589 74404 None 0 Human Functional pIC50 = 9.0 9.0 - 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 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11250446 92398 None 0 Human Functional pIC50 = 9.0 9.0 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(F)cc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430180 92398 None 0 Human Functional pIC50 = 9.0 9.0 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(F)cc2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11467108 74413 None 0 Human Functional pIC50 = 9 9.0 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024598 74413 None 0 Human Functional pIC50 = 9 9.0 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
76321477 105261 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114676 105261 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
23656921 90256 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238276 90256 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
46885185 7971 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1090515 7971 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
54583842 61529 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770722 61529 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
11192748 74405 None 0 Human Functional pIC50 = 8.9 8.9 - 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 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024590 74405 None 0 Human Functional pIC50 = 8.9 8.9 - 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 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
45267481 199118 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
CHEMBL564487 199118 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
46885244 7795 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089433 7795 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
11520007 61524 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770717 61524 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54586710 61526 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770719 61526 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11226747 74411 None 0 Human Functional pIC50 = 8.9 8.9 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024596 74411 None 0 Human Functional pIC50 = 8.9 8.9 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
54587762 61532 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770725 61532 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
46885299 8210 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092208 8210 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
54582783 61503 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770556 61503 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11456078 92389 None 0 Human Functional pIC50 = 8.8 8.8 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430171 92389 None 0 Human Functional pIC50 = 8.8 8.8 - 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 589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
44570579 190940 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL518422 190940 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
54581897 61525 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770718 61525 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54581909 61530 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770723 61530 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
73355345 92382 None 0 Human Functional pIC50 = 8.8 8.8 - 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 579 6 2 7 5.0 CCN1CCn2c(cnc2C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1 10.1016/j.bmcl.2013.08.031
CHEMBL2430164 92382 None 0 Human Functional pIC50 = 8.8 8.8 - 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 579 6 2 7 5.0 CCN1CCn2c(cnc2C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1 10.1016/j.bmcl.2013.08.031
46885135 8038 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090848 8038 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11599135 188408 None 0 Human Functional pIC50 = 8.7 8.7 - 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 541 5 2 5 4.7 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
CHEMBL500384 188408 None 0 Human Functional pIC50 = 8.7 8.7 - 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 541 5 2 5 4.7 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2009.04.150
54580838 61521 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770714 61521 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11466363 74408 None 0 Human Functional pIC50 = 8.7 8.7 - 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 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024593 74408 None 0 Human Functional pIC50 = 8.7 8.7 - 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 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11169408 92399 None 0 Human Functional pIC50 = 8.7 8.7 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2F)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430181 92399 None 0 Human Functional pIC50 = 8.7 8.7 - 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 606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2F)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
44563028 194674 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
CHEMBL530116 194674 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
59555048 105227 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114486 105227 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11387595 147070 None 1 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392635 147070 None 1 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11752904 147439 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392937 147439 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44570498 184146 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL482178 184146 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44416824 80314 None 0 Human Functional pIC50 = 7 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
CHEMBL213976 80314 None 0 Human Functional pIC50 = 7 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
135461116 141640 None 0 Human Functional pIC50 = 7 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384799 141640 None 0 Human Functional pIC50 = 7 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
58864267 73798 None 0 Human Functional pIC50 = 7 7.0 - 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 649 7 3 5 4.7 O=C(Nc1ccccc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018491 73798 None 0 Human Functional pIC50 = 7 7.0 - 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 649 7 3 5 4.7 O=C(Nc1ccccc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
23656587 90255 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238275 90255 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11848908 95498 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257094 95498 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11848647 155453 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL403373 155453 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44416912 80888 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215274 80888 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
16115156 97259 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1221 29 12 14 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)N[C@H]1CC[C@H]2CC[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm061343w
CHEMBL268420 97259 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1221 29 12 14 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)N[C@H]1CC[C@H]2CC[C@@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm061343w
11495985 95723 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258070 95723 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11319053 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
70689654 73825 None 0 Human Functional pIC50 = 8.0 8.0 - 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
CHEMBL2018518 73825 None 0 Human Functional pIC50 = 8.0 8.0 - 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
11319053 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
11319053 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
11526993 200048 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
CHEMBL570531 200048 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
11319053 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
11526993 200048 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
CHEMBL570531 200048 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
11584808 200144 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
CHEMBL571203 200144 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
44420228 84271 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL221009 84271 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44420255 137972 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL376292 137972 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
72194610 152680 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3971889 152680 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
11432505 200089 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570793 200089 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
11215322 141865 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386113 141865 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
11848966 95455 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256901 95455 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11848857 95264 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255999 95264 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44563200 174594 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL455458 174594 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
44593445 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
CHEMBL519421 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
11678239 61507 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770560 61507 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54582784 61511 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770564 61511 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54581838 61509 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770562 61509 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54583774 61510 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770563 61510 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44593445 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL519421 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
44563125 173931 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL453865 173931 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
58864421 73804 None 0 Human Functional pIC50 = 6.9 6.9 - 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 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018497 73804 None 0 Human Functional pIC50 = 6.9 6.9 - 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 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
11375696 92393 None 0 Human Functional pIC50 = 6.9 6.9 - 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 512 5 4 4 4.4 Cc1c[nH]c(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2013.08.031
CHEMBL2430175 92393 None 0 Human Functional pIC50 = 6.9 6.9 - 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 512 5 4 4 4.4 Cc1c[nH]c(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2013.08.031
11351794 91014 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL239630 91014 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11599531 200902 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577320 200902 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44420228 84271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221009 84271 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420228 84271 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL221009 84271 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44562936 179042 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL470321 179042 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563025 192604 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL520905 192604 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563028 194674 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
CHEMBL530116 194674 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
46885184 8341 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1092883 8341 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11706251 200981 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
CHEMBL577957 200981 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
59555056 105201 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114460 105201 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
44563052 186141 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
CHEMBL487068 186141 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
44563200 174594 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL455458 174594 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
54583844 61534 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770727 61534 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11191890 74326 None 0 Human Functional pIC50 = 7.9 7.9 - 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 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024172 74326 None 0 Human Functional pIC50 = 7.9 7.9 - 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 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
46905052 10421 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
CHEMBL1162991 10421 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
45487036 200082 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
CHEMBL570748 200082 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
11692628 200081 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL570746 200081 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
44593545 178559 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
44562984 186148 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL487077 186148 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
44563091 192649 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL521076 192649 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59555245 105210 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114469 105210 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11330650 162031 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL415453 162031 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
59554947 105228 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114487 105228 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11215502 166230 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL426142 166230 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
11342207 141626 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384723 141626 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
11707040 81109 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215499 81109 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44563162 174681 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL455674 174681 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
44593445 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
CHEMBL519421 191638 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
11215412 74415 None 0 Human Functional pIC50 = 7.9 7.9 - 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 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024600 74415 None 0 Human Functional pIC50 = 7.9 7.9 - 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 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11397560 89742 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237661 89742 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
46885135 8038 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090848 8038 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
44563052 186141 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
CHEMBL487068 186141 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
44420286 84289 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221160 84289 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44455153 97520 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270175 97520 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11849024 155373 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402887 155373 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
54582784 61511 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770564 61511 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
23656920 89182 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL236590 89182 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11284233 89921 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237849 89921 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44562982 186147 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487076 186147 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563091 192649 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL521076 192649 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563050 186753 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488082 186753 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
23656918 91828 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241118 91828 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
122238743 160853 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL4114031 160853 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 nan
44563026 186749 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL488065 186749 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
59554867 105266 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114681 105266 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11848755 95432 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
CHEMBL256802 95432 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
11519899 141574 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL384408 141574 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
11365194 140822 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL381798 140822 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
23656922 168959 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL438120 168959 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
59555260 105216 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114475 105216 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
44570536 183979 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL480999 183979 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
11848908 95498 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257094 95498 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555152 105214 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114473 105214 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
11848855 97641 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270796 97641 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44420240 83508 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL220101 83508 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
11785754 74402 None 0 Human Functional pIC50 = 7.8 7.8 - 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 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
CHEMBL2024587 74402 None 0 Human Functional pIC50 = 7.8 7.8 - 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 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
11849025 95538 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL257252 95538 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
59554953 105211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114470 105211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
44420231 137130 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374666 137130 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
23656749 91614 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240686 91614 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11261842 81094 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215424 81094 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44455080 95681 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257902 95681 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11848965 166795 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL428247 166795 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11691938 61505 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770558 61505 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59555331 105229 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114488 105229 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555277 105213 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114472 105213 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
72194610 152680 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3971889 152680 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
11650307 80549 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL214800 80549 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
11319053 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11706981 61527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770720 61527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
59555031 105235 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114494 105235 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
21102037 73818 None 0 Human Functional pIC50 = 8.7 8.7 - 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 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018511 73818 None 0 Human Functional pIC50 = 8.7 8.7 - 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 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11364735 89743 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237662 89743 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11753021 89744 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237663 89744 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11387595 147070 None 1 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392635 147070 None 1 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11432931 162006 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL415263 162006 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11192602 147073 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392636 147073 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
45267476 198740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL562069 198740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11319053 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
11387141 74417 None 0 Human Functional pIC50 = 8.7 8.7 - 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 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024602 74417 None 0 Human Functional pIC50 = 8.7 8.7 - 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 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11319053 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against human CGRP receptor by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor by cell based cAMP accumulation assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against human CGRP receptor by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor by cell based cAMP accumulation assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
46885243 8330 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092838 8330 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
54584803 61528 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770721 61528 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
25227362 173837 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL453643 173837 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
54582783 61503 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770556 61503 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11319053 89187 None 36 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
CHEMBL236593 89187 None 36 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
23582940 199058 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
25227362 173837 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL453643 173837 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
44593545 178559 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
46885183 8340 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092882 8340 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
44570614 177706 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464078 177706 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11541560 61513 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770566 61513 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54580803 61504 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770557 61504 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54584803 61528 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770721 61528 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11692628 200081 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL570746 200081 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
54583843 61533 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770726 61533 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
72191699 92381 None 0 Human Functional pIC50 = 8.5 8.5 - 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 551 5 3 7 4.3 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCNC3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430163 92381 None 0 Human Functional pIC50 = 8.5 8.5 - 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 551 5 3 7 4.3 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCNC3)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11443894 74325 None 0 Human Functional pIC50 = 7.7 7.7 - 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 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024171 74325 None 0 Human Functional pIC50 = 7.7 7.7 - 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 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
44562897 179172 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471530 179172 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11848964 95257 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255966 95257 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44563162 174681 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL455674 174681 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
11753021 89744 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237663 89744 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45487036 200082 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
CHEMBL570748 200082 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
59555008 105212 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114471 105212 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
11397560 89742 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237661 89742 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11225752 89745 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237664 89745 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
72194611 149252 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3943580 149252 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
117992045 154233 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 555 3 2 5 5.2 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3985425 154233 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 555 3 2 5 5.2 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
44416514 155825 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405544 155825 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44563161 173838 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL453644 173838 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
11454113 145840 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL391660 145840 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
46905052 10421 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
CHEMBL1162991 10421 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
44570499 192505 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL520778 192505 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
11157626 166531 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL427743 166531 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44562895 179148 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL471358 179148 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
44593445 191638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
CHEMBL519421 191638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
23656920 89182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL236590 89182 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45271754 197301 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL549503 197301 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11548734 200880 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577110 200880 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44593445 191638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL519421 191638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
58901616 73806 None 0 Human Functional pIC50 = 6.6 6.6 - 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018499 73806 None 0 Human Functional pIC50 = 6.6 6.6 - 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44563160 174679 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 174679 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
23582940 199058 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570614 177706 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464078 177706 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420236 137676 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375533 137676 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
76310534 105206 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114465 105206 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
23656918 91828 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241118 91828 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11454113 145840 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL391660 145840 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44563090 186754 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 186754 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
11678239 61507 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770560 61507 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44562937 179199 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 179199 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44570499 192505 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL520778 192505 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44570580 177552 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 177552 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11692140 61508 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 61508 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
11238250 74135 None 0 Human Functional pIC50 = 7.6 7.6 - 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022595 74135 None 0 Human Functional pIC50 = 7.6 7.6 - 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
44563123 188994 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL507339 188994 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11848855 97641 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270796 97641 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11849020 95100 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 95100 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11444589 79820 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL211931 79820 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
117992192 147349 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@@H]1c2cccnc2[C@@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
CHEMBL3928622 147349 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@@H]1c2cccnc2[C@@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
10340456 83542 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL220336 83542 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
59555236 105207 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114466 105207 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59554895 105231 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114490 105231 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11192602 147073 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392636 147073 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11364735 89743 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237662 89743 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23657089 147068 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 147068 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45271754 197301 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL549503 197301 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11606400 61515 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770568 61515 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11584808 200144 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
CHEMBL571203 200144 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
11341430 74416 None 0 Human Functional pIC50 = 8.5 8.5 - 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
CHEMBL2024601 74416 None 0 Human Functional pIC50 = 8.5 8.5 - 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
11721278 61514 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 61514 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44563160 174679 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 174679 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11249157 74406 None 0 Human Functional pIC50 = 7.5 7.5 - 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024591 74406 None 0 Human Functional pIC50 = 7.5 7.5 - 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11375693 89920 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 89920 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
58864453 73721 None 0 Human Functional pIC50 = 6.5 6.5 - 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018356 73721 None 0 Human Functional pIC50 = 6.5 6.5 - 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11848963 155524 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL403765 155524 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455457 95263 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 95263 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44563161 173838 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL453644 173838 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
46905052 10421 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
CHEMBL1162991 10421 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
11497403 166171 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL425807 166171 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
70685453 73801 None 0 Human Functional pIC50 = 7.5 7.5 - 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018494 73801 None 0 Human Functional pIC50 = 7.5 7.5 - 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
59554855 105197 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114456 105197 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
10483468 73822 None 0 Human Functional pIC50 = 6.5 6.5 - 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018515 73822 None 0 Human Functional pIC50 = 6.5 6.5 - 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11699891 61506 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 61506 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59554993 105230 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114489 105230 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
46885184 8341 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1092883 8341 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11848750 95640 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257731 95640 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
10453991 137967 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL376263 137967 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44455043 95779 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258329 95779 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11410749 165924 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL424864 165924 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11541560 61513 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770566 61513 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
24756768 73819 None 0 Human Functional pIC50 = 7.5 7.5 - 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018512 73819 None 0 Human Functional pIC50 = 7.5 7.5 - 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
23656919 154835 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL400020 154835 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11168000 154272 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 154272 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11848968 95258 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255967 95258 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44570579 190940 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL518422 190940 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420287 83471 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL219782 83471 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL2371945 212616 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)NN(C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
59554975 105224 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114483 105224 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
11849147 95306 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256203 95306 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
44417050 141596 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384539 141596 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
11541725 141473 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL383872 141473 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
45273525 198142 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 198142 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
45269221 199113 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 199113 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44563028 194674 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serum
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
CHEMBL530116 194674 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% rhesus monkey serum
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
59554982 105198 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114457 105198 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
24853374 105264 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114679 105264 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
44416436 80586 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214873 80586 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
11168000 154272 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 154272 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
23656752 91779 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 91779 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
72194744 153001 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 537 3 2 5 4.7 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3974762 153001 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 537 3 2 5 4.7 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
44420691 161997 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 12 14 -1.7 CC(C)[C@H](NC(=O)N(CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL415186 161997 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 12 14 -1.7 CC(C)[C@H](NC(=O)N(CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44570615 177707 None 13 Human Functional pIC50 = 7.4 7.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 177707 None 13 Human Functional pIC50 = 7.4 7.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420241 136799 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374064 136799 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44455457 95263 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 95263 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
54587752 61523 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770716 61523 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
6918509 77070 None 33 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
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.2013.12.089
CHEMBL207197 77070 None 33 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
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.2013.12.089
59555074 105225 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114484 105225 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
23657089 147068 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 147068 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
54581838 61509 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770562 61509 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54583775 61512 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 61512 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11295168 74407 None 0 Human Functional pIC50 = 8.4 8.4 - 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024592 74407 None 0 Human Functional pIC50 = 8.4 8.4 - 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
45271740 199002 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 199002 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
46885242 8329 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092837 8329 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
44570616 190323 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL517467 190323 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
54581897 61525 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770718 61525 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
72194609 160756 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 537 3 2 5 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL4113356 160756 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 537 3 2 5 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
70695974 73827 None 0 Human Functional pIC50 = 8.3 8.3 - 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 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
CHEMBL2018520 73827 None 0 Human Functional pIC50 = 8.3 8.3 - 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 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
46885134 8037 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 8037 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11398863 74412 None 0 Human Functional pIC50 = 8.3 8.3 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024597 74412 None 0 Human Functional pIC50 = 8.3 8.3 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11273798 92390 None 0 Human Functional pIC50 = 8.3 8.3 - 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 654 5 4 4 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)c(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430172 92390 None 0 Human Functional pIC50 = 8.3 8.3 - 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 654 5 4 4 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)c(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11785573 92402 None 0 Human Functional pIC50 = 8.3 8.3 - 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 512 5 3 5 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2C)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430184 92402 None 0 Human Functional pIC50 = 8.3 8.3 - 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 512 5 3 5 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2C)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
24853164 105217 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114476 105217 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44563089 186266 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 186266 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
44562897 179172 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471530 179172 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44570578 178515 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 178515 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44563090 186754 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 186754 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
44563126 189041 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 189041 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
46885186 8035 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 8035 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11786529 139618 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL379548 139618 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
44420227 83464 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL219721 83464 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44417049 168922 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL437718 168922 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44563089 186266 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 186266 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
59554936 105218 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114477 105218 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
59555036 105223 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114482 105223 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11432505 200089 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570793 200089 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
46885245 7849 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 7849 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
44562937 179199 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 179199 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44416437 141881 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386204 141881 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
11423175 137065 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 949 23 11 12 -2.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCCN1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL374579 137065 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 949 23 11 12 -2.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCCN1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
59555102 105265 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114680 105265 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11549001 141966 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386701 141966 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44563027 186750 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL488066 186750 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
44562983 191496 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 191496 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
59555274 105200 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114459 105200 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11628731 80424 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214507 80424 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
76332330 105262 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114677 105262 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
58864250 73799 None 0 Human Functional pIC50 = 7.3 7.3 - 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018492 73799 None 0 Human Functional pIC50 = 7.3 7.3 - 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
122238743 160853 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL4114031 160853 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 nan
44455078 95641 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257732 95641 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
72194610 152680 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3971889 152680 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
59554876 105202 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114461 105202 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11421827 157696 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL408093 157696 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
11421827 157696 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 157696 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
44562939 179201 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 179201 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11495985 95723 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258070 95723 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11284233 89921 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237849 89921 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11752904 147439 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392937 147439 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11180666 147182 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 147182 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11512928 141758 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
CHEMBL385454 141758 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
44570580 177552 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 177552 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
23582940 199058 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
25227362 173837 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL453643 173837 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
25227362 173837 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL453643 173837 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
44593545 178559 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
44563050 186753 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488082 186753 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
44570615 177707 None 13 Human Functional pIC50 = 8.2 8.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 177707 None 13 Human Functional pIC50 = 8.2 8.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
10438558 73816 None 0 Human Functional pIC50 = 8.2 8.2 - 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018509 73816 None 0 Human Functional pIC50 = 8.2 8.2 - 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
46885133 8036 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 8036 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
44420260 83513 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220146 83513 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420250 137015 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374251 137015 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
59555111 105195 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114454 105195 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59555024 105205 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114464 105205 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11453687 167552 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 167552 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
24756769 73821 None 0 Human Functional pIC50 = 7.3 7.3 - 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018514 73821 None 0 Human Functional pIC50 = 7.3 7.3 - 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
44420235 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
45273525 198142 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 198142 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
44420235 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
44420235 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 84808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
9978597 141729 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
CHEMBL385322 141729 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
44420245 84038 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
CHEMBL220715 84038 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
44454954 95438 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL256813 95438 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487057 200264 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 200264 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
11849024 155373 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402887 155373 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455041 170700 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL445069 170700 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44570536 183979 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL480999 183979 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
72194743 160157 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 555 3 2 5 5.2 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)[C@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL4108361 160157 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay C: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay C): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 3,500 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 555 3 2 5 5.2 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)[C@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
44420693 168580 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 12 14 -1.4 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL435149 168580 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 12 14 -1.4 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL438426 216232 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)N(N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44562896 179149 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471359 179149 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
58864479 73805 None 0 Human Functional pIC50 = 7.2 7.2 - 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018498 73805 None 0 Human Functional pIC50 = 7.2 7.2 - 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44562938 179200 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471705 179200 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
11753024 74403 None 0 Human Functional pIC50 = 8.2 8.2 - 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024588 74403 None 0 Human Functional pIC50 = 8.2 8.2 - 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11375693 89920 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 89920 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23656921 90256 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238276 90256 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
72194608 144267 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@H]1c2cccnc2[C@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
CHEMBL3904139 144267 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@H]1c2cccnc2[C@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
45267481 199118 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
CHEMBL564487 199118 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
46885243 8330 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092838 8330 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11691938 61505 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770558 61505 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
21102038 73820 None 0 Human Functional pIC50 = 8.2 8.2 - 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018513 73820 None 0 Human Functional pIC50 = 8.2 8.2 - 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
44562939 179201 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 179201 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59555157 105215 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114474 105215 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
11555955 200181 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 200181 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
44420240 83508 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL220101 83508 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420240 83508 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220101 83508 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11456102 80076 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL212942 80076 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
59554885 105220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
CHEMBL3114479 105220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
23656752 91779 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 91779 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11330786 138475 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL377252 138475 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44562985 186268 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487244 186268 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
11721278 61514 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 61514 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44420256 84981 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223756 84981 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420261 137370 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375224 137370 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
59555066 105234 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114493 105234 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11351794 91014 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL239630 91014 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
117992083 144983 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@H]1c2cccnc2[C@@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
CHEMBL3910081 144983 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 552 3 3 6 4.2 N[C@H]1c2cccnc2[C@@H](NC(=O)c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)CC[C@H]1c1cccc(F)c1F nan
11849023 95211 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255755 95211 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11848800 155362 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL402844 155362 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45271740 199002 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 199002 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
44420692 161846 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 13 14 -1.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NNC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL413872 161846 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL 1196 28 13 14 -1.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NNC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
11692206 80240 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213670 80240 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
10340395 85029 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL223805 85029 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
11599531 200902 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577320 200902 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
11699891 61506 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 61506 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
45269221 199113 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 199113 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46885245 7849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 7849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
46885186 8035 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 8035 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
54583775 61512 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 61512 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11444574 92391 None 0 Human Functional pIC50 = 8.1 8.1 - 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 576 5 4 4 4.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430173 92391 None 0 Human Functional pIC50 = 8.1 8.1 - 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 576 5 4 4 4.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54583774 61510 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770563 61510 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11453687 167552 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 167552 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL376719 214715 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
24853163 105204 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114463 105204 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416512 155824 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405543 155824 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44455153 97520 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270175 97520 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44563051 186781 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488255 186781 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
59554934 105233 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114492 105233 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11421827 157696 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 157696 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
11571094 141977 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386757 141977 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44570498 184146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL482178 184146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
76310551 105263 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114678 105263 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59554924 105208 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114467 105208 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
23656749 91614 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240686 91614 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44562936 179042 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL470321 179042 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563126 189041 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 189041 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serumAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production in presence of 50% human serum
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59554857 105199 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114458 105199 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL223642 211904 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP productionAntagonist activity against human CGRP1 expressed in HEK293 cells assessed as inhibition of human alpha-CGRP-promoted cAMP production
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44420235 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44420235 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP productionAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
44420235 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420235 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223156 84808 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
72194611 149252 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3943580 149252 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).Recombinant Receptor Functional Assay B: RECOMBINANT RECEPTOR FUNCTIONAL ASSAY (Assay B): Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 uM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio).
ChEMBL 487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
44563025 192604 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL520905 192604 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
11520022 80595 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214904 80595 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11555955 200181 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 200181 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
11225752 89745 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237664 89745 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11180666 147182 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 147182 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11432931 162006 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL415263 162006 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23656922 168959 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL438120 168959 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serumAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23582940 199058 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11156698 74327 None 0 Human Functional pIC50 = 8.1 8.1 - 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024173 74327 None 0 Human Functional pIC50 = 8.1 8.1 - 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
11520007 61524 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770717 61524 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serumAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
44570578 178515 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 178515 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP productionAntagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11692140 61508 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 61508 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assayAntagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
11432183 74324 None 0 Human Functional pIC50 = 8.1 8.1 - 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024170 74324 None 0 Human Functional pIC50 = 8.1 8.1 - 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
24756767 73817 None 0 Human Functional pIC50 = 8.1 8.1 - 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018510 73817 None 0 Human Functional pIC50 = 8.1 8.1 - 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
59554942 105209 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114468 105209 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11527287 80578 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214829 80578 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46885134 8037 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 8037 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11849025 95538 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL257252 95538 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11848645 97563 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270392 97563 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555055 105232 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114491 105232 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555326 105196 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114455 105196 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11585317 80949 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL215325 80949 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
46885133 8036 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 8036 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
59555012 105219 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114478 105219 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
11548734 200880 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577110 200880 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44455080 95681 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257902 95681 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555230 105221 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114480 105221 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
11848646 97562 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270390 97562 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation by cell based assay
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
23656753 91827 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241117 91827 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP productionAntagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11706251 200981 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
CHEMBL577957 200981 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
76325057 105203 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114462 105203 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
45487057 200264 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 200264 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
46885185 7971 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1090515 7971 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serumAntagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11409395 92401 None 0 Human Functional pIC50 = 7.0 7.0 - 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 498 5 4 4 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430183 92401 None 0 Human Functional pIC50 = 7.0 7.0 - 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 498 5 4 4 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11849020 95100 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 95100 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assayAntagonist activity at human recombinant CL receptor /RAMP1 assessed as inhibition of cAMP accumulation in presence of 50% human serum by cell based assay
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44562983 191496 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 191496 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP productionAntagonist activity against human cloned CGRP receptor expressed in HEK93 cells assessed as inhibition of CGRP-induced cAMP production
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
59555258 105226 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114485 105226 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555100 105222 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114481 105222 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
70693851 73802 None 0 Human Functional pIC50 = 7 7.0 - 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018495 73802 None 0 Human Functional pIC50 = 7 7.0 - 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11713729 80581 None 0 Human Functional pIC50 = 6 6.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL214845 80581 None 0 Human Functional pIC50 = 6 6.0 - 1
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
44403860 141150 None 0 Human Functional pKd = 10.1 10.1 75 2
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
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 Functional pKd = 10.1 10.1 75 2
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
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
56944164 75114 None 5 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to controlAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to control
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to controlAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to control
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44403859 134188 None 0 Human Functional pKd = 9.1 9.1 - 1
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL371646 134188 None 0 Human Functional pKd = 9.1 9.1 - 1
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
44403858 72378 None 0 Human Functional pKd = 8 8.0 - 1
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198502 72378 None 0 Human Functional pKd = 8 8.0 - 1
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
44403855 72498 None 0 Human Functional pKd = 6.9 6.9 354 2
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 72498 None 0 Human Functional pKd = 6.9 6.9 354 2
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
57404496 74227 None 0 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
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 Functional pKi = 9.7 9.7 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
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
25153832 203410 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
CHEMBL601857 203410 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
25153832 203410 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
CHEMBL601857 203410 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
46232565 203267 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccc(Cl)cc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600820 203267 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccc(Cl)cc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152370 203311 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 516 4 1 7 3.6 O=C(Cc1nnc(-c2cc(Cl)cc(Br)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601246 203311 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 516 4 1 7 3.6 O=C(Cc1nnc(-c2cc(Cl)cc(Br)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232822 203495 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602475 203495 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152564 203171 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)ccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600010 203171 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)ccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152563 203914 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 440 4 1 7 2.5 O=C(Cc1nnc(-c2cc(F)cc(F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL604955 203914 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 440 4 1 7 2.5 O=C(Cc1nnc(-c2cc(F)cc(F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25110584 203277 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600837 203277 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25154034 204675 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
CHEMBL609757 204675 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
25152560 203445 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602085 203445 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232822 203495 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602475 203495 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25151968 204733 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL610062 204733 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232591 203580 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cccc(Cl)c2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL603098 203580 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cccc(Cl)c2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151777 203407 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601854 203407 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232693 202014 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 565 6 1 9 3.7 O=C(Cc1nnc(-c2cc(-c3ccccc3)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592406 202014 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 565 6 1 9 3.7 O=C(Cc1nnc(-c2cc(-c3ccccc3)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232562 203839 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 404 4 1 7 2.2 O=C(Cc1nnc(-c2ccccc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL604539 203839 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 404 4 1 7 2.2 O=C(Cc1nnc(-c2ccccc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152169 203276 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 514 5 1 7 4.5 O=C(Cc1nnc(-c2cc(Cl)cc(-c3ccccc3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600836 203276 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 514 5 1 7 4.5 O=C(Cc1nnc(-c2cc(Cl)cc(-c3ccccc3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25154034 204675 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
CHEMBL609757 204675 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
25152561 203296 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 456 4 1 7 3.0 O=C(Cc1nnc(-c2cc(F)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601034 203296 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 456 4 1 7 3.0 O=C(Cc1nnc(-c2cc(F)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152984 203347 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 540 4 1 7 4.2 O=C(Cc1nnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601455 203347 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 540 4 1 7 4.2 O=C(Cc1nnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152985 203446 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 432 4 1 7 2.8 Cc1cc(C)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602086 203446 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 432 4 1 7 2.8 Cc1cc(C)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152167 203372 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601639 203372 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232593 203497 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2ccc(Cl)c(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602492 203497 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2ccc(Cl)c(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232527 203443 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 442 5 1 5 3.8 COc1ccc(-c2ccccc2)cc1CC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602075 203443 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 442 5 1 5 3.8 COc1ccc(-c2ccccc2)cc1CC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151968 204733 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL610062 204733 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
70685595 74224 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(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
CHEMBL2023188 74224 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(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
25154032 202052 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592649 202052 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152766 203248 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 506 4 1 7 3.9 O=C(Cc1nnc(-c2cc(Cl)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600636 203248 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 506 4 1 7 3.9 O=C(Cc1nnc(-c2cc(Cl)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151777 203407 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601854 203407 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232564 203245 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2cccc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600620 203245 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2cccc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152167 203372 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601639 203372 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232777 204039 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL605579 204039 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152981 203295 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 464 6 1 9 2.2 COc1cc(OC)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL601033 203295 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 464 6 1 9 2.2 COc1cc(OC)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
46232777 204039 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL605579 204039 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
46232563 203378 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601657 203378 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25110584 203277 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600837 203277 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152765 204630 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 503 5 1 9 2.3 Cc1cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)cc(N2CCOCC2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL609472 204630 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 503 5 1 9 2.3 Cc1cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)cc(N2CCOCC2)c1 10.1016/j.bmcl.2010.01.012
25152367 203912 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 468 5 1 8 2.8 COc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL604949 203912 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 468 5 1 8 2.8 COc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25154032 202052 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592649 202052 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232592 203172 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2c(Cl)cccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600011 203172 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2c(Cl)cccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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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
70689756 74139 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 587 6 2 6 6.3 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(-c3ccncc3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022599 74139 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 587 6 2 6 6.3 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(-c3ccncc3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11308069 74140 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 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022600 74140 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 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685595 74224 None 0 Human Binding pIC50 = 9.6 9.6 - 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 612 6 2 6 5.8 Cc1cc(CC(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
CHEMBL2023188 74224 None 0 Human Binding pIC50 = 9.6 9.6 - 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 612 6 2 6 5.8 Cc1cc(CC(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
70681270 73815 None 0 Human Binding pIC50 = 9.5 9.5 - 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 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018508 73815 None 0 Human Binding pIC50 = 9.5 9.5 - 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 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
24756690 73810 None 0 Human Binding pIC50 = 9.5 9.5 - 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 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018503 73810 None 0 Human Binding pIC50 = 9.5 9.5 - 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 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
70691910 74138 None 0 Human Binding pIC50 = 9.5 9.5 - 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 581 6 2 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022598 74138 None 0 Human Binding pIC50 = 9.5 9.5 - 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 581 6 2 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685565 74147 None 0 Human Binding pIC50 = 9.5 9.5 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Br)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022607 74147 None 0 Human Binding pIC50 = 9.5 9.5 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Br)n[nH]c12 10.1016/j.bmcl.2012.02.065
11169454 73813 None 0 Human Binding pIC50 = 9.5 9.5 - 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 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018506 73813 None 0 Human Binding pIC50 = 9.5 9.5 - 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 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11786642 74410 None 0 Human Binding pIC50 = 9.4 9.4 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024595 74410 None 0 Human Binding pIC50 = 9.4 9.4 - 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 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685566 74148 None 0 Human Binding pIC50 = 9.4 9.4 - 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 544 5 2 5 5.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Cl)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022608 74148 None 0 Human Binding pIC50 = 9.4 9.4 - 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 544 5 2 5 5.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Cl)n[nH]c12 10.1016/j.bmcl.2012.02.065
11295951 74414 None 0 Human Binding pIC50 = 9.3 9.3 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024599 74414 None 0 Human Binding pIC50 = 9.3 9.3 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11215446 74409 None 0 Human Binding pIC50 = 9.3 9.3 - 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 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024594 74409 None 0 Human Binding pIC50 = 9.3 9.3 - 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 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369463 212078 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](N)[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/jm00090a003
CHEMBL525571 218142 None 22 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](N)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/jm00090a003
CHEMBL525571 218142 None 22 Rat Binding pIC50 = 9.2 9.2 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](N)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/jm00090a003
11467108 74413 None 0 Human Binding pIC50 = 9.1 9.1 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024598 74413 None 0 Human Binding pIC50 = 9.1 9.1 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369463 212078 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](N)[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/jm00090a003
11341642 74404 None 0 Human Binding pIC50 = 9.0 9.0 - 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 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024589 74404 None 0 Human Binding pIC50 = 9.0 9.0 - 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 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696078 74145 None 0 Human Binding pIC50 = 8.9 8.9 - 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 606 7 2 7 5.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCOCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022605 74145 None 0 Human Binding pIC50 = 8.9 8.9 - 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 606 7 2 7 5.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCOCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696080 74150 None 0 Human Binding pIC50 = 8.9 8.9 - 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)c2ccccn2)cc2c(C=O)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022610 74150 None 0 Human Binding pIC50 = 8.9 8.9 - 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)c2ccccn2)cc2c(C=O)n[nH]c12 10.1016/j.bmcl.2012.02.065
11398863 74412 None 0 Human Binding pIC50 = 8.9 8.9 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024597 74412 None 0 Human Binding pIC50 = 8.9 8.9 - 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11466363 74408 None 0 Human Binding pIC50 = 8.8 8.8 - 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 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024593 74408 None 0 Human Binding pIC50 = 8.8 8.8 - 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 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369459 212076 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparationBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation
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/jm00090a003
11192748 74405 None 0 Human Binding pIC50 = 8.7 8.7 - 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 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024590 74405 None 0 Human Binding pIC50 = 8.7 8.7 - 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 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70693987 74222 None 0 Human Binding pIC50 = 8.7 8.7 - 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 609 7 2 7 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCOCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023186 74222 None 0 Human Binding pIC50 = 8.7 8.7 - 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 609 7 2 7 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCOCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369452 212072 None 0 Rat Binding pIC50 = 8 8.0 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](N)Cc1c[nH]cn1)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/jm00090a003
11191890 74326 None 0 Human Binding pIC50 = 8 8.0 - 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 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024172 74326 None 0 Human Binding pIC50 = 8 8.0 - 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 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
44403854 72241 None 0 Human Binding pIC50 = 6 6.0 - 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 787 15 5 8 3.7 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198105 72241 None 0 Human Binding pIC50 = 6 6.0 - 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 787 15 5 8 3.7 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL216229 211780 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL267137 213170 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL267182 213171 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL269027 213233 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL405694 215035 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL409205 215212 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL438008 216203 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL438224 216218 None 0 Human Binding pIC50 = 5 5.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403917 72318 None 0 Human Binding pIC50 = 5.0 5.0 - 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 755 15 4 7 4.2 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198311 72318 None 0 Human Binding pIC50 = 5.0 5.0 - 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 755 15 4 7 4.2 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL2369454 212073 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](C)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
70689654 73825 None 0 Human Binding pIC50 = 8.0 8.0 - 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
CHEMBL2018518 73825 None 0 Human Binding pIC50 = 8.0 8.0 - 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
CHEMBL2369457 212074 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
CHEMBL2369454 212073 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](C)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
70696076 74142 None 0 Human Binding pIC50 = 7.9 7.9 - 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 507 5 2 5 5.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022602 74142 None 0 Human Binding pIC50 = 7.9 7.9 - 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 507 5 2 5 5.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11785754 74402 None 0 Human Binding pIC50 = 7.9 7.9 - 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 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
CHEMBL2024587 74402 None 0 Human Binding pIC50 = 7.9 7.9 - 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 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
11215412 74415 None 0 Human Binding pIC50 = 7.9 7.9 - 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 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024600 74415 None 0 Human Binding pIC50 = 7.9 7.9 - 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 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685454 73808 None 0 Human Binding pIC50 = 6.9 6.9 - 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 700 7 2 5 6.3 O=C(C[C@H](Nc1ccc(Br)c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018501 73808 None 0 Human Binding pIC50 = 6.9 6.9 - 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 700 7 2 5 6.3 O=C(C[C@H](Nc1ccc(Br)c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL216710 211798 None 0 Human Binding pIC50 = 5.9 5.9 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323097 208971 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 494 7 1 5 6.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Oc3ccccc3)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88441 208971 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 494 7 1 5 6.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Oc3ccccc3)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864453 73721 None 0 Human Binding pIC50 = 6.9 6.9 - 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018356 73721 None 0 Human Binding pIC50 = 6.9 6.9 - 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44403853 72444 None 0 Human Binding pIC50 = 4.9 4.9 - 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 745 17 6 6 4.4 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL198762 72444 None 0 Human Binding pIC50 = 4.9 4.9 - 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 745 17 6 6 4.4 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL2369742 212125 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL None None None CC(C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)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(C)C)C(C)C)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 10.1016/0960-894X(95)00078-8
CHEMBL2369457 212074 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
70696851 76537 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccncc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059903 76537 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccncc1)NC2=O 10.1016/j.bmcl.2012.05.118
58864279 73800 None 0 Human Binding pIC50 = 5.9 5.9 - 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 574 7 2 7 3.2 O=C(C[C@H](Nc1ccncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018493 73800 None 0 Human Binding pIC50 = 5.9 5.9 - 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 574 7 2 7 3.2 O=C(C[C@H](Nc1ccncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL376040 214701 None 0 Human Binding pIC50 = 4.9 4.9 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2371143 212474 None 0 Human Binding pIC50 = 6.8 6.8 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCN=C(N)N)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)C(N)=O 10.1021/jm970533r
24756769 73821 None 0 Human Binding pIC50 = 7.8 7.8 - 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018514 73821 None 0 Human Binding pIC50 = 7.8 7.8 - 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
24756612 76532 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 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 Binding pIC50 = 6.8 6.8 - 0
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 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
CHEMBL406459 215069 None 0 Human Binding pIC50 = 6.8 6.8 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2369464 212079 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](N)CCCN=C(N)N)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/jm00090a003
CHEMBL2369464 212079 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](N)CCCN=C(N)N)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/jm00090a003
CHEMBL411804 215418 None 0 Human Binding pIC50 = 6.8 6.8 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
70690619 76529 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 599 5 2 5 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)Nc1ccccc12 10.1016/j.bmcl.2012.05.118
CHEMBL2059895 76529 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 599 5 2 5 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)Nc1ccccc12 10.1016/j.bmcl.2012.05.118
58901616 73806 None 0 Human Binding pIC50 = 6.8 6.8 - 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018499 73806 None 0 Human Binding pIC50 = 6.8 6.8 - 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11534977 72287 None 0 Human Binding pIC50 = 4.8 4.8 - 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 714 17 5 5 4.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL198232 72287 None 0 Human Binding pIC50 = 4.8 4.8 - 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 714 17 5 5 4.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
11578671 71749 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 714 17 5 5 4.9 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm500364u
CHEMBL196582 71749 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 714 17 5 5 4.9 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm500364u
44323001 106237 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 454 5 1 4 5.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(F)c(Cl)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL313797 106237 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 454 5 1 4 5.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(F)c(Cl)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864479 73805 None 0 Human Binding pIC50 = 6.8 6.8 - 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018498 73805 None 0 Human Binding pIC50 = 6.8 6.8 - 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL267406 213178 None 0 Human Binding pIC50 = 4.8 4.8 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
56675112 63357 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
91930235 63357 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL1794015 63357 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
24756768 73819 None 0 Human Binding pIC50 = 7.7 7.7 - 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018512 73819 None 0 Human Binding pIC50 = 7.7 7.7 - 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL3350392 213937 None 0 Human Binding pIC50 = 4.7 4.7 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL2369459 212076 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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/jm00090a003
11226747 74411 None 0 Human Binding pIC50 = 8.7 8.7 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024596 74411 None 0 Human Binding pIC50 = 8.7 8.7 - 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 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11387141 74417 None 0 Human Binding pIC50 = 8.7 8.7 - 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 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024602 74417 None 0 Human Binding pIC50 = 8.7 8.7 - 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 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL3037882 213384 None 0 Human Binding pIC50 = 8.7 8.7 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)
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](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(N)=O)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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL3037882 213384 None 0 Human Binding pIC50 = 8.7 8.7 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
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](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(N)=O)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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL2369463 212078 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](N)[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/jm00090a003
CHEMBL525571 218142 None 22 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](N)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/jm00090a003
CHEMBL2369459 212076 None 0 Rat Binding pIC50 = 8.6 8.6 - 1
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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/jm00090a003
44403860 141150 None 0 Human Binding pIC50 = 8.6 8.6 - 1
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 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 = 8.6 8.6 - 1
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 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
86298538 112013 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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 pIC50 = 8.6 8.6 - 0
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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
21102037 73818 None 0 Human Binding pIC50 = 8.6 8.6 - 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 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018511 73818 None 0 Human Binding pIC50 = 8.6 8.6 - 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 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
70694804 76534 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 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 Binding pIC50 = 7.7 7.7 - 0
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 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
21102224 76539 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 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 Binding pIC50 = 7.7 7.7 - 0
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 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
CHEMBL2369464 212079 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](N)CCCN=C(N)N)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/jm00090a003
44403855 72498 None 0 Human Binding pIC50 = 6.7 6.7 - 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 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 72498 None 0 Human Binding pIC50 = 6.7 6.7 - 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 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL429765 216007 None 0 Human Binding pIC50 = 6.7 6.7 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL268539 213216 None 0 Human Binding pIC50 = 6.7 6.7 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=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(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL2369465 212080 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
70684299 76538 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1cccnc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059904 76538 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1cccnc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2369457 212074 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
CHEMBL20034 211566 None 0 Human Binding pIC50 = 6.7 6.7 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70681269 73809 None 0 Human Binding pIC50 = 6.7 6.7 - 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 622 7 2 5 5.5 O=C(C[C@H](Nc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018502 73809 None 0 Human Binding pIC50 = 6.7 6.7 - 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 622 7 2 5 5.5 O=C(C[C@H](Nc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44403856 70506 None 0 Human Binding pIC50 = 6.7 6.7 - 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 828 13 4 9 3.7 COc1ccccc1N1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
CHEMBL194631 70506 None 0 Human Binding pIC50 = 6.7 6.7 - 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 828 13 4 9 3.7 COc1ccccc1N1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
24756611 76530 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 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 Binding pIC50 = 7.6 7.6 - 0
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 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
11249157 74406 None 0 Human Binding pIC50 = 7.6 7.6 - 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024591 74406 None 0 Human Binding pIC50 = 7.6 7.6 - 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL404977 214997 None 0 Human Binding pIC50 = 4.6 4.6 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL439085 216281 None 0 Human Binding pIC50 = 4.6 4.6 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
172461864 196758 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human CGRP1Inhibition of human CGRP1
ChEMBL 300 4 1 5 3.8 COc1cc(-c2cc3ccc(O)cc3o2)cc(OC)c1OC 10.1016/j.ejmech.2022.114962
CHEMBL5431521 196758 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human CGRP1Inhibition of human CGRP1
ChEMBL 300 4 1 5 3.8 COc1cc(-c2cc3ccc(O)cc3o2)cc(OC)c1OC 10.1016/j.ejmech.2022.114962
CHEMBL2369465 212080 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
86298539 112012 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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 pIC50 = 7.6 7.6 - 0
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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
44403857 70507 None 0 Human Binding pIC50 = 6.6 6.6 - 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 827 13 4 8 4.8 COc1ccccc1C1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
CHEMBL194632 70507 None 0 Human Binding pIC50 = 6.6 6.6 - 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 827 13 4 8 4.8 COc1ccccc1C1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
70693851 73802 None 0 Human Binding pIC50 = 6.6 6.6 - 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018495 73802 None 0 Human Binding pIC50 = 6.6 6.6 - 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL407774 215143 None 0 Human Binding pIC50 = 5.6 5.6 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
163049270 196484 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human CGRP1Inhibition of human CGRP1
ChEMBL 258 1 4 5 2.9 Oc1ccc2cc(-c3cc(O)c(O)c(O)c3)oc2c1 10.1016/j.ejmech.2022.114962
CHEMBL5424856 196484 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human CGRP1Inhibition of human CGRP1
ChEMBL 258 1 4 5 2.9 Oc1ccc2cc(-c3cc(O)c(O)c(O)c3)oc2c1 10.1016/j.ejmech.2022.114962
CHEMBL407854 215148 None 0 Human Binding pIC50 = 6.6 6.6 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864407 73794 None 0 Human Binding pIC50 = 6.6 6.6 - 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 616 7 2 6 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)Oc1ccccc1 10.1016/j.bmcl.2012.02.066
CHEMBL2018487 73794 None 0 Human Binding pIC50 = 6.6 6.6 - 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 616 7 2 6 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)Oc1ccccc1 10.1016/j.bmcl.2012.02.066
CHEMBL264010 213061 None 0 Human Binding pIC50 = 7.5 7.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70694803 76531 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 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 Binding pIC50 = 7.5 7.5 - 0
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 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
CHEMBL2369454 212073 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](C)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
25034109 178599 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL466555 178599 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.118
70683458 74137 None 0 Human Binding pIC50 = 8.5 8.5 - 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 535 5 2 6 5.1 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C#N)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022597 74137 None 0 Human Binding pIC50 = 8.5 8.5 - 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 535 5 2 6 5.1 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C#N)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11295168 74407 None 0 Human Binding pIC50 = 8.5 8.5 - 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024592 74407 None 0 Human Binding pIC50 = 8.5 8.5 - 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
10438558 73816 None 0 Human Binding pIC50 = 8.5 8.5 - 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018509 73816 None 0 Human Binding pIC50 = 8.5 8.5 - 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
21102038 73820 None 0 Human Binding pIC50 = 8.4 8.4 - 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018513 73820 None 0 Human Binding pIC50 = 8.4 8.4 - 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11341430 74416 None 0 Human Binding pIC50 = 8.4 8.4 - 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
CHEMBL2024601 74416 None 0 Human Binding pIC50 = 8.4 8.4 - 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
11238250 74135 None 0 Human Binding pIC50 = 7.5 7.5 - 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022595 74135 None 0 Human Binding pIC50 = 7.5 7.5 - 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL384581 214791 None 0 Human Binding pIC50 = 6.5 6.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL407740 215141 None 0 Human Binding pIC50 = 5.5 5.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL440990 216335 None 0 Human Binding pIC50 = 5.5 5.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70685453 73801 None 0 Human Binding pIC50 = 7.5 7.5 - 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018494 73801 None 0 Human Binding pIC50 = 7.5 7.5 - 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL405767 215038 None 0 Human Binding pIC50 = 4.5 4.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2369465 212080 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)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/jm00090a003
70686453 76535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 628 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.05.118
CHEMBL2059901 76535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 628 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.05.118
44323139 208772 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 452 5 1 4 6.2 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc3ccccc23)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL87174 208772 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 452 5 1 4 6.2 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc3ccccc23)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL407401 215120 None 0 Human Binding pIC50 = 5.5 5.5 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
11443894 74325 None 0 Human Binding pIC50 = 7.5 7.5 - 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 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024171 74325 None 0 Human Binding pIC50 = 7.5 7.5 - 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 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864296 73796 None 0 Human Binding pIC50 = 7.4 7.4 - 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 683 7 3 5 5.4 O=C(Nc1ccc(Cl)cc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018489 73796 None 0 Human Binding pIC50 = 7.4 7.4 - 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 683 7 3 5 5.4 O=C(Nc1ccc(Cl)cc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL405511 215023 None 0 Human Binding pIC50 = 6.4 6.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323338 208995 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.4 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2Cl)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88582 208995 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.4 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2Cl)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
70681261 73720 None 0 Human Binding pIC50 = 6.4 6.4 - 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 8 3 5 4.5 O=C(C[C@H](NCc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018355 73720 None 0 Human Binding pIC50 = 6.4 6.4 - 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 8 3 5 4.5 O=C(C[C@H](NCc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
70688557 76528 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 614 6 3 6 4.7 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(C2CCNCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2059881 76528 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 614 6 3 6 4.7 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(C2CCNCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2369742 212125 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL None None None CC(C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)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(C)C)C(C)C)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 10.1016/0960-894X(95)00078-8
70687709 74136 None 0 Human Binding pIC50 = 8.4 8.4 - 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 568 6 2 7 5.0 COC(=O)c1ccnc(C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c1 10.1016/j.bmcl.2012.02.065
CHEMBL2022596 74136 None 0 Human Binding pIC50 = 8.4 8.4 - 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 568 6 2 7 5.0 COC(=O)c1ccnc(C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c1 10.1016/j.bmcl.2012.02.065
11156698 74327 None 0 Human Binding pIC50 = 8.4 8.4 - 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024173 74327 None 0 Human Binding pIC50 = 8.4 8.4 - 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
44403859 134188 None 0 Human Binding pIC50 = 8.3 8.3 - 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 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL371646 134188 None 0 Human Binding pIC50 = 8.3 8.3 - 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 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL404978 214998 None 0 Human Binding pIC50 = 5.4 5.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44404069 172877 None 0 Human Binding pIC50 = 4.4 4.4 - 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 713 17 5 5 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL451246 172877 None 0 Human Binding pIC50 = 4.4 4.4 - 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 713 17 5 5 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
44323332 112453 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 447 6 1 6 5.0 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc([N+](=O)[O-])c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL329678 112453 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 447 6 1 6 5.0 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc([N+](=O)[O-])c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL269328 213244 None 0 Human Binding pIC50 = 5.4 5.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864477 73723 None 0 Human Binding pIC50 = 6.4 6.4 - 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 636 7 2 5 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2012.02.066
CHEMBL2018358 73723 None 0 Human Binding pIC50 = 6.4 6.4 - 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 636 7 2 5 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2012.02.066
44403858 72378 None 0 Human Binding pIC50 = 7.4 7.4 - 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 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198502 72378 None 0 Human Binding pIC50 = 7.4 7.4 - 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 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
11693761 114529 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 854 12 4 10 4.1 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL3334623 114529 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 854 12 4 10 4.1 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
58864506 73797 None 0 Human Binding pIC50 = 7.4 7.4 - 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 633 7 3 5 4.2 O=C(Nc1ccccc1F)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018490 73797 None 0 Human Binding pIC50 = 7.4 7.4 - 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 633 7 3 5 4.2 O=C(Nc1ccccc1F)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL262749 213006 None 0 Human Binding pIC50 = 5.4 5.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=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](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL406587 215074 None 0 Human Binding pIC50 = 5.4 5.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864520 73722 None 0 Human Binding pIC50 = 5.4 5.4 - 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 594 7 3 6 3.2 O=C(C[C@H](NC1CCC(O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018357 73722 None 0 Human Binding pIC50 = 5.4 5.4 - 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 594 7 3 6 3.2 O=C(C[C@H](NC1CCC(O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL262961 213013 None 0 Human Binding pIC50 = 4.4 4.4 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
24756770 73823 None 0 Human Binding pIC50 = 6.3 6.3 - 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 573 5 2 7 3.6 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC4(CC3)OCCO4)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018516 73823 None 0 Human Binding pIC50 = 6.3 6.3 - 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 573 5 2 7 3.6 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC4(CC3)OCCO4)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL274851 213276 None 0 Human Binding pIC50 = 6.3 6.3 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL411078 215321 None 0 Human Binding pIC50 = 5.3 5.3 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL217867 211842 None 0 Human Binding pIC50 = 6.3 6.3 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O 10.1021/jm970533r
62705051 76540 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 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 Binding pIC50 = 8.3 8.3 - 0
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 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
24756767 73817 None 0 Human Binding pIC50 = 8.2 8.2 - 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018510 73817 None 0 Human Binding pIC50 = 8.2 8.2 - 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL216101 211777 None 0 Human Binding pIC50 = 5.3 5.3 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403914 166315 None 0 Human Binding pIC50 = 4.3 4.3 - 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 685 15 5 5 5.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)Nc1ccccc1 10.1021/jm0490641
CHEMBL426646 166315 None 0 Human Binding pIC50 = 4.3 4.3 - 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 685 15 5 5 5.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)Nc1ccccc1 10.1021/jm0490641
CHEMBL410450 215281 None 0 Human Binding pIC50 = 4.3 4.3 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323095 107017 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(C(F)(F)F)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL314992 107017 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(C(F)(F)F)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
10433192 163520 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Compound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligandCompound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligand
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL419684 163520 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Compound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligandCompound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligand
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
44403860 141150 None 0 Rat Binding pIC50 = 7.3 7.3 - 1
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen 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 Rat Binding pIC50 = 7.3 7.3 - 1
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen 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
58864463 73724 None 0 Human Binding pIC50 = 6.2 6.2 - 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 596 6 2 6 3.8 CC(C)(C)OC(=O)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018359 73724 None 0 Human Binding pIC50 = 6.2 6.2 - 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 596 6 2 6 3.8 CC(C)(C)OC(=O)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
10433192 163520 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL419684 163520 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
44403861 72047 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen 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 Rat Binding pIC50 = 8.2 8.2 - 0
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen 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
70687746 74221 None 0 Human Binding pIC50 = 8.2 8.2 - 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)c2ccccn2)cc2c(CN3CCCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023185 74221 None 0 Human Binding pIC50 = 8.2 8.2 - 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)c2ccccn2)cc2c(CN3CCCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
70695974 73827 None 0 Human Binding pIC50 = 8.2 8.2 - 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 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
CHEMBL2018520 73827 None 0 Human Binding pIC50 = 8.2 8.2 - 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 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
CHEMBL2369458 212075 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
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](C)NC(=O)[C@@H](N)C(C)C)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/jm00090a003
70685594 74223 None 0 Human Binding pIC50 = 8.2 8.2 - 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 593 7 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023187 74223 None 0 Human Binding pIC50 = 8.2 8.2 - 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 593 7 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369458 212075 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](C)NC(=O)[C@@H](N)C(C)C)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/jm00090a003
CHEMBL265906 213128 None 0 Human Binding pIC50 = 6.2 6.2 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL386824 214856 None 0 Human Binding pIC50 = 5.2 5.2 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL415812 215662 None 0 Human Binding pIC50 = 5.2 5.2 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
11753024 74403 None 0 Human Binding pIC50 = 8.1 8.1 - 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024588 74403 None 0 Human Binding pIC50 = 8.1 8.1 - 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864272 73719 None 0 Human Binding pIC50 = 6.2 6.2 - 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 587 8 2 6 3.4 O=C(C[C@H](NCc1ccccn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018354 73719 None 0 Human Binding pIC50 = 6.2 6.2 - 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 587 8 2 6 3.4 O=C(C[C@H](NCc1ccccn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL428096 215872 None 0 Human Binding pIC50 = 5.2 5.2 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL266666 213151 None 0 Human Binding pIC50 = 4.2 4.2 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403855 72498 None 0 Rat Binding pIC50 = 4.2 4.2 - 1
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 72498 None 0 Rat Binding pIC50 = 4.2 4.2 - 1
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
58864421 73804 None 0 Human Binding pIC50 = 7.1 7.1 - 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 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018497 73804 None 0 Human Binding pIC50 = 7.1 7.1 - 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 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
44323341 208918 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 446 5 1 6 4.8 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88111 208918 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 446 5 1 6 4.8 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL2369458 212075 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](C)NC(=O)[C@@H](N)C(C)C)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/jm00090a003
11432183 74324 None 0 Human Binding pIC50 = 8.1 8.1 - 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024170 74324 None 0 Human Binding pIC50 = 8.1 8.1 - 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864325 73803 None 0 Human Binding pIC50 = 7.1 7.1 - 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 648 8 3 10 3.0 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc(N)c1[N+](=O)[O-] 10.1016/j.bmcl.2012.02.066
CHEMBL2018496 73803 None 0 Human Binding pIC50 = 7.1 7.1 - 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 648 8 3 10 3.0 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc(N)c1[N+](=O)[O-] 10.1016/j.bmcl.2012.02.066
CHEMBL265399 213104 None 0 Human Binding pIC50 = 5.1 5.1 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL410354 215274 None 0 Human Binding pIC50 = 4.1 4.1 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
70686454 76536 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 632 6 2 6 4.9 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
CHEMBL2059902 76536 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 632 6 2 6 4.9 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
CHEMBL275984 213283 None 0 Human Binding pIC50 = 5.1 5.1 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70692761 76533 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 628 5 2 6 4.7 CN1c2ccccc2C(=O)NC12CCN(C(=O)N[C@H](Cc1csc3ccccc13)C(=O)N1CCC(N3CCCCC3)CC1)CC2 10.1016/j.bmcl.2012.05.118
CHEMBL2059899 76533 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 628 5 2 6 4.7 CN1c2ccccc2C(=O)NC12CCN(C(=O)N[C@H](Cc1csc3ccccc13)C(=O)N1CCC(N3CCCCC3)CC1)CC2 10.1016/j.bmcl.2012.05.118
10483468 73822 None 0 Human Binding pIC50 = 7.1 7.1 - 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018515 73822 None 0 Human Binding pIC50 = 7.1 7.1 - 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
70695973 73807 None 0 Human Binding pIC50 = 6.1 6.1 - 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 623 7 2 6 4.9 O=C(C[C@H](Nc1cccc2ncccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018500 73807 None 0 Human Binding pIC50 = 6.1 6.1 - 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 623 7 2 6 4.9 O=C(C[C@H](Nc1cccc2ncccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2369452 212072 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
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](N)Cc1c[nH]cn1)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/jm00090a003
CHEMBL2369452 212072 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
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](N)Cc1c[nH]cn1)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/jm00090a003
70694802 76527 None 0 Human Binding pIC50 = 8.1 8.1 - 1
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 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2059880 76527 None 0 Human Binding pIC50 = 8.1 8.1 - 1
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 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL407697 215139 None 0 Human Binding pIC50 = 5.1 5.1 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL2371144 212475 None 0 Human Binding pIC50 = 6.0 6.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL269517 213253 None 0 Human Binding pIC50 = 4.0 4.0 - 0
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323110 107205 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 402 5 1 4 5.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccccc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL316211 107205 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 402 5 1 4 5.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccccc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864368 73795 None 0 Human Binding pIC50 = 7.0 7.0 - 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 683 7 3 5 5.4 O=C(Nc1cccc(Cl)c1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018488 73795 None 0 Human Binding pIC50 = 7.0 7.0 - 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 683 7 3 5 5.4 O=C(Nc1cccc(Cl)c1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
58864250 73799 None 0 Human Binding pIC50 = 7.0 7.0 - 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018492 73799 None 0 Human Binding pIC50 = 7.0 7.0 - 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44323180 209084 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc(C(F)(F)F)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL89148 209084 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc(C(F)(F)F)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
56675112 63357 None 0 Human Binding pIC50 = 6 6.0 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
91930235 63357 None 0 Human Binding pIC50 = 6 6.0 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL1794015 63357 None 0 Human Binding pIC50 = 6 6.0 - 0
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=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(=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(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
6918509 77070 None 33 Human Binding pKd = 10.4 10.4 131 2
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
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 pKd = 10.4 10.4 131 2
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
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
6918509 77070 None 33 Human Binding pKd = 10.1 10.1 131 2
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteries
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 pKd = 10.1 10.1 131 2
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteries
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
11319053 89187 None 36 Human Binding pKd = 8.7 8.7 - 1
Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compoundReversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 89187 None 36 Human Binding pKd = 8.7 8.7 - 1
Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compoundReversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 89187 None 36 Human Binding pKd = 8.4 8.4 - 1
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 89187 None 36 Human Binding pKd = 8.4 8.4 - 1
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
6918509 77070 None 33 Human Binding pKi = 11 11.0 131 2
Antagonist activity at human CGRP receptorAntagonist activity at 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 10.1016/j.bmcl.2013.04.012
CHEMBL207197 77070 None 33 Human Binding pKi = 11 11.0 131 2
Antagonist activity at human CGRP receptorAntagonist activity at 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 10.1016/j.bmcl.2013.04.012
6918509 77070 None 33 Human Binding pKi = 11 11.0 131 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 10.1021/ml300021s
CHEMBL207197 77070 None 33 Human Binding pKi = 11 11.0 131 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 10.1021/ml300021s
6918509 77070 None 33 Human Binding pKi = 11 11.0 131 2
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
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.2013.12.089
CHEMBL207197 77070 None 33 Human Binding pKi = 11 11.0 131 2
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
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.2013.12.089
11467753 174300 None 0 Human Binding pKi = 11 11.0 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
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 10.1021/jm800546t
CHEMBL454791 174300 None 0 Human Binding pKi = 11 11.0 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
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 10.1021/jm800546t
10394458 87707 None 0 Human Binding pKi = 11.0 11.0 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 646 6 3 5 4.8 O=C(NC(Cc1cc(Cl)c2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336422 87707 None 0 Human Binding pKi = 11.0 11.0 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 646 6 3 5 4.8 O=C(NC(Cc1cc(Cl)c2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
10077700 87709 None 0 Human Binding pKi = 10.9 10.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336424 87709 None 0 Human Binding pKi = 10.9 10.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(CC(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 Binding pKi = 10.9 10.9 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
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 Binding pKi = 10.9 10.9 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
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
44593666 172833 None 8 Human Binding pKi = 10.9 10.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
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.2013.04.012
CHEMBL450668 172833 None 8 Human Binding pKi = 10.9 10.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
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.2013.04.012
44593666 172833 None 8 Human Binding pKi = 10.9 10.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
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.2013.01.011
CHEMBL450668 172833 None 8 Human Binding pKi = 10.9 10.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
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.2013.01.011
44593666 172833 None 8 Human Binding pKi = 10.9 10.9 - 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 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.2012.02.065
CHEMBL450668 172833 None 8 Human Binding pKi = 10.9 10.9 - 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 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.2012.02.065
6918509 77070 None 33 Human Binding pKi = 10.9 10.9 131 2
Binding affinity to human CGRP receptorBinding affinity to 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 pKi = 10.9 10.9 131 2
Binding affinity to human CGRP receptorBinding affinity to 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
6918509 77070 None 33 Human Binding pKi = 10.9 10.9 131 2
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma counting
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.2012.04.105
CHEMBL207197 77070 None 33 Human Binding pKi = 10.9 10.9 131 2
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma counting
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.2012.04.105
164614302 185448 None 0 Human Binding pKi = 10.9 10.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 646 5 2 5 4.5 CCn1c(=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
CHEMBL4859941 185448 None 0 Human Binding pKi = 10.9 10.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 646 5 2 5 4.5 CCn1c(=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
71569533 87697 None 0 Human Binding pKi = 10.8 10.8 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 627 6 3 6 3.9 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2nn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336411 87697 None 0 Human Binding pKi = 10.8 10.8 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 627 6 3 6 3.9 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2nn[nH]c12 10.1016/j.bmcl.2013.01.011
164618286 184651 None 0 Human Binding pKi = 10.8 10.8 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
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 Binding pKi = 10.8 10.8 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
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
73356952 92531 None 0 Human Binding pKi = 10.8 10.8 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 586 4 2 6 3.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431249 92531 None 0 Human Binding pKi = 10.8 10.8 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 586 4 2 6 3.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
44469664 92528 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 567 2 1 5 4.1 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431246 92528 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 567 2 1 5 4.1 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
164617750 184676 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 618 4 3 4 4.0 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)[nH]c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4848486 184676 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 618 4 3 4 4.0 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)[nH]c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
59555187 105236 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114495 105236 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
164614208 185310 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4857649 185310 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
25019940 67971 None 29 Human Binding pKi = 10.7 10.7 478 2
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2013.04.012
CHEMBL1910936 67971 None 29 Human Binding pKi = 10.7 10.7 478 2
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2013.04.012
25019940 67971 None 29 Human Binding pKi = 10.7 10.7 478 2
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
CHEMBL1910936 67971 None 29 Human Binding pKi = 10.7 10.7 478 2
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
44469946 92535 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 569 4 1 5 4.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431253 92535 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 569 4 1 5 4.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
57977594 92538 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 2 5 3.6 CN1C[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
CHEMBL2431256 92538 None 0 Human Binding pKi = 10.7 10.7 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 2 5 3.6 CN1C[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
11377534 87702 None 0 Human Binding pKi = 10.6 10.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc(Br)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336416 87702 None 0 Human Binding pKi = 10.6 10.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc(Br)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
53472683 91090 None 15 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
53472683.0 91090 None 15 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
CHEMBL2397415 91090 None 15 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
DB15688 91090 None 15 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
46885183 8340 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092882 8340 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
164628650 186465 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 673 5 2 7 3.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4875327 186465 None 0 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 673 5 2 7 3.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
51049968 82592 None 40 Human Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
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 Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
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 Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
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 Binding pKi = 10.6 10.6 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
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
CHEMBL2369459 212076 None 0 Human Binding pKi = 10.6 10.6 - 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
76321477 105261 None 0 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114676 105261 None 0 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
71569375 87704 None 0 Human Binding pKi = 10.5 10.5 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 660 6 3 5 5.1 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c(Cl)c2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336418 87704 None 0 Human Binding pKi = 10.5 10.5 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 660 6 3 5 5.1 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c(Cl)c2cn[nH]c12 10.1016/j.bmcl.2013.01.011
25019993 92536 None 1 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 3 5 3.2 CC1(C)NC[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
CHEMBL2431254 92536 None 1 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 3 5 3.2 CC1(C)NC[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
45485692 201456 None 0 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
CHEMBL585568 201456 None 0 Human Binding pKi = 10.5 10.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
54581910 61536 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
CHEMBL1770729 61536 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
52940673 18170 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269644 18170 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
11204595 87703 None 0 Human Binding pKi = 10.4 10.4 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc(Cl)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336417 87703 None 0 Human Binding pKi = 10.4 10.4 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc(Cl)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
54586725 61535 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770728 61535 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
25181509 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL512773 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
54585731 61522 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770715 61522 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
57977652 75112 None 0 Human Binding pKi = 10.4 10.4 85 2
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
CHEMBL2035981 75112 None 0 Human Binding pKi = 10.4 10.4 85 2
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
25181509 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL512773 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
25181509 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL512773 189474 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
44631920 125906 None 0 Human Binding pKi = 10.4 10.4 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 534 7 1 4 5.3 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CF nan
CHEMBL3648345 125906 None 0 Human Binding pKi = 10.4 10.4 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 534 7 1 4 5.3 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CF nan
164627356 186391 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 633 4 2 6 3.5 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ncccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4874157 186391 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 633 4 2 6 3.5 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ncccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
44470090 92533 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 5 1 5 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431251 92533 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 5 1 5 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
50939479 92530 None 1 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431248 92530 None 1 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
17751102 180045 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4746351 180045 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
58864297 87705 None 0 Human Binding pKi = 10.3 10.3 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.0 CCc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2c(C)n[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336419 87705 None 0 Human Binding pKi = 10.3 10.3 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.0 CCc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2c(C)n[nH]c12 10.1016/j.bmcl.2013.01.011
54580850 61531 None 1 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770724 61531 None 1 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54583843 61533 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770726 61533 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
58379673 104373 None 0 Human Binding pKi = 10.3 10.3 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 568 6 1 4 5.7 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C1(C(F)(F)F)CC1 nan
CHEMBL3099925 104373 None 0 Human Binding pKi = 10.3 10.3 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 568 6 1 4 5.7 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C1(C(F)(F)F)CC1 nan
56944164 75114 None 5 Human Binding pKi = 10.3 10.3 194 4
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Human Binding pKi = 10.3 10.3 194 4
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
11388586 87701 None 0 Human Binding pKi = 10.3 10.3 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 755 6 3 6 4.3 O=C(N[C@H](Cc1cc(I)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336415 87701 None 0 Human Binding pKi = 10.3 10.3 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 755 6 3 6 4.3 O=C(N[C@H](Cc1cc(I)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
50939608 92529 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 559 4 2 5 3.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
CHEMBL2431247 92529 None 0 Human Binding pKi = 10.3 10.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 559 4 2 5 3.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
44631936 125246 None 0 Human Binding pKi = 10.2 10.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 557 3 1 5 5.0 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCc3ccccc32)C1=O nan
CHEMBL3645137 125246 None 0 Human Binding pKi = 10.2 10.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 557 3 1 5 5.0 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCc3ccccc32)C1=O nan
164619429 186176 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 599 4 2 6 4.0 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4871223 186176 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 599 4 2 6 4.0 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
164627588 186406 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 4 5.2 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4874451 186406 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 4 5.2 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
46179077 125252 None 0 Human Binding pKi = 10.2 10.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 593 3 1 5 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(=O)C12CCCC2 nan
CHEMBL3645143 125252 None 0 Human Binding pKi = 10.2 10.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 593 3 1 5 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(=O)C12CCCC2 nan
58379669 125905 None 0 Human Binding pKi = 10.2 10.2 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 550 7 1 4 5.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CCl nan
CHEMBL3648344 125905 None 0 Human Binding pKi = 10.2 10.2 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 550 7 1 4 5.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CCl nan
51357856 82590 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 560 4 1 7 5.8 [N-]=[N+]=N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
CHEMBL2178420 82590 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 560 4 1 7 5.8 [N-]=[N+]=N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
164620407 186333 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 653 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4873378 186333 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 653 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
46174937 76609 None 8 Human Binding pKi = 10.2 10.2 - 1
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 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
CHEMBL2063115 76609 None 8 Human Binding pKi = 10.2 10.2 - 1
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 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
11706981 61527 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770720 61527 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
59555031 105235 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114494 105235 None 0 Human Binding pKi = 10.2 10.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
57404496 74227 None 0 Human Binding pKi = 10.2 10.2 - 1
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 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 10.1021/ml300021s
CHEMBL2023191 74227 None 0 Human Binding pKi = 10.2 10.2 - 1
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 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 10.1021/ml300021s
46885299 8210 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092208 8210 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
51357585 82594 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178424 82594 None 0 Human Binding pKi = 10.1 10.1 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
23658217 180043 None 0 Human Binding pKi = 10.1 10.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 575 4 2 6 3.6 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4746329 180043 None 0 Human Binding pKi = 10.1 10.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 575 4 2 6 3.6 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2020.127624
44468576 92534 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 568 4 1 4 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431252 92534 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 568 4 1 4 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
17751102 180045 None 0 Human Binding pKi = 10 10.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4746351 180045 None 0 Human Binding pKi = 10 10.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
59554856 105237 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114496 105237 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
52940932 18260 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 504 4 1 4 5.8 C[C@H](c1ccccc1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
CHEMBL1270291 18260 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 504 4 1 4 5.8 C[C@H](c1ccccc1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
44469523 92373 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 2 1 4 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2429882 92373 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 2 1 4 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
69747490 92537 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 3 5 3.4 CC1(C)NC[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
CHEMBL2431255 92537 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 3 5 3.4 CC1(C)NC[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
52941862 18171 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1ccc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269645 18171 None 0 Human Binding pKi = 10.0 10.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1ccc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
164625304 186311 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 619 4 2 5 4.3 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)oc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4873084 186311 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 619 4 2 5 4.3 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)oc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
52942173 18276 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 540 4 1 4 6.0 C[C@H](c1cc(F)cc(F)c1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
CHEMBL1270391 18276 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 540 4 1 4 6.0 C[C@H](c1cc(F)cc(F)c1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
45267476 198740 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL562069 198740 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46885244 7795 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089433 7795 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
164612132 184764 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 6 3.7 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4849710 184764 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 6 3.7 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
45485605 200110 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
CHEMBL570933 200110 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
58379682 104372 None 0 Human Binding pKi = 9.9 9.9 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 512 5 1 4 5.6 Cc1ccc([C@@H](C)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C(C)(C)C)cc1F nan
CHEMBL3099923 104372 None 0 Human Binding pKi = 9.9 9.9 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 512 5 1 4 5.6 Cc1ccc([C@@H](C)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C(C)(C)C)cc1F nan
46178994 125248 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 565 3 2 5 4.9 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CNC12CCCC2 nan
CHEMBL3645139 125248 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 565 3 2 5 4.9 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CNC12CCCC2 nan
11354531 87698 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Br)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336412 87698 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Br)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
54580803 61504 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770557 61504 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54581909 61530 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770723 61530 None 0 Human Binding pKi = 9.9 9.9 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
52944286 18172 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 1 5 5.1 CC(C)(C)C(=O)N(Cc1cnc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269646 18172 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 1 5 5.1 CC(C)(C)C(=O)N(Cc1cnc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
54583844 61534 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770727 61534 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
164609291 184566 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]cnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4846749 184566 None 0 Human Binding pKi = 9.8 9.8 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]cnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
54583842 61529 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770722 61529 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
23656921 90256 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238276 90256 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44570616 190323 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL517467 190323 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
46182711 127050 None 0 Human Binding pKi = 9.7 9.7 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655571 127050 None 0 Human Binding pKi = 9.7 9.7 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11158071 87706 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.3 CC(C)c1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336420 87706 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.3 CC(C)c1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
11977527 179676 None 0 Human Binding pKi = 9.6 9.6 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 588 4 2 4 4.7 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4741882 179676 None 0 Human Binding pKi = 9.6 9.6 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 588 4 2 4 4.7 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
24863333 174284 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL454751 174284 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
44593545 178559 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
46905052 10421 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
CHEMBL1162991 10421 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
45485687 200039 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 4 3.6 C[C@H](c1cc(F)cc(F)c1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL570474 200039 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 4 3.6 C[C@H](c1cc(F)cc(F)c1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
24863333 174284 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
CHEMBL454751 174284 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
24863332 76505 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 629 6 3 6 3.7 O=C(N[C@H](Cc1ccc2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059853 76505 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 629 6 3 6 3.7 O=C(N[C@H](Cc1ccc2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
46179076 125251 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 531 4 1 5 4.7 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(C)(c2ccccc2)C1=O nan
CHEMBL3645142 125251 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 531 4 1 5 4.7 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(C)(c2ccccc2)C1=O nan
11445240 87699 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Cl)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336413 87699 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Cl)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
45267481 199118 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
CHEMBL564487 199118 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
54587762 61532 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770725 61532 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
23654987 114530 None 8 Human Binding pKi = 9.5 9.5 - 1
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 633 6 2 7 3.9 Cc1cc(C[C@@H](OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCOCC3)CC2)cc(C)c1O 10.1021/jm500364u
CHEMBL3334624 114530 None 8 Human Binding pKi = 9.5 9.5 - 1
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 633 6 2 7 3.9 Cc1cc(C[C@@H](OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCOCC3)CC2)cc(C)c1O 10.1021/jm500364u
11364735 89743 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237662 89743 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
46178835 18290 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 538 3 1 4 5.8 CC1(C)CC[C@@H](c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2010.08.105
CHEMBL1270484 18290 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 538 3 1 4 5.8 CC1(C)CC[C@@H](c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2010.08.105
46885135 8038 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090848 8038 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11979131 180766 None 0 Human Binding pKi = 9.5 9.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 594 4 2 4 5.3 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755081 180766 None 0 Human Binding pKi = 9.5 9.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 594 4 2 4 5.3 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46178992 125247 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 523 3 1 5 4.9 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCCCC2)C1=O nan
CHEMBL3645138 125247 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 523 3 1 5 4.9 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCCCC2)C1=O nan
23582940 199058 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
54580838 61521 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770714 61521 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54586710 61526 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770719 61526 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
164626848 186606 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 617 5 3 6 3.3 NC(=O)c1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4877386 186606 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 617 5 3 6 3.3 NC(=O)c1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
11979011 180811 None 0 Human Binding pKi = 9.4 9.4 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 576 4 2 4 5.2 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755588 180811 None 0 Human Binding pKi = 9.4 9.4 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 576 4 2 4 5.2 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46885185 7971 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1090515 7971 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
58379670 125907 None 0 Human Binding pKi = 9.4 9.4 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 495 5 1 3 4.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C nan
CHEMBL3648346 125907 None 0 Human Binding pKi = 9.4 9.4 - 1
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 495 5 1 3 4.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C nan
164612882 185010 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 603 4 2 5 4.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]nnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4853137 185010 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 603 4 2 5 4.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]nnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
54584803 61528 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770721 61528 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
46179163 125253 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
CHEMBL3645144 125253 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
44468711 92532 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 570 5 1 4 5.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431250 92532 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 570 5 1 4 5.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
23657089 147068 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 147068 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11192602 147073 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392636 147073 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
59554895 105231 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114490 105231 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44593545 178559 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 178559 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
25227362 173837 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL453643 173837 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
25227362 173837 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL453643 173837 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
46885243 8330 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092838 8330 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11977643 180752 None 0 Human Binding pKi = 9.3 9.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 585 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3ccccc3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4754995 180752 None 0 Human Binding pKi = 9.3 9.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 585 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3ccccc3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
24863323 76525 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 613 6 3 6 3.6 O=C(N[C@H](Cc1ccc2[nH]nnc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059878 76525 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 613 6 3 6 3.6 O=C(N[C@H](Cc1ccc2[nH]nnc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
70694802 76527 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059880 76527 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
45485640 199846 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 498 5 2 4 3.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL569340 199846 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 498 5 2 4 3.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
46885242 8329 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092837 8329 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
25034109 178599 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
CHEMBL466555 178599 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
54587752 61523 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770716 61523 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
44570579 190940 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL518422 190940 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
54581897 61525 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770718 61525 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11520007 61524 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770717 61524 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
70690615 76486 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 730 6 3 6 5.0 O=C(N[C@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059794 76486 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 730 6 3 6 5.0 O=C(N[C@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
24863334 76524 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 627 6 3 5 3.8 O=C1Cc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2N1 10.1016/j.bmcl.2012.05.074
CHEMBL2059877 76524 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 627 6 3 5 3.8 O=C1Cc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2N1 10.1016/j.bmcl.2012.05.074
51357855 82591 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178421 82591 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
11606400 61515 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770568 61515 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
52943413 18245 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 526 4 1 4 5.5 CC(C)(C)C(=O)N(Cc1cc(F)cc(F)c1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1270197 18245 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 526 4 1 4 5.5 CC(C)(C)C(=O)N(Cc1cc(F)cc(F)c1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
11432931 162006 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL415263 162006 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11979133 179560 None 0 Human Binding pKi = 9.1 9.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 573 4 2 4 5.4 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4740622 179560 None 0 Human Binding pKi = 9.1 9.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 573 4 2 4 5.4 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2013.04.012
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2013.04.012
46178995 125249 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 564 3 1 4 6.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCC12CCCC2 nan
CHEMBL3645140 125249 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 564 3 1 4 6.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCC12CCCC2 nan
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/ml400199p
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/ml400199p
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
11319053 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
CHEMBL236593 89187 None 36 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
45485677 201290 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL583679 201290 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
164626466 186399 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 601 4 2 3 5.4 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ccc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4874351 186399 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 601 4 2 3 5.4 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ccc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
44570614 177706 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464078 177706 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
46179164 125254 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2ccc3nc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
CHEMBL3645145 125254 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2ccc3nc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
11284233 89921 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237849 89921 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11387595 147070 None 1 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392635 147070 None 1 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555048 105227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114486 105227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11628603 181826 None 0 Human Binding pKi = 9 9.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 597 4 3 4 4.9 O=C(N[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4777037 181826 None 0 Human Binding pKi = 9 9.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 597 4 3 4 4.9 O=C(N[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
54582783 61503 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770556 61503 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59554993 105230 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114489 105230 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
59555066 105234 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114493 105234 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
76332330 105262 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114677 105262 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11541560 61513 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770566 61513 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11721278 61514 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 61514 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11512928 141758 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
CHEMBL385454 141758 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
11692628 200081 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL570746 200081 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
45271754 197301 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL549503 197301 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570580 177552 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 177552 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
45485646 200229 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 514 5 2 4 3.5 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571797 200229 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 514 5 2 4 3.5 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
23582940 199058 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 199058 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46179074 125250 None 0 Human Binding pKi = 8.9 8.9 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 547 3 1 5 5.4 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(c2ccccc2Cl)=NC12CCCC2 nan
CHEMBL3645141 125250 None 0 Human Binding pKi = 8.9 8.9 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 547 3 1 5 5.4 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(c2ccccc2Cl)=NC12CCCC2 nan
52947106 18227 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 490 4 1 4 5.2 CC(C)(C)C(=O)N(Cc1ccccc1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1270088 18227 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 490 4 1 4 5.2 CC(C)(C)C(=O)N(Cc1ccccc1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
46885245 7849 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 7849 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
11753021 89744 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237663 89744 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11752904 147439 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392937 147439 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45271740 199002 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 199002 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
46885134 8037 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 8037 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11979010 183556 None 0 Human Binding pKi = 8.8 8.8 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 577 3 3 4 4.7 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4798946 183556 None 0 Human Binding pKi = 8.8 8.8 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 577 3 3 4 4.7 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46885186 8035 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 8035 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
45485645 200199 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571580 200199 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45254467 127051 None 0 Human Binding pKi = 8.8 8.8 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 597 5 3 5 4.0 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655572 127051 None 0 Human Binding pKi = 8.8 8.8 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 597 5 3 5 4.0 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11180666 147182 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 147182 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
44570615 177707 None 13 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 177707 None 13 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44593445 191638 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL519421 191638 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
44593445 191638 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
CHEMBL519421 191638 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
11584808 200144 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
CHEMBL571203 200144 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
45485664 199794 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 496 5 2 4 3.4 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL568920 199794 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 496 5 2 4 3.4 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45485625 200235 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL571823 200235 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2010.08.105
45485625 200235 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571823 200235 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44563052 186141 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
CHEMBL487068 186141 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
25019940 67971 None 29 Rat Binding pKi = 8 8.0 -478 2
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/jm500364u
CHEMBL1910936 67971 None 29 Rat Binding pKi = 8 8.0 -478 2
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/jm500364u
59555258 105226 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114485 105226 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
25019940 67971 None 29 Rat Binding pKi = 8 8.0 -478 2
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL1910936 67971 None 29 Rat Binding pKi = 8 8.0 -478 2
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44420250 137015 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374251 137015 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11432505 200089 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570793 200089 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
44562938 179200 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471705 179200 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45487023 201275 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 526 4 2 3 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccc[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL583547 201275 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 526 4 2 3 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccc[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
44416442 80608 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 593 4 2 7 3.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214950 80608 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 593 4 2 7 3.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2006.07.044
44420286 84289 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221160 84289 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44417049 168922 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL437718 168922 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11848968 95258 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255967 95258 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11570753 169670 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3cccnc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL443577 169670 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3cccnc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44420290 84661 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL222198 84661 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44416513 141969 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 619 5 3 7 4.0 NC(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386714 141969 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 619 5 3 7 4.0 NC(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
71569532 87700 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 6 3 7 3.6 N#Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2oc(=O)[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336414 87700 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 6 3 7 3.6 N#Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2oc(=O)[nH]c12 10.1016/j.bmcl.2013.01.011
11168000 154272 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 154272 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11628731 80424 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214507 80424 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44416912 80888 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215274 80888 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11707040 81109 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215499 81109 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11519899 141574 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL384408 141574 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
23656751 91775 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 3 3 5 2.4 Cc1ccc(C2CC[C@@H](NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)C(=O)NC2)cc1 10.1021/jm070668p
CHEMBL240903 91775 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 3 3 5 2.4 Cc1ccc(C2CC[C@@H](NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)C(=O)NC2)cc1 10.1021/jm070668p
11549001 141966 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386701 141966 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
59554867 105266 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114681 105266 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
59555008 105212 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114471 105212 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
11978769 182480 None 0 Human Binding pKi = 7.9 7.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 563 4 3 4 4.2 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785088 182480 None 0 Human Binding pKi = 7.9 7.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 563 4 3 4 4.2 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
52945887 18226 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)[C@]12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1270087 18226 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)[C@]12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
44420256 84981 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223756 84981 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44563026 186749 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL488065 186749 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
59555056 105201 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114460 105201 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11713849 201345 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 564 3 2 3 4.6 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)Cc1ccccc1NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL584311 201345 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 564 3 2 3 4.6 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)Cc1ccccc1NC2=O 10.1016/j.bmcl.2009.09.066
70685988 75116 None 0 Rat Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 606 4 3 6 4.0 C[C@@]1(c2cc(F)c(Cl)c(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035985 75116 None 0 Rat Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 606 4 3 6 4.0 C[C@@]1(c2cc(F)c(Cl)c(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44570499 192505 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL520778 192505 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44562897 179172 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471530 179172 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563126 189041 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 189041 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44570461 179352 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2cccnc2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL472829 179352 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2cccnc2)NC1=O 10.1016/j.bmcl.2008.10.106
45254662 127048 None 0 Human Binding pKi = 6.9 6.9 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cccnc2)NC1=O nan
CHEMBL3655569 127048 None 0 Human Binding pKi = 6.9 6.9 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cccnc2)NC1=O nan
25119464 182650 None 0 Human Binding pKi = 7.9 7.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 529 4 3 4 3.7 CC(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4787479 182650 None 0 Human Binding pKi = 7.9 7.9 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 529 4 3 4 3.7 CC(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
59555055 105232 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114491 105232 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59554934 105233 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114492 105233 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
45485631 200169 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccccc3F)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571350 200169 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccccc3F)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44455457 95263 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 95263 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487059 200143 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 502 3 2 3 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CCNC2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL571185 200143 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 502 3 2 3 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CCNC2=O)CC1 10.1016/j.bmcl.2009.09.066
70690614 76485 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 2 6 3.8 COc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059793 76485 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 2 6 3.8 COc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
44416437 141881 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386204 141881 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
44420245 84038 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
CHEMBL220715 84038 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
44562939 179201 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 179201 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563025 192604 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL520905 192604 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
44455043 95779 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258329 95779 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11444589 79820 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL211931 79820 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
70690616 76494 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 611 6 2 6 4.3 Cn1cc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.074
CHEMBL2059802 76494 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 611 6 2 6 4.3 Cn1cc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.074
44570498 184146 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL482178 184146 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
45254661 127049 None 0 Human Binding pKi = 6.8 6.8 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccncc2)NC1=O nan
CHEMBL3655570 127049 None 0 Human Binding pKi = 6.8 6.8 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccncc2)NC1=O nan
44455041 170700 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL445069 170700 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
56944164 75114 None 5 Rat Binding pKi = 7.8 7.8 -194 4
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Rat Binding pKi = 7.8 7.8 -194 4
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
11849025 95538 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL257252 95538 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44420261 137370 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375224 137370 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46885132 8173 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 490 3 1 7 2.8 CN1C(=O)NC(=O)[C@]12Cc1cc3ccc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1091903 8173 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 490 3 1 7 2.8 CN1C(=O)NC(=O)[C@]12Cc1cc3ccc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11977970 181138 None 0 Human Binding pKi = 6.8 6.8 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 544 5 3 5 2.6 CN(C)CCN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4759318 181138 None 0 Human Binding pKi = 6.8 6.8 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 544 5 3 5 2.6 CN(C)CCN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11848963 155524 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL403765 155524 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
23656750 91764 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 478 4 3 6 2.1 COc1ccccc1C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240902 91764 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 478 4 3 6 2.1 COc1ccccc1C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11848753 158990 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 522 4 2 8 2.4 Cn1cc(-c2ccc(S(C)(=O)=O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL409535 158990 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 522 4 2 8 2.4 Cn1cc(-c2ccc(S(C)(=O)=O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59554936 105218 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114477 105218 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
70685987 75115 None 0 Rat Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 592 4 3 6 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)c(Cl)c(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035984 75115 None 0 Rat Binding pKi = 7.8 7.8 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 592 4 3 6 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)c(Cl)c(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44562982 186147 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487076 186147 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59554947 105228 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114487 105228 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
16745090 7769 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 491 3 1 8 2.2 CN1C(=O)NC(=O)C12Cc1cc3ncc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089207 7769 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 491 3 1 8 2.2 CN1C(=O)NC(=O)C12Cc1cc3ncc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
59554857 105199 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114458 105199 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11571094 141977 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386757 141977 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
56944164 75114 None 5 Mouse Binding pKi = 7.7 7.7 -218 4
Displacement of [125I]CGRP from mouse CGRP receptorDisplacement of [125I]CGRP from mouse CGRP receptor
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 75114 None 5 Mouse Binding pKi = 7.7 7.7 -218 4
Displacement of [125I]CGRP from mouse CGRP receptorDisplacement of [125I]CGRP from mouse CGRP receptor
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
70686451 76488 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 615 7 3 6 3.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059797 76488 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 615 7 3 6 3.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
11848798 95722 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 446 3 2 8 1.7 Cn1cc(-c2ncccn2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258069 95722 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 446 3 2 8 1.7 Cn1cc(-c2ncccn2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555157 105215 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114474 105215 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
24853164 105217 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114476 105217 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555074 105225 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114484 105225 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555331 105229 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114488 105229 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44563050 186753 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488082 186753 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
52949562 18206 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3ccc(CN(Cc4ccccc4)C(=O)C(C)(C)C)nc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1269977 18206 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3ccc(CN(Cc4ccccc4)C(=O)C(C)(C)C)nc3cc1C2 10.1016/j.bmcl.2010.08.105
54581838 61509 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770562 61509 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44563200 174594 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL455458 174594 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
45269221 199113 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 199113 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570578 178515 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 178515 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11375693 89920 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 89920 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
54583774 61510 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770563 61510 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
70688552 76483 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 574 6 3 6 3.5 O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059790 76483 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 574 6 3 6 3.5 O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
11225752 89745 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237664 89745 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
44563028 194674 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
CHEMBL530116 194674 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
54583775 61512 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 61512 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59555100 105222 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114481 105222 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
44420240 83508 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL220101 83508 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420235 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420240 83508 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220101 83508 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420235 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
11505361 141575 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccn3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384409 141575 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccn3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11678456 80251 None 0 Human Binding pKi = 4.7 4.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 556 5 3 7 3.2 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(CO)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213717 80251 None 0 Human Binding pKi = 4.7 4.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 556 5 3 7 3.2 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(CO)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44416516 81121 None 0 Human Binding pKi = 4.7 4.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2nc(O)n(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c12 10.1016/j.bmcl.2006.07.044
CHEMBL215549 81121 None 0 Human Binding pKi = 4.7 4.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2nc(O)n(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c12 10.1016/j.bmcl.2006.07.044
59555245 105210 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114469 105210 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59555102 105265 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114680 105265 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11650307 80549 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL214800 80549 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
11849024 155373 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402887 155373 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455188 161336 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 1.4 Cn1cc(C2C=NC=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL411896 161336 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 1.4 Cn1cc(C2C=NC=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44420235 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223156 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420235 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 84808 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563051 186781 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488255 186781 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
70692757 76484 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 3 6 3.9 O=C(N[C@H](CCc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059792 76484 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 3 6 3.9 O=C(N[C@H](CCc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
44455078 95641 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257732 95641 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
162666990 182514 None 0 Human Binding pKi = 7.7 7.7 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 564 4 3 5 3.6 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785645 182514 None 0 Human Binding pKi = 7.7 7.7 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 564 4 3 5 3.6 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
11351794 91014 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL239630 91014 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555230 105221 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114480 105221 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
11421827 157696 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 157696 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
44563123 188994 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL507339 188994 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11848645 97563 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270392 97563 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11365194 140822 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL381798 140822 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2008.10.106
11365194 140822 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL381798 140822 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
11848800 155362 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL402844 155362 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11421827 157696 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL408093 157696 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
45485600 200278 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 487 5 2 5 2.6 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(C#N)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL572225 200278 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 487 5 2 5 2.6 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(C#N)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44562984 186148 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL487077 186148 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
70692759 76490 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059799 76490 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
44570375 178474 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 468 4 3 7 1.5 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL465279 178474 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 468 4 3 7 1.5 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2008.10.106
45487037 200055 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 603 5 2 4 4.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2cc(-c3ccccc3)n[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570626 200055 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 603 5 2 4 4.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2cc(-c3ccccc3)n[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
70696845 76480 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 524 6 2 5 3.6 CC(C)C[C@@H](NC(=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059786 76480 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 524 6 2 5 3.6 CC(C)C[C@@H](NC(=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.05.074
44420255 137972 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL376292 137972 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
45485609 200900 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 3.7 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(C(F)(F)F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL577304 200900 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 3.7 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(C(F)(F)F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45254862 127042 None 0 Human Binding pKi = 7.6 7.6 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 534 5 2 8 3.3 O=C(Cn1c(=O)n(-c2nccs2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655563 127042 None 0 Human Binding pKi = 7.6 7.6 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 534 5 2 8 3.3 O=C(Cn1c(=O)n(-c2nccs2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
70682194 76492 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 634 7 2 5 5.4 O=C(N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059800 76492 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 634 7 2 5 5.4 O=C(N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
70690617 76504 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 612 6 3 5 4.2 O=C(N[C@@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059852 76504 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 612 6 3 5 4.2 O=C(N[C@@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
44563027 186750 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL488066 186750 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
135461116 141640 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384799 141640 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44562937 179199 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 179199 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44563089 186266 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 186266 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
59554942 105209 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114468 105209 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416514 155825 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405544 155825 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44570462 184031 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(C2CC2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL481382 184031 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(C2CC2)NC1=O 10.1016/j.bmcl.2008.10.106
45254859 127044 None 0 Human Binding pKi = 5.6 5.6 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(C2CC2)NC1=O nan
CHEMBL3655565 127044 None 0 Human Binding pKi = 5.6 5.6 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(C2CC2)NC1=O nan
71569374 87708 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
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
CHEMBL2336423 87708 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
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
11541725 141473 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL383872 141473 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44417050 141596 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384539 141596 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
11848647 155453 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL403373 155453 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11576078 178475 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 453 4 2 6 2.4 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCNC1=O)C2 10.1016/j.bmcl.2008.10.106
CHEMBL465280 178475 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 453 4 2 6 2.4 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCNC1=O)C2 10.1016/j.bmcl.2008.10.106
44570421 177855 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 6 2.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCCNC1=O)C2 10.1016/j.bmcl.2008.10.106
CHEMBL464264 177855 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 6 2.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCCNC1=O)C2 10.1016/j.bmcl.2008.10.106
24863246 76526 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 626 6 3 5 4.5 Cc1nc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2[nH]1 10.1016/j.bmcl.2012.05.074
CHEMBL2059879 76526 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 626 6 3 5 4.5 Cc1nc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2[nH]1 10.1016/j.bmcl.2012.05.074
10340395 85029 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL223805 85029 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
11238717 141967 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386706 141967 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
76310551 105263 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114678 105263 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416824 80314 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
CHEMBL213976 80314 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
44420231 137130 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374666 137130 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46182711 127050 None 0 Human Binding pKi = 7.5 7.5 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655571 127050 None 0 Human Binding pKi = 7.5 7.5 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11978083 182998 None 0 Human Binding pKi = 6.5 6.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 556 3 4 5 2.8 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(C2CCNCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4792127 182998 None 0 Human Binding pKi = 6.5 6.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 556 3 4 5 2.8 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(C2CCNCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
11671386 141506 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 570 5 3 7 3.4 O=C(O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL384091 141506 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 570 5 3 7 3.4 O=C(O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
11456102 80076 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL212942 80076 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
76325057 105203 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114462 105203 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
59555036 105223 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114482 105223 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
46885184 8341 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1092883 8341 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11691938 61505 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770558 61505 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11678239 61507 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770560 61507 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
23658195 181480 None 0 Human Binding pKi = 8.5 8.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 574 4 2 5 4.2 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4763305 181480 None 0 Human Binding pKi = 8.5 8.5 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 574 4 2 5 4.2 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2020.127624
6918509 77070 None 33 Rat Binding pKi = 8.5 8.5 -131 2
Binding affinity to rat CGRP receptorBinding affinity to rat 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 Rat Binding pKi = 8.5 8.5 -131 2
Binding affinity to rat CGRP receptorBinding affinity to rat 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
57977652 75112 None 0 Rat Binding pKi = 8.5 8.5 -85 2
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035981 75112 None 0 Rat Binding pKi = 8.5 8.5 -85 2
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
6918509 77070 None 33 Rat Binding pKi = 8.5 8.5 -131 2
Displacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma counting
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.2012.04.105
CHEMBL207197 77070 None 33 Rat Binding pKi = 8.5 8.5 -131 2
Displacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma counting
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.2012.04.105
11526993 200048 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
CHEMBL570531 200048 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
11397560 89742 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237661 89742 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11562434 179433 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL473445 179433 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
45485654 200041 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL570488 200041 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
11699891 61506 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 61506 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59555277 105213 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114472 105213 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
11548734 200880 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577110 200880 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
70690613 76481 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 558 6 2 5 3.8 O=C(N[C@H](Cc1ccccc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059787 76481 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 558 6 2 5 3.8 O=C(N[C@H](Cc1ccccc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59554876 105202 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114461 105202 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
10340456 83542 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL220336 83542 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44563124 189180 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 476 6 3 7 0.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL509718 189180 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 476 6 3 7 0.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
10483685 76495 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(NC(Cc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059803 76495 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(NC(Cc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59554982 105198 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114457 105198 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
24853374 105264 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114679 105264 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
44562936 179042 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL470321 179042 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11330786 138475 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL377252 138475 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46884948 7817 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
57774187 7817 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089497 7817 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
11520022 80595 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214904 80595 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44570422 190820 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2ccccc2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL518236 190820 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2ccccc2)NC1=O 10.1016/j.bmcl.2008.10.106
45487016 200241 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CCC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL571861 200241 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CCC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
44455348 155374 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1ccc(-c2ccccc2)n(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402888 155374 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1ccc(-c2ccccc2)n(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
23627980 18207 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1269978 18207 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
44570536 183979 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL480999 183979 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
45254663 127047 None 0 Human Binding pKi = 7.5 7.5 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655568 127047 None 0 Human Binding pKi = 7.5 7.5 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11157626 166531 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL427743 166531 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44563125 173931 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL453865 173931 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
23656918 91828 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241118 91828 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44563091 192649 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL521076 192649 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11977861 183313 None 0 Human Binding pKi = 6.4 6.4 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 487 2 3 4 2.7 CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4795912 183313 None 0 Human Binding pKi = 6.4 6.4 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 487 2 3 4 2.7 CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
44416436 80586 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214873 80586 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
70692303 75113 None 0 Rat Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 558 4 3 6 3.2 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035982 75113 None 0 Rat Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 558 4 3 6 3.2 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44420228 84271 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL221009 84271 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11599531 200902 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577320 200902 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44416488 137778 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 644 4 2 6 5.9 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL375872 137778 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 644 4 2 6 5.9 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
44454954 95438 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL256813 95438 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487042 200047 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)CC(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL570527 200047 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)CC(=O)N1 10.1016/j.bmcl.2009.09.066
11692140 61508 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 61508 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
23656920 89182 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL236590 89182 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
51357854 82593 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178423 82593 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
44563090 186754 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 186754 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
45485666 199877 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 4.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(Cl)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL569588 199877 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 4.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(Cl)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44563162 174681 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL455674 174681 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
25119463 181160 None 0 Human Binding pKi = 8.3 8.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 543 3 3 4 4.1 CC(C)(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4759604 181160 None 0 Human Binding pKi = 8.3 8.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 543 3 3 4 4.1 CC(C)(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
23656922 168959 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL438120 168959 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
59554885 105220 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
CHEMBL3114479 105220 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
11848908 95498 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257094 95498 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44562896 179149 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471359 179149 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45487057 200264 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 200264 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
11848966 95455 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256901 95455 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455153 97520 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270175 97520 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11215322 141865 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386113 141865 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
11848646 97562 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270390 97562 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44420228 84271 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221009 84271 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
23656586 154483 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2ccccn2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398779 154483 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2ccccn2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555326 105196 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114455 105196 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45485590 200140 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 492 6 2 5 2.7 COc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
CHEMBL571137 200140 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 492 6 2 5 2.7 COc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
11555955 200181 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 200181 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
11706251 200981 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
CHEMBL577957 200981 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
23656749 91614 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240686 91614 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
23656752 91779 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 91779 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11410749 165924 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL424864 165924 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44420287 83471 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL219782 83471 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11848755 95432 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
CHEMBL256802 95432 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
11495985 95723 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258070 95723 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44562895 179148 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL471358 179148 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
54582784 61511 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770564 61511 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11977972 181997 None 0 Human Binding pKi = 7.3 7.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 586 5 3 6 2.4 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCN2CCOCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4779094 181997 None 0 Human Binding pKi = 7.3 7.3 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 586 5 3 6 2.4 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCN2CCOCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
45487060 200083 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 449 3 2 3 2.8 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570750 200083 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 449 3 2 3 2.8 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(O)CC1 10.1016/j.bmcl.2009.09.066
11454113 145840 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL391660 145840 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11786529 139618 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL379548 139618 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
45487055 201415 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 531 3 2 4 2.3 CN1C(=O)NC(=O)C12CCN(C(=O)N[C@@H]1CC[C@@H](c3cccc(F)c3F)CN(CC(F)(F)F)C1=O)CC2 10.1016/j.bmcl.2009.09.066
CHEMBL585017 201415 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 531 3 2 4 2.3 CN1C(=O)NC(=O)C12CCN(C(=O)N[C@@H]1CC[C@@H](c3cccc(F)c3F)CN(CC(F)(F)F)C1=O)CC2 10.1016/j.bmcl.2009.09.066
59555260 105216 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114475 105216 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
44416824 80314 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2008.10.106
CHEMBL213976 80314 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2008.10.106
44570463 189753 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 501 4 2 6 3.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ccccc21 10.1016/j.bmcl.2008.10.106
CHEMBL515087 189753 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 501 4 2 6 3.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ccccc21 10.1016/j.bmcl.2008.10.106
11570464 141749 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 568 5 2 6 4.8 CC(C)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL385399 141749 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 568 5 2 6 4.8 CC(C)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
59554953 105211 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114470 105211 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
11848965 166795 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL428247 166795 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
46884946 8383 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)c(F)c1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1093189 8383 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)c(F)c1C2 10.1016/j.bmcl.2010.02.086
59554924 105208 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114467 105208 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45485676 199790 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL568880 199790 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
46179165 125255 None 0 Human Binding pKi = 7.2 7.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 493 3 2 5 3.4 O=C1NCCN(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1c1ccc(F)cc1 nan
CHEMBL3645146 125255 None 0 Human Binding pKi = 7.2 7.2 - 1
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 493 3 2 5 3.4 O=C1NCCN(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1c1ccc(F)cc1 nan
58432803 127043 None 0 Human Binding pKi = 6.2 6.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccn2)NC1=O nan
CHEMBL3655564 127043 None 0 Human Binding pKi = 6.2 6.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccn2)NC1=O nan
11713729 80581 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL214845 80581 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
11692206 80240 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213670 80240 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
24782724 181501 None 0 Human Binding pKi = 7.2 7.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 515 3 3 4 3.4 CC(C)N1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4763543 181501 None 0 Human Binding pKi = 7.2 7.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 515 3 3 4 3.4 CC(C)N1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
59555152 105214 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114473 105214 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
59731892 180797 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 591 4 2 4 5.5 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755474 180797 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 591 4 2 4 5.5 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11977740 182526 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 603 4 2 4 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3cccc(F)c3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785845 182526 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 603 4 2 4 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3cccc(F)c3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
11585317 80949 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL215325 80949 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
45487036 200082 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
CHEMBL570748 200082 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
44420241 136799 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374064 136799 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
70683851 75117 None 0 Rat Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 586 5 3 6 3.7 CC[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035986 75117 None 0 Rat Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 586 5 3 6 3.7 CC[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
46884999 7728 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 1 8 2.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)oc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1088906 7728 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 1 8 2.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)oc3cc1C2 10.1016/j.bmcl.2010.02.086
10453991 137967 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL376263 137967 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
23656753 91827 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241117 91827 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11444699 80536 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214751 80536 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44562983 191496 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 191496 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45254858 127046 None 0 Human Binding pKi = 6.2 6.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 530 5 2 9 2.0 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cnccn2)NC1=O nan
CHEMBL3655567 127046 None 0 Human Binding pKi = 6.2 6.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 530 5 2 9 2.0 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cnccn2)NC1=O nan
11849023 95211 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255755 95211 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
59554855 105197 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114456 105197 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11215639 141604 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384565 141604 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2006.07.044
45254860 127045 None 0 Human Binding pKi = 5.2 5.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 494 6 2 7 3.0 CCCC1=NC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 nan
CHEMBL3655566 127045 None 0 Human Binding pKi = 5.2 5.2 - 1
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 494 6 2 7 3.0 CCCC1=NC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 nan
45487061 200095 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 582 4 2 5 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570860 200095 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 582 4 2 5 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2009.09.066
46884948 7817 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
57774187 7817 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089497 7817 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
24862842 76496 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 598 6 3 6 3.6 O=C(NC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059804 76496 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 598 6 3 6 3.6 O=C(NC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59555024 105205 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114464 105205 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11330650 162031 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL415453 162031 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
11157609 141504 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2c1nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384080 141504 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2c1nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
11848857 95264 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255999 95264 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555012 105219 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114478 105219 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
162649395 180278 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 578 5 3 5 3.7 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4749085 180278 None 0 Human Binding pKi = 8.2 8.2 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 578 5 3 5 3.7 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
46905052 10421 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
CHEMBL1162991 10421 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
44563161 173838 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL453644 173838 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
70682193 76489 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059798 76489 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
45485665 199795 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.0 Cc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
CHEMBL568921 199795 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.0 Cc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
44455080 95681 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257902 95681 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11527287 80578 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214829 80578 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46884947 7816 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1cc(F)c(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089496 7816 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1cc(F)c(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
11848855 97641 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270796 97641 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11848750 95640 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257731 95640 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
70684297 76487 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 573 6 3 6 3.3 Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059796 76487 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 573 6 3 6 3.3 Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
59555274 105200 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114459 105200 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
23656587 90255 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238275 90255 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
9978597 141729 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
CHEMBL385322 141729 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
59554975 105224 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114483 105224 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
44420236 137676 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375533 137676 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46885133 8036 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 8036 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11849147 95306 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256203 95306 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
45485621 200952 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL577737 200952 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
59555236 105207 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114466 105207 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416512 155824 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405543 155824 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
11453687 167552 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 167552 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
70696847 76493 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059801 76493 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
11342207 141626 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384723 141626 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
11497403 166171 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL425807 166171 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
59555111 105195 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114454 105195 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44420227 83464 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL219721 83464 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
24853163 105204 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114463 105204 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45487056 200151 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 518 3 2 5 2.4 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571236 200151 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 518 3 2 5 2.4 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
76310534 105206 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114465 105206 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
23658240 181358 None 0 Human Binding pKi = 8.0 8.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 620 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3cccc(F)c3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4761776 181358 None 0 Human Binding pKi = 8.0 8.0 - 1
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 620 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3cccc(F)c3NC2=O)CC1 10.1016/j.bmcl.2020.127624
44420260 83513 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220146 83513 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44562985 186268 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487244 186268 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563160 174679 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 174679 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
45273525 198142 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 198142 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
11848698 95473 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 4 3 7 2.7 Cn1cc(-c2ccc(C(=O)O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257004 95473 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 4 3 7 2.7 Cn1cc(-c2ccc(C(=O)O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
23656919 154835 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL400020 154835 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
70694861 76610 None 0 Human Binding pKi = 6.0 6.0 - 1
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 519 3 1 6 5.0 O=C(O[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
CHEMBL2063116 76610 None 0 Human Binding pKi = 6.0 6.0 - 1
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 519 3 1 6 5.0 O=C(O[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
11848964 95257 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255966 95257 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11849020 95100 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 95100 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11532845 177854 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 7 2.0 O=C1CC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 10.1016/j.bmcl.2008.10.106
CHEMBL464263 177854 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 7 2.0 O=C1CC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 10.1016/j.bmcl.2008.10.106
11261842 81094 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215424 81094 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11215502 166230 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL426142 166230 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
23656588 91613 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2cccnc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240685 91613 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2cccnc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
68748835 220234 None 0 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
68748835.0 220234 None 0 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
CHEMBL2364638 220234 None 0 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
DB15328 220234 None 0 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
51049968 82592 None 40 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 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 None
51049968.0 82592 None 40 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 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 None
CHEMBL2178422 82592 None 40 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 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 None
DB12457 82592 None 40 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 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 None