Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11467753 173614 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
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 173614 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
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 172151 3 None - 1 Human 10.5 pEC50 = 10.5 Functional
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 172151 3 None - 1 Human 10.5 pEC50 = 10.5 Functional
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 82134 40 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 82134 40 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 211281 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 76135 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 76135 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 76139 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 76139 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 76137 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 76137 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 76136 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 76136 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 76145 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 76145 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 76144 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 76144 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 172880 0 None - 1 Human 11.0 pIC50 = 11 Functional
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 172880 0 None - 1 Human 11.0 pIC50 = 11 Functional
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 188381 0 None - 1 Human 11.0 pIC50 = 11.0 Functional
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 188381 0 None - 1 Human 11.0 pIC50 = 11.0 Functional
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 188357 0 None - 1 Human 10.8 pIC50 = 10.8 Functional
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 188357 0 None - 1 Human 10.8 pIC50 = 10.8 Functional
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 73435 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 73435 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 73752 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 73752 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 171553 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 171553 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 172187 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 172187 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
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 172151 3 None - 1 Human 10.6 pIC50 = 10.6 Functional
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 172151 3 None - 1 Human 10.6 pIC50 = 10.6 Functional
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 73757 0 None - 1 Human 10.4 pIC50 = 10.4 Functional
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 73757 0 None - 1 Human 10.4 pIC50 = 10.4 Functional
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 187793 0 None - 1 Human 10.4 pIC50 = 10.4 Functional
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 187793 0 None - 1 Human 10.4 pIC50 = 10.4 Functional
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 73425 0 None - 1 Human 10.3 pIC50 = 10.3 Functional
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 73425 0 None - 1 Human 10.3 pIC50 = 10.3 Functional
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 187644 0 None - 1 Human 10.3 pIC50 = 10.3 Functional
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 187644 0 None - 1 Human 10.3 pIC50 = 10.3 Functional
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 172758 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 172758 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 183952 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 183952 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 188373 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 188373 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 73836 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 73836 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 73422 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 73422 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 187833 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 187833 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
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 8239 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 8239 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 91887 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 91887 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 73437 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 73437 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 73423 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 73423 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 184750 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 184750 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
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 92032 1 None - 1 Human 10.0 pIC50 = 10.0 Functional
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 92032 1 None - 1 Human 10.0 pIC50 = 10.0 Functional
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 73751 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 73751 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 73754 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 73754 0 None - 1 Human 10.0 pIC50 = 10 Functional
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 184611 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 184611 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 73426 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 73426 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 197312 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 197312 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 91889 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 91889 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 188328 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 188328 0 None - 1 Human 9.9 pIC50 = 9.9 Functional
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 187668 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 187668 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 91897 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 91897 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 61172 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 61172 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 76213 6 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 76213 6 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 91886 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 91886 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
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 74723 2 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 74723 2 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 61167 1 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 61167 1 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 61171 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 61171 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 91885 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 91885 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 179349 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 179349 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 74028 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 74028 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 188766 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
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 104688 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 104688 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 61158 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 61158 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 61169 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 61169 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 73835 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 73835 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 74723 2 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 74723 2 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 73424 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 73424 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
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 61140 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 61140 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91894 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91894 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 92032 1 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 92032 1 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91896 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91896 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91898 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91898 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 61163 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 61163 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 61171 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 61171 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91890 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 91890 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 74020 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
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 74020 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
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 7696 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
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 7696 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
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 104689 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 104689 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61166 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61166 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61158 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61158 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 194600 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 194600 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61151 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61151 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 195967 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 195967 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 188766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61157 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61157 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61167 1 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61167 1 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 74024 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 74024 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 91899 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 91899 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61170 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61170 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 8109 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 8109 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 73421 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 73421 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 61172 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61172 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91905 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91905 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61162 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61162 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 74019 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 74019 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61165 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61165 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91888 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91888 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61168 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 61168 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 8228 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 8228 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 189610 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 189610 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91902 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 91902 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 10305 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 10305 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 177869 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 177869 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 144756 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 144756 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 61159 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 61159 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 74014 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 74014 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 91900 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 91900 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 74023 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 74023 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 104713 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 104713 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 89777 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 89777 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 7872 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 7872 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61165 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61165 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 74015 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 74015 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 194977 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 194977 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 7696 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 7696 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61160 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61160 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61162 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61162 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 74021 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 74021 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 61168 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61168 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 8109 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 8109 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61139 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61139 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 91891 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 91891 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 190227 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 190227 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61161 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61161 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61166 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 61166 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 91884 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 91884 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 7939 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 7939 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 187707 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 187707 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 61157 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 61157 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 74018 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 74018 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 91901 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 91901 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 192959 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 192959 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 104679 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 104679 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 146437 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 146437 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 146806 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 146806 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 183448 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 183448 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 79858 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 79858 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 141009 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 141009 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 73409 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 73409 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 89776 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 89776 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 94988 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 94988 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 154812 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 154812 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 80430 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 80430 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 96745 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 96745 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 95213 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
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 95213 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 73436 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 73436 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 195905 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 195905 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 88709 46 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 195905 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 195905 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 196001 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 196001 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 83807 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 83807 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 137346 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 137346 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 152047 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 152047 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 195946 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 195946 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 141234 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 141234 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 94945 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 94945 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 94754 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 94754 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 173908 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173908 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61143 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61143 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61147 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61147 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61145 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61145 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61146 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61146 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173245 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 173245 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 73415 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 73415 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 91895 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 91895 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 90535 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 90535 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 196759 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 196759 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 83807 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 83807 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 83807 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 83807 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 178348 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 178348 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 191887 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 191887 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 192959 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 192959 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 8240 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 8240 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 196838 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 196838 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 104653 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 104653 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 185443 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 185443 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173908 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173908 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61170 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 61170 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 73936 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 73936 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 10305 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 10305 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 195939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 195939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 195938 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 195938 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 177869 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 177869 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 185450 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 185450 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 191931 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 191931 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 104662 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 104662 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 161376 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 161376 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 104680 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 104680 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 165571 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 165571 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 140995 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 140995 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 80651 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 80651 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173995 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173995 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 190923 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 74025 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 74025 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 89264 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 89264 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 7939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 7939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 185443 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 185443 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 83825 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 83825 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 97005 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 97005 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 154732 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 154732 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 61147 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 61147 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 88704 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 88704 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 89443 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 89443 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 185449 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 185449 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 191931 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 191931 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 186055 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 186055 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91348 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91348 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 160200 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 160200 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 186051 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 186051 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 104718 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 104718 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 94922 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 94922 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 140943 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 140943 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 140191 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 140191 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 168279 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 168279 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 104668 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 104668 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 183281 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 183281 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 94988 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 94988 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 104666 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 104666 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 97126 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 97126 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 83048 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 83048 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 74012 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 74012 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 95028 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 95028 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 104663 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 104663 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 136506 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 136506 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91135 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 91135 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 80636 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 80636 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 95171 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 95171 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 166135 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 166135 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 61141 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 61141 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 104681 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 104681 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 104665 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 104665 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 152047 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 152047 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 80091 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 80091 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 61163 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 61163 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 104687 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 104687 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 73429 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 73429 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 89265 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 89265 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 89266 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 89266 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 146437 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 146437 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 161351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 161351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 146440 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 146440 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 194600 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 194600 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 74027 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 74027 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88709 46 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 8229 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 8229 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 61164 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61164 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 173151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 173151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61139 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61139 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 88709 46 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 88709 46 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 194917 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 194917 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 173151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 173151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 177869 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 177869 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 8239 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 8239 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 177017 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 177017 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61149 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61149 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61140 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61140 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61164 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61164 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 195938 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 195938 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 61169 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 61169 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 91883 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 91883 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 73935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 73935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 178478 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 178478 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 94747 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 94747 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 173995 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 173995 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 89266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 89266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 195939 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 195939 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 104664 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 104664 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 89264 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 89264 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 89267 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 89267 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 148620 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 148620 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 153598 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 153598 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 155182 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 155182 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 173152 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 173152 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 145207 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 145207 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 10305 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 10305 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 191788 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 191788 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 165872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 165872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 178454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 178454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 190923 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 190923 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 88704 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 88704 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 193374 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 193374 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 196737 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 196737 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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