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 180975 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 180975 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 179509 7 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 179509 7 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 89335 47 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 89335 47 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
DB12457 89335 47 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 219818 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 83278 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 83278 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 83282 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 83282 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 83280 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 83280 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 83279 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 83279 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 83288 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 83288 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 83287 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 83287 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 180241 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 180241 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 195757 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 195757 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 195733 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 195733 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 80573 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 80573 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 80890 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 80890 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 178908 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 178908 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 179545 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 179545 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 179509 7 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 179509 7 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 80895 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 80895 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 195166 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 195166 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 80563 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 80563 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 195016 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 195016 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 180119 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 180119 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 191324 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 191324 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 195749 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 195749 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 80974 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 80974 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 80560 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 80560 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 195206 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 195206 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 15110 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 15110 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 99108 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 99108 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 80575 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 80575 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 80561 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 80561 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 192121 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 192121 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 99253 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 99253 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 80889 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 80889 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 80892 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 80892 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 191983 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 191983 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 80564 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 80564 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 205779 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 205779 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 99110 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 99110 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 195704 1 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 195704 1 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 195040 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 195040 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 99118 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 99118 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 68290 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 68290 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 83356 7 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 83356 7 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 99107 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 99107 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 81863 3 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 81863 3 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 68285 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 68285 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 68289 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 68289 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 99106 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 99106 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 186718 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 186718 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 81167 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 81167 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 196144 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 196144 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 196144 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 196144 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 196144 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 196144 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 111957 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 111957 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 68276 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 68276 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 68287 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 68287 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 80973 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 80973 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 81863 3 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 81863 3 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 80562 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 80562 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 68258 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 68258 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 99115 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 99115 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 99253 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 99253 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 99117 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 99117 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 99119 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 99119 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 68281 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 68281 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 68289 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 68289 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 99111 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 99111 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 81159 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 81159 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 14565 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 14565 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 111958 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 111958 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 68284 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 68284 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 68276 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 68276 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 203063 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 203063 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 68269 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 68269 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 196144 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 196144 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 196144 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 196144 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 204433 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 204433 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 196144 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 196144 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 68275 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 68275 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 68285 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 68285 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 81163 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 81163 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 99120 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 99120 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 68288 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 68288 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 14980 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 14980 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 80559 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 80559 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 68290 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 68290 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 99126 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 99126 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 68280 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 68280 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 81158 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 81158 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 68283 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 68283 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 99109 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 99109 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 68286 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 68286 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 15099 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 15099 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 196993 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 196993 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 99123 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 99123 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 17190 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 17190 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 185233 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 185233 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 152079 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 152079 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 68277 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 68277 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 81153 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 81153 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 99121 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 99121 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 81162 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 81162 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 111982 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 111982 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 96997 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 96997 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 14741 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 14741 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 68283 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 68283 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 81154 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 81154 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 203441 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 203441 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 14565 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 14565 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 68278 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 68278 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 68280 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 68280 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 81160 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 81160 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 68286 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 68286 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 14980 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 14980 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 68257 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 68257 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 99112 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 99112 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 197610 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 197610 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 68279 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 68279 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 68284 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 68284 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 99105 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 99105 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 14808 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 14808 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 195080 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 195080 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 68275 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 68275 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 81157 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 81157 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 99122 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 99122 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 201345 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 201345 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 111948 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 111948 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 153760 1 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 153760 1 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 154129 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 154129 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 190819 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 190819 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 87058 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 87058 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 148331 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 148331 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 80547 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 80547 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 96996 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 96996 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 102220 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 102220 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 162142 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 162142 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 87632 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 87632 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 103981 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 103981 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 102445 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 102445 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 95928 51 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 95928 51 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 95928 51 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 95928 51 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 80574 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 80574 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 95928 51 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 95928 51 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 95928 51 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 95928 51 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 204371 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 204371 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 95928 51 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 95928 51 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 204371 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 204371 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 204467 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 204467 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 91012 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 91012 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 144663 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 144663 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 159370 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 159370 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 204412 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 204412 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 148556 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 148556 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 102177 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 102177 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 101986 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 101986 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 181269 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 181269 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 198308 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 198308 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 68261 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 68261 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 68265 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 68265 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 68263 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 68263 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 68264 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 68264 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 198308 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 198308 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 180606 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 180606 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 80553 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 80553 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 99116 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 99116 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 97755 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 97755 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 205225 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 205225 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 91012 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 91012 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 91012 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 91012 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 185715 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 185715 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 199274 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 199274 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 201345 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 201345 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 15111 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 15111 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 205304 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 205304 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 111922 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 111922 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 192814 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 192814 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 181269 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 181269 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 68288 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 68288 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 81075 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 81075 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 17190 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 17190 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 204405 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 204405 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 204404 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 204404 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 185233 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 185233 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 192821 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 192821 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 199319 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 199319 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 111931 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 111931 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 168716 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 168716 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 111949 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 111949 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 172914 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 172914 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 148317 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 148317 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 87853 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 87853 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 181356 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 181356 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 198308 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 198308 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 81164 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 81164 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 96483 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 96483 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 14808 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 14808 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 192814 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 192814 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 91030 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 91030 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 104243 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 104243 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 162062 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 162062 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 68265 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 68265 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 95923 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 95923 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 96662 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 96662 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 192820 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 192820 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 199319 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 199319 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 193426 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 193426 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 98569 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 98569 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 167538 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 167538 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 193422 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 193422 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 111987 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 111987 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 102154 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 102154 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 148265 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 148265 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 147513 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 147513 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 175635 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 175635 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 111937 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 111937 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 190652 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 190652 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 102220 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 102220 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 111935 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 111935 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 104364 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 104364 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 90250 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 90250 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 81151 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 81151 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 102260 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 102260 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 111932 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 111932 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 143821 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 143821 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 98355 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 98355 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 87838 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 87838 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 102403 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 102403 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 173478 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 173478 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 68259 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 68259 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 111950 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 111950 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 111934 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 111934 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 159370 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 159370 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 87293 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 87293 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 95928 51 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 95928 51 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 68281 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 68281 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 111956 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 111956 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 80567 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 80567 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 96484 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 96484 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 96485 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 96485 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 153760 1 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 153760 1 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 168691 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 168691 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 153763 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 153763 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 203063 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 203063 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 95928 51 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 95928 51 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 81166 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 81166 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 95928 51 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 95928 51 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 95928 51 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 95928 51 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 15100 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 15100 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 68282 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 68282 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 180512 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 180512 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 68257 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 68257 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 95928 51 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 95928 51 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 203381 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 203381 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 180512 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 180512 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 185233 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 185233 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 15110 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 15110 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 184380 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 184380 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 68267 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 68267 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 68258 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 68258 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 68282 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 68282 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 204404 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 204404 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 68287 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 68287 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 99104 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 99104 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 81074 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 81074 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 185845 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 185845 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 101979 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 101979 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 181356 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 181356 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 96485 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 96485 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 204405 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 204405 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 111933 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 111933 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 96483 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 96483 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 96486 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 96486 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 155943 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 155943 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 160923 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 160923 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 162514 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 162514 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 180513 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 180513 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 152530 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 152530 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 17190 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 17190 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 199175 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 199175 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 173215 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 173215 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 185821 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 185821 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 198308 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 198308 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 95923 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 95923 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 201833 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 201833 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 205203 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 205203 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
44593445 198308 0 None - 1 Human 7.6 pIC50 = 7.6 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 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 198308 0 None - 1 Human 7.6 pIC50 = 7.6 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 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
58901616 80555 0 None - 1 Human 6.6 pIC50 = 6.6 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018499 80555 0 None - 1 Human 6.6 pIC50 = 6.6 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 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44563160 181354 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 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 181354 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 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
23582940 203381 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 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 203381 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 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570614 184380 0 None - 1 Human 7.6 pIC50 = 7.6 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 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 184380 0 None - 1 Human 7.6 pIC50 = 7.6 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 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420236 144367 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375533 144367 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
76310534 111927 0 None - 1 Human 6.6 pIC50 = 6.6 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 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114465 111927 0 None - 1 Human 6.6 pIC50 = 6.6 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 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
23656918 98569 0 None - 1 Human 6.6 pIC50 = 6.6 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 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241118 98569 0 None - 1 Human 6.6 pIC50 = 6.6 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 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11454113 152530 0 None - 1 Human 6.6 pIC50 = 6.6 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 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 152530 0 None - 1 Human 6.6 pIC50 = 6.6 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 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44563090 193427 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 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 193427 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 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
11678239 68261 0 None - 1 Human 7.6 pIC50 = 7.6 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 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 68261 0 None - 1 Human 7.6 pIC50 = 7.6 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 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44562937 185872 0 None - 1 Human 6.6 pIC50 = 6.6 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 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 185872 0 None - 1 Human 6.6 pIC50 = 6.6 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 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44570499 199175 0 None - 1 Human 7.6 pIC50 = 7.6 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 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 199175 0 None - 1 Human 7.6 pIC50 = 7.6 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 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44570580 184226 0 None - 1 Human 7.6 pIC50 = 7.6 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 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 184226 0 None - 1 Human 7.6 pIC50 = 7.6 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 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11692140 68262 0 None - 1 Human 7.6 pIC50 = 7.6 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 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 68262 0 None - 1 Human 7.6 pIC50 = 7.6 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 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
11238250 80884 0 None - 1 Human 7.6 pIC50 = 7.6 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022595 80884 0 None - 1 Human 7.6 pIC50 = 7.6 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 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
44563123 195665 0 None - 1 Human 6.6 pIC50 = 6.6 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 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL507339 195665 0 None - 1 Human 6.6 pIC50 = 6.6 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 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11848855 104364 0 None - 1 Human 6.6 pIC50 = 6.6 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 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 104364 0 None - 1 Human 6.6 pIC50 = 6.6 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 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11849020 101822 0 None - 1 Human 6.6 pIC50 = 6.6 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 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 101822 0 None - 1 Human 6.6 pIC50 = 6.6 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 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11444589 86564 0 None - 1 Human 6.5 pIC50 = 6.5 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 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL211931 86564 0 None - 1 Human 6.5 pIC50 = 6.5 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 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
117992192 154039 0 None - 1 Human 6.5 pIC50 = 6.5 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
CHEMBL3928622 154039 0 None - 1 Human 6.5 pIC50 = 6.5 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
10340456 90284 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL220336 90284 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
59555236 111928 0 None - 1 Human 5.5 pIC50 = 5.5 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 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114466 111928 0 None - 1 Human 5.5 pIC50 = 5.5 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 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59554895 111952 0 None - 1 Human 8.5 pIC50 = 8.5 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 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114490 111952 0 None - 1 Human 8.5 pIC50 = 8.5 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 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11192602 153763 0 None - 1 Human 8.5 pIC50 = 8.5 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 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 153763 0 None - 1 Human 8.5 pIC50 = 8.5 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 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11364735 96484 0 None - 1 Human 8.5 pIC50 = 8.5 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 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 96484 0 None - 1 Human 8.5 pIC50 = 8.5 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 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23657089 153758 0 None - 1 Human 8.5 pIC50 = 8.5 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 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 153758 0 None - 1 Human 8.5 pIC50 = 8.5 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 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45271754 201833 0 None - 1 Human 8.5 pIC50 = 8.5 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 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL549503 201833 0 None - 1 Human 8.5 pIC50 = 8.5 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 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11606400 68269 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 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 68269 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 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11584808 204467 0 None - 1 Human 8.5 pIC50 = 8.5 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 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 204467 0 None - 1 Human 8.5 pIC50 = 8.5 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 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
11341430 81165 0 None - 1 Human 8.5 pIC50 = 8.5 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
CHEMBL2024601 81165 0 None - 1 Human 8.5 pIC50 = 8.5 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 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
11721278 68268 0 None - 1 Human 8.4 pIC50 = 8.4 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 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 68268 0 None - 1 Human 8.4 pIC50 = 8.4 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 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44563160 181354 0 None - 1 Human 7.5 pIC50 = 7.5 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 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 181354 0 None - 1 Human 7.5 pIC50 = 7.5 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 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11249157 81155 0 None - 1 Human 7.5 pIC50 = 7.5 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024591 81155 0 None - 1 Human 7.5 pIC50 = 7.5 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 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11375693 96661 0 None - 1 Human 7.5 pIC50 = 7.5 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 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 96661 0 None - 1 Human 7.5 pIC50 = 7.5 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 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
58864453 80470 0 None - 1 Human 6.5 pIC50 = 6.5 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018356 80470 0 None - 1 Human 6.5 pIC50 = 6.5 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 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11848963 162213 0 None - 1 Human 6.5 pIC50 = 6.5 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 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL403765 162213 0 None - 1 Human 6.5 pIC50 = 6.5 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 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455457 101985 0 None - 1 Human 6.5 pIC50 = 6.5 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 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 101985 0 None - 1 Human 6.5 pIC50 = 6.5 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 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44563161 180513 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 180513 0 None - 1 Human 7.5 pIC50 = 7.5 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 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
46905052 17190 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 17190 0 None - 1 Human 7.5 pIC50 = 7.5 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 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
11497403 172855 0 None - 1 Human 5.5 pIC50 = 5.5 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 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL425807 172855 0 None - 1 Human 5.5 pIC50 = 5.5 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 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
70685453 80550 0 None - 1 Human 7.5 pIC50 = 7.5 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018494 80550 0 None - 1 Human 7.5 pIC50 = 7.5 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 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
59554855 111918 0 None - 1 Human 6.5 pIC50 = 6.5 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 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114456 111918 0 None - 1 Human 6.5 pIC50 = 6.5 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 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
10483468 80571 0 None - 1 Human 6.5 pIC50 = 6.5 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018515 80571 0 None - 1 Human 6.5 pIC50 = 6.5 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 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11699891 68260 0 None - 1 Human 7.5 pIC50 = 7.5 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 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 68260 0 None - 1 Human 7.5 pIC50 = 7.5 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 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59554993 111951 0 None - 1 Human 7.5 pIC50 = 7.5 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 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114489 111951 0 None - 1 Human 7.5 pIC50 = 7.5 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 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
46885184 15111 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 15111 0 None - 1 Human 7.5 pIC50 = 7.5 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 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11848750 102362 0 None - 1 Human 6.5 pIC50 = 6.5 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 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257731 102362 0 None - 1 Human 6.5 pIC50 = 6.5 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 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
10453991 144658 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL376263 144658 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44455043 102501 0 None - 1 Human 6.5 pIC50 = 6.5 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 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258329 102501 0 None - 1 Human 6.5 pIC50 = 6.5 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 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11410749 172608 0 None - 1 Human 7.5 pIC50 = 7.5 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 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL424864 172608 0 None - 1 Human 7.5 pIC50 = 7.5 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 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11541560 68267 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 68267 0 None - 1 Human 7.5 pIC50 = 7.5 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 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
24756768 80568 0 None - 1 Human 7.5 pIC50 = 7.5 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018512 80568 0 None - 1 Human 7.5 pIC50 = 7.5 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 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
23656919 161524 0 None - 1 Human 6.5 pIC50 = 6.5 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(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL400020 161524 0 None - 1 Human 6.5 pIC50 = 6.5 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(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11168000 160962 0 None - 1 Human 6.5 pIC50 = 6.5 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 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 160962 0 None - 1 Human 6.5 pIC50 = 6.5 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 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11848968 101980 0 None - 1 Human 6.5 pIC50 = 6.5 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 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255967 101980 0 None - 1 Human 6.5 pIC50 = 6.5 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 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44570579 197610 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 197610 0 None - 1 Human 7.5 pIC50 = 7.5 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 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420287 90214 0 None - 1 Human 6.5 pIC50 = 6.5 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)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL219782 90214 0 None - 1 Human 6.5 pIC50 = 6.5 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)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL2371945 216936 0 None - 1 Human 5.5 pIC50 = 5.5 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 None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)NN(C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
59554975 111945 0 None - 1 Human 7.4 pIC50 = 7.4 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 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114483 111945 0 None - 1 Human 7.4 pIC50 = 7.4 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 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
11849147 102028 0 None - 1 Human 6.4 pIC50 = 6.4 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 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256203 102028 0 None - 1 Human 6.4 pIC50 = 6.4 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 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
44417050 148287 0 None - 1 Human 6.4 pIC50 = 6.4 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 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384539 148287 0 None - 1 Human 6.4 pIC50 = 6.4 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 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
11541725 148164 0 None - 1 Human 7.4 pIC50 = 7.4 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(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL383872 148164 0 None - 1 Human 7.4 pIC50 = 7.4 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(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
45273525 202465 0 None - 1 Human 7.4 pIC50 = 7.4 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 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 202465 0 None - 1 Human 7.4 pIC50 = 7.4 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 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
45269221 203436 0 None - 1 Human 7.4 pIC50 = 7.4 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 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 203436 0 None - 1 Human 7.4 pIC50 = 7.4 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 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44563028 201345 0 None - 1 Human 6.4 pIC50 = 6.4 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 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 201345 0 None - 1 Human 6.4 pIC50 = 6.4 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 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
59554982 111919 0 None - 1 Human 6.4 pIC50 = 6.4 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 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114457 111919 0 None - 1 Human 6.4 pIC50 = 6.4 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 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
24853374 111985 0 None - 1 Human 6.4 pIC50 = 6.4 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 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114679 111985 0 None - 1 Human 6.4 pIC50 = 6.4 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 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
44416436 87330 0 None - 1 Human 6.4 pIC50 = 6.4 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)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214873 87330 0 None - 1 Human 6.4 pIC50 = 6.4 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)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
11168000 160962 0 None - 1 Human 7.4 pIC50 = 7.4 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 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 160962 0 None - 1 Human 7.4 pIC50 = 7.4 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 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
23656752 98520 0 None - 1 Human 6.4 pIC50 = 6.4 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 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 98520 0 None - 1 Human 6.4 pIC50 = 6.4 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 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
72194744 159691 0 None - 1 Human 6.4 pIC50 = 6.4 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 537 3 2 5 4.7 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL3974762 159691 0 None - 1 Human 6.4 pIC50 = 6.4 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 537 3 2 5 4.7 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
44420691 168682 0 None - 1 Human 6.4 pIC50 = 6.4 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 1196 28 12 14 -1.7 CC(C)[C@H](NC(=O)N(CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL415186 168682 0 None - 1 Human 6.4 pIC50 = 6.4 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 1196 28 12 14 -1.7 CC(C)[C@H](NC(=O)N(CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44570615 184381 9 None - 1 Human 7.4 pIC50 = 7.4 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 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 184381 9 None - 1 Human 7.4 pIC50 = 7.4 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 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44420241 143490 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374064 143490 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44455457 101985 0 None - 1 Human 6.4 pIC50 = 6.4 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 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 101985 0 None - 1 Human 6.4 pIC50 = 6.4 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 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
54587752 68277 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 68277 0 None - 1 Human 8.4 pIC50 = 8.4 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 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
6918509 83817 41 None - 1 Human 8.4 pIC50 = 8.4 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 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL207197 83817 41 None - 1 Human 8.4 pIC50 = 8.4 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 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.12.089
59555074 111946 0 None - 1 Human 8.4 pIC50 = 8.4 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
CHEMBL3114484 111946 0 None - 1 Human 8.4 pIC50 = 8.4 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
23657089 153758 0 None - 1 Human 8.4 pIC50 = 8.4 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 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 153758 0 None - 1 Human 8.4 pIC50 = 8.4 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 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
54581838 68263 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 68263 0 None - 1 Human 8.4 pIC50 = 8.4 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 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54583775 68266 0 None - 1 Human 8.4 pIC50 = 8.4 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 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 68266 0 None - 1 Human 8.4 pIC50 = 8.4 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 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11295168 81156 0 None - 1 Human 8.4 pIC50 = 8.4 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024592 81156 0 None - 1 Human 8.4 pIC50 = 8.4 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 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
45271740 203325 0 None - 1 Human 8.4 pIC50 = 8.4 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 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 203325 0 None - 1 Human 8.4 pIC50 = 8.4 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 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
46885242 15099 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 15099 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 196993 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 196993 0 None - 1 Human 8.4 pIC50 = 8.4 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 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
54581897 68279 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 68279 0 None - 1 Human 8.4 pIC50 = 8.4 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 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
72194609 167441 0 None - 1 Human 8.4 pIC50 = 8.4 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 537 3 2 5 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
CHEMBL4113356 167441 0 None - 1 Human 8.4 pIC50 = 8.4 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 537 3 2 5 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 nan
70695974 80576 0 None - 1 Human 8.3 pIC50 = 8.3 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 643 7 2 5 5.1 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018520 80576 0 None - 1 Human 8.3 pIC50 = 8.3 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 643 7 2 5 5.1 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
46885134 14807 0 None - 1 Human 8.3 pIC50 = 8.3 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 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 14807 0 None - 1 Human 8.3 pIC50 = 8.3 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 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11398863 81161 0 None - 1 Human 8.3 pIC50 = 8.3 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024597 81161 0 None - 1 Human 8.3 pIC50 = 8.3 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 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11273798 99113 0 None - 1 Human 8.3 pIC50 = 8.3 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 654 5 4 4 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)c(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430172 99113 0 None - 1 Human 8.3 pIC50 = 8.3 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 654 5 4 4 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)c(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11785573 99125 0 None - 1 Human 8.3 pIC50 = 8.3 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 512 5 3 5 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2C)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430184 99125 0 None - 1 Human 8.3 pIC50 = 8.3 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 512 5 3 5 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2C)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
24853164 111938 0 None - 1 Human 7.4 pIC50 = 7.4 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(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114476 111938 0 None - 1 Human 7.4 pIC50 = 7.4 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(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44563089 192939 0 None - 1 Human 5.4 pIC50 = 5.4 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 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 192939 0 None - 1 Human 5.4 pIC50 = 5.4 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 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
44562897 185845 0 None - 1 Human 7.4 pIC50 = 7.4 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 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 185845 0 None - 1 Human 7.4 pIC50 = 7.4 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44570578 185189 0 None - 1 Human 6.4 pIC50 = 6.4 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 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 185189 0 None - 1 Human 6.4 pIC50 = 6.4 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 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44563090 193427 0 None - 1 Human 6.4 pIC50 = 6.4 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 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 193427 0 None - 1 Human 6.4 pIC50 = 6.4 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 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
44563126 195712 0 None - 1 Human 7.4 pIC50 = 7.4 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 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 195712 0 None - 1 Human 7.4 pIC50 = 7.4 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 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
46885186 14805 0 None - 1 Human 7.4 pIC50 = 7.4 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 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 14805 0 None - 1 Human 7.4 pIC50 = 7.4 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 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11786529 146309 0 None - 1 Human 6.4 pIC50 = 6.4 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 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL379548 146309 0 None - 1 Human 6.4 pIC50 = 6.4 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 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
44420227 90207 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL219721 90207 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44417049 175598 0 None - 1 Human 6.4 pIC50 = 6.4 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 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL437718 175598 0 None - 1 Human 6.4 pIC50 = 6.4 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 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44563089 192939 0 None - 1 Human 7.4 pIC50 = 7.4 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 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 192939 0 None - 1 Human 7.4 pIC50 = 7.4 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 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
59554936 111939 0 None - 1 Human 7.4 pIC50 = 7.4 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 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114477 111939 0 None - 1 Human 7.4 pIC50 = 7.4 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 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
59555036 111944 0 None - 1 Human 7.4 pIC50 = 7.4 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 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114482 111944 0 None - 1 Human 7.4 pIC50 = 7.4 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 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11432505 204412 0 None - 1 Human 7.4 pIC50 = 7.4 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 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 204412 0 None - 1 Human 7.4 pIC50 = 7.4 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 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
46885245 14619 0 None - 1 Human 7.4 pIC50 = 7.4 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 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 14619 0 None - 1 Human 7.4 pIC50 = 7.4 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 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
44562937 185872 0 None - 1 Human 5.4 pIC50 = 5.4 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 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 185872 0 None - 1 Human 5.4 pIC50 = 5.4 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 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44416437 148572 0 None - 1 Human 6.4 pIC50 = 6.4 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 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386204 148572 0 None - 1 Human 6.4 pIC50 = 6.4 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 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
11423175 143756 0 None - 1 Human 5.4 pIC50 = 5.4 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 949 23 11 12 -2.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCCN1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL374579 143756 0 None - 1 Human 5.4 pIC50 = 5.4 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 949 23 11 12 -2.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCCN1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
59555102 111986 0 None - 1 Human 5.4 pIC50 = 5.4 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 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114680 111986 0 None - 1 Human 5.4 pIC50 = 5.4 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 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11549001 148657 0 None - 1 Human 6.4 pIC50 = 6.4 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 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386701 148657 0 None - 1 Human 6.4 pIC50 = 6.4 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 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44563027 193423 0 None - 1 Human 6.4 pIC50 = 6.4 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL488066 193423 0 None - 1 Human 6.4 pIC50 = 6.4 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
44562983 198166 0 None - 1 Human 5.4 pIC50 = 5.4 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 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 198166 0 None - 1 Human 5.4 pIC50 = 5.4 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 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
59555274 111921 0 None - 1 Human 5.3 pIC50 = 5.3 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 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114459 111921 0 None - 1 Human 5.3 pIC50 = 5.3 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 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11628731 87168 0 None - 1 Human 7.3 pIC50 = 7.3 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(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214507 87168 0 None - 1 Human 7.3 pIC50 = 7.3 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(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
76332330 111983 0 None - 1 Human 7.3 pIC50 = 7.3 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
CHEMBL3114677 111983 0 None - 1 Human 7.3 pIC50 = 7.3 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
58864250 80548 0 None - 1 Human 7.3 pIC50 = 7.3 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018492 80548 0 None - 1 Human 7.3 pIC50 = 7.3 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 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
122238743 167538 0 None - 1 Human 5.3 pIC50 = 5.3 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 167538 0 None - 1 Human 5.3 pIC50 = 5.3 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
44455078 102363 0 None - 1 Human 6.3 pIC50 = 6.3 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 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257732 102363 0 None - 1 Human 6.3 pIC50 = 6.3 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 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
72194610 159370 0 None - 1 Human 6.3 pIC50 = 6.3 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 159370 0 None - 1 Human 6.3 pIC50 = 6.3 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
59554876 111923 0 None - 1 Human 5.3 pIC50 = 5.3 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 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114461 111923 0 None - 1 Human 5.3 pIC50 = 5.3 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 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11421827 164383 0 None - 1 Human 7.3 pIC50 = 7.3 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 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL408093 164383 0 None - 1 Human 7.3 pIC50 = 7.3 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 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
11421827 164383 0 None - 1 Human 7.3 pIC50 = 7.3 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 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 164383 0 None - 1 Human 7.3 pIC50 = 7.3 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 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
44562939 185874 0 None - 1 Human 6.3 pIC50 = 6.3 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]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 185874 0 None - 1 Human 6.3 pIC50 = 6.3 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]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11495985 102445 0 None - 1 Human 6.3 pIC50 = 6.3 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 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 102445 0 None - 1 Human 6.3 pIC50 = 6.3 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 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11284233 96662 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 96662 0 None - 1 Human 8.3 pIC50 = 8.3 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 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11752904 154129 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 154129 0 None - 1 Human 8.3 pIC50 = 8.3 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 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11180666 153872 0 None - 1 Human 8.3 pIC50 = 8.3 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 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 153872 0 None - 1 Human 8.3 pIC50 = 8.3 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 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11512928 148449 0 None - 1 Human 8.3 pIC50 = 8.3 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 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
CHEMBL385454 148449 0 None - 1 Human 8.3 pIC50 = 8.3 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 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
44570580 184226 0 None - 1 Human 8.3 pIC50 = 8.3 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 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 184226 0 None - 1 Human 8.3 pIC50 = 8.3 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 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
23582940 203381 0 None - 1 Human 8.3 pIC50 = 8.3 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 203381 0 None - 1 Human 8.3 pIC50 = 8.3 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 180512 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 180512 0 None - 1 Human 8.3 pIC50 = 8.3 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 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
25227362 180512 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 180512 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 185233 0 None - 1 Human 8.3 pIC50 = 8.3 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 185233 0 None - 1 Human 8.3 pIC50 = 8.3 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
44563050 193426 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 193426 0 None - 1 Human 8.3 pIC50 = 8.3 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 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
44570615 184381 9 None - 1 Human 8.2 pIC50 = 8.2 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 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 184381 9 None - 1 Human 8.2 pIC50 = 8.2 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 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
10438558 80565 0 None - 1 Human 8.2 pIC50 = 8.2 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018509 80565 0 None - 1 Human 8.2 pIC50 = 8.2 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 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
46885133 14806 0 None - 1 Human 7.3 pIC50 = 7.3 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 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 14806 0 None - 1 Human 7.3 pIC50 = 7.3 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 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
44420260 90255 0 None - 1 Human 7.3 pIC50 = 7.3 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(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220146 90255 0 None - 1 Human 7.3 pIC50 = 7.3 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(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420250 143706 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374251 143706 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
59555111 111916 0 None - 1 Human 5.3 pIC50 = 5.3 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 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114454 111916 0 None - 1 Human 5.3 pIC50 = 5.3 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 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59555024 111926 0 None - 1 Human 6.3 pIC50 = 6.3 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 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114464 111926 0 None - 1 Human 6.3 pIC50 = 6.3 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 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11453687 174233 0 None - 1 Human 6.3 pIC50 = 6.3 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 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 174233 0 None - 1 Human 6.3 pIC50 = 6.3 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 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
24756769 80570 0 None - 1 Human 7.3 pIC50 = 7.3 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018514 80570 0 None - 1 Human 7.3 pIC50 = 7.3 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 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
44420235 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
45273525 202465 0 None - 1 Human 6.3 pIC50 = 6.3 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 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 202465 0 None - 1 Human 6.3 pIC50 = 6.3 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 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
44420235 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
44420235 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 91549 0 None - 1 Human 6.3 pIC50 = 6.3 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
9978597 148420 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
CHEMBL385322 148420 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
44420245 90779 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
CHEMBL220715 90779 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
44454954 102160 0 None - 1 Human 6.3 pIC50 = 6.3 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 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL256813 102160 0 None - 1 Human 6.3 pIC50 = 6.3 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 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487057 204587 0 None - 1 Human 7.3 pIC50 = 7.3 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 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 204587 0 None - 1 Human 7.3 pIC50 = 7.3 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 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
11849024 162062 0 None - 1 Human 6.3 pIC50 = 6.3 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 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 162062 0 None - 1 Human 6.3 pIC50 = 6.3 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 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455041 177376 0 None - 1 Human 6.3 pIC50 = 6.3 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 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL445069 177376 0 None - 1 Human 6.3 pIC50 = 6.3 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 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44570536 190652 0 None - 1 Human 7.2 pIC50 = 7.2 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 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 190652 0 None - 1 Human 7.2 pIC50 = 7.2 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 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
72194743 166842 0 None - 1 Human 6.2 pIC50 = 6.2 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
CHEMBL4108361 166842 0 None - 1 Human 6.2 pIC50 = 6.2 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
44420693 175256 0 None - 1 Human 5.2 pIC50 = 5.2 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 1196 28 12 14 -1.4 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL435149 175256 0 None - 1 Human 5.2 pIC50 = 5.2 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 1196 28 12 14 -1.4 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL438426 220550 0 None - 1 Human 6.2 pIC50 = 6.2 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 None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)N(N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44562896 185822 0 None - 1 Human 7.2 pIC50 = 7.2 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 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471359 185822 0 None - 1 Human 7.2 pIC50 = 7.2 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 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
58864479 80554 0 None - 1 Human 7.2 pIC50 = 7.2 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018498 80554 0 None - 1 Human 7.2 pIC50 = 7.2 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 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44562938 185873 0 None - 1 Human 6.2 pIC50 = 6.2 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 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471705 185873 0 None - 1 Human 6.2 pIC50 = 6.2 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 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
11753024 81152 0 None - 1 Human 8.2 pIC50 = 8.2 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024588 81152 0 None - 1 Human 8.2 pIC50 = 8.2 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 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11375693 96661 0 None - 1 Human 8.2 pIC50 = 8.2 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 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 96661 0 None - 1 Human 8.2 pIC50 = 8.2 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 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23656921 96997 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 96997 0 None - 1 Human 8.2 pIC50 = 8.2 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 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
72194608 150957 0 None - 1 Human 8.2 pIC50 = 8.2 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
CHEMBL3904139 150957 0 None - 1 Human 8.2 pIC50 = 8.2 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
45267481 203441 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 203441 0 None - 1 Human 8.2 pIC50 = 8.2 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 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
46885243 15100 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 15100 0 None - 1 Human 8.2 pIC50 = 8.2 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 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11691938 68259 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 68259 0 None - 1 Human 8.2 pIC50 = 8.2 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 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
21102038 80569 0 None - 1 Human 8.2 pIC50 = 8.2 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018513 80569 0 None - 1 Human 8.2 pIC50 = 8.2 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 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
44562939 185874 0 None - 1 Human 7.2 pIC50 = 7.2 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 185874 0 None - 1 Human 7.2 pIC50 = 7.2 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59555157 111936 0 None - 1 Human 7.2 pIC50 = 7.2 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 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114474 111936 0 None - 1 Human 7.2 pIC50 = 7.2 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 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
11555955 204504 0 None - 1 Human 7.2 pIC50 = 7.2 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 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 204504 0 None - 1 Human 7.2 pIC50 = 7.2 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 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
44420240 90250 0 None - 1 Human 7.2 pIC50 = 7.2 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 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 90250 0 None - 1 Human 7.2 pIC50 = 7.2 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 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420240 90250 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220101 90250 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11456102 86820 0 None - 1 Human 6.2 pIC50 = 6.2 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(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL212942 86820 0 None - 1 Human 6.2 pIC50 = 6.2 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(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
59554885 111941 0 None - 1 Human 7.2 pIC50 = 7.2 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 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
CHEMBL3114479 111941 0 None - 1 Human 7.2 pIC50 = 7.2 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 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
23656752 98520 0 None - 1 Human 6.2 pIC50 = 6.2 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 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 98520 0 None - 1 Human 6.2 pIC50 = 6.2 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 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11330786 145166 0 None - 1 Human 6.2 pIC50 = 6.2 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(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL377252 145166 0 None - 1 Human 6.2 pIC50 = 6.2 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(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44562985 192941 0 None - 1 Human 7.2 pIC50 = 7.2 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487244 192941 0 None - 1 Human 7.2 pIC50 = 7.2 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 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
11721278 68268 0 None - 1 Human 7.2 pIC50 = 7.2 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 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 68268 0 None - 1 Human 7.2 pIC50 = 7.2 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 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44420256 91722 0 None - 1 Human 7.2 pIC50 = 7.2 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(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223756 91722 0 None - 1 Human 7.2 pIC50 = 7.2 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(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420261 144061 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375224 144061 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
59555066 111955 0 None - 1 Human 7.2 pIC50 = 7.2 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 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114493 111955 0 None - 1 Human 7.2 pIC50 = 7.2 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 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11351794 97755 0 None - 1 Human 7.2 pIC50 = 7.2 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](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL239630 97755 0 None - 1 Human 7.2 pIC50 = 7.2 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](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
117992083 151673 0 None - 1 Human 7.2 pIC50 = 7.2 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
CHEMBL3910081 151673 0 None - 1 Human 7.2 pIC50 = 7.2 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
11849023 101933 0 None - 1 Human 6.2 pIC50 = 6.2 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 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255755 101933 0 None - 1 Human 6.2 pIC50 = 6.2 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 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11848800 162051 0 None - 1 Human 6.2 pIC50 = 6.2 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 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL402844 162051 0 None - 1 Human 6.2 pIC50 = 6.2 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 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45271740 203325 0 None - 1 Human 7.2 pIC50 = 7.2 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 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 203325 0 None - 1 Human 7.2 pIC50 = 7.2 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 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
44420692 168531 0 None - 1 Human 7.2 pIC50 = 7.2 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 1196 28 13 14 -1.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NNC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
CHEMBL413872 168531 0 None - 1 Human 7.2 pIC50 = 7.2 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 1196 28 13 14 -1.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NNC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
11692206 86984 0 None - 1 Human 6.2 pIC50 = 6.2 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 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213670 86984 0 None - 1 Human 6.2 pIC50 = 6.2 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 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
10340395 91770 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL223805 91770 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
11599531 205225 0 None - 1 Human 6.2 pIC50 = 6.2 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 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 205225 0 None - 1 Human 6.2 pIC50 = 6.2 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 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
11699891 68260 0 None - 1 Human 8.1 pIC50 = 8.1 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 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 68260 0 None - 1 Human 8.1 pIC50 = 8.1 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 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
45269221 203436 0 None - 1 Human 8.1 pIC50 = 8.1 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 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 203436 0 None - 1 Human 8.1 pIC50 = 8.1 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 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46885245 14619 0 None - 1 Human 8.1 pIC50 = 8.1 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 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 14619 0 None - 1 Human 8.1 pIC50 = 8.1 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 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
46885186 14805 0 None - 1 Human 8.1 pIC50 = 8.1 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 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 14805 0 None - 1 Human 8.1 pIC50 = 8.1 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 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
54583775 68266 0 None - 1 Human 8.1 pIC50 = 8.1 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 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 68266 0 None - 1 Human 8.1 pIC50 = 8.1 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 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11444574 99114 0 None - 1 Human 8.1 pIC50 = 8.1 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 576 5 4 4 4.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430173 99114 0 None - 1 Human 8.1 pIC50 = 8.1 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 576 5 4 4 4.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(Br)[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
54583774 68264 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 68264 0 None - 1 Human 8.1 pIC50 = 8.1 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 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11453687 174233 0 None - 1 Human 6.2 pIC50 = 6.2 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 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 174233 0 None - 1 Human 6.2 pIC50 = 6.2 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 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL376719 219034 0 None - 1 Human 6.2 pIC50 = 6.2 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 None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
24853163 111925 0 None - 1 Human 6.2 pIC50 = 6.2 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 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114463 111925 0 None - 1 Human 6.2 pIC50 = 6.2 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 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416512 162513 0 None - 1 Human 6.2 pIC50 = 6.2 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 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405543 162513 0 None - 1 Human 6.2 pIC50 = 6.2 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 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44455153 104243 0 None - 1 Human 6.2 pIC50 = 6.2 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 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 104243 0 None - 1 Human 6.2 pIC50 = 6.2 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 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44563051 193454 0 None - 1 Human 7.1 pIC50 = 7.1 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 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488255 193454 0 None - 1 Human 7.1 pIC50 = 7.1 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 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
59554934 111954 0 None - 1 Human 7.1 pIC50 = 7.1 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 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114492 111954 0 None - 1 Human 7.1 pIC50 = 7.1 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 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11421827 164383 0 None - 1 Human 6.1 pIC50 = 6.1 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 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 164383 0 None - 1 Human 6.1 pIC50 = 6.1 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 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
11571094 148668 0 None - 1 Human 7.1 pIC50 = 7.1 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 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386757 148668 0 None - 1 Human 7.1 pIC50 = 7.1 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 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44570498 190819 0 None - 1 Human 7.1 pIC50 = 7.1 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 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 190819 0 None - 1 Human 7.1 pIC50 = 7.1 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 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
76310551 111984 0 None - 1 Human 6.1 pIC50 = 6.1 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 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114678 111984 0 None - 1 Human 6.1 pIC50 = 6.1 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 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59554924 111929 0 None - 1 Human 6.1 pIC50 = 6.1 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 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114467 111929 0 None - 1 Human 6.1 pIC50 = 6.1 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 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
23656749 98355 0 None - 1 Human 6.1 pIC50 = 6.1 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 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240686 98355 0 None - 1 Human 6.1 pIC50 = 6.1 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 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44562936 185715 0 None - 1 Human 7.1 pIC50 = 7.1 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]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL470321 185715 0 None - 1 Human 7.1 pIC50 = 7.1 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]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563126 195712 0 None - 1 Human 7.1 pIC50 = 7.1 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 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 195712 0 None - 1 Human 7.1 pIC50 = 7.1 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 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59554857 111920 0 None - 1 Human 5.1 pIC50 = 5.1 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 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114458 111920 0 None - 1 Human 5.1 pIC50 = 5.1 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 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL223642 216224 0 None - 1 Human 6.1 pIC50 = 6.1 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 None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061343w
44420235 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44420235 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
44420235 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 91549 0 None - 1 Human 7.1 pIC50 = 7.1 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 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420235 91549 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223156 91549 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
72194611 155943 0 None - 1 Human 7.1 pIC50 = 7.1 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 155943 0 None - 1 Human 7.1 pIC50 = 7.1 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
44563025 199274 0 None - 1 Human 6.1 pIC50 = 6.1 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]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL520905 199274 0 None - 1 Human 6.1 pIC50 = 6.1 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]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
11520022 87339 0 None - 1 Human 6.1 pIC50 = 6.1 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 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214904 87339 0 None - 1 Human 6.1 pIC50 = 6.1 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 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11555955 204504 0 None - 1 Human 6.1 pIC50 = 6.1 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 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 204504 0 None - 1 Human 6.1 pIC50 = 6.1 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 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
11225752 96486 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 96486 0 None - 1 Human 8.1 pIC50 = 8.1 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 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11180666 153872 0 None - 1 Human 8.1 pIC50 = 8.1 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 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 153872 0 None - 1 Human 8.1 pIC50 = 8.1 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 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11432931 168691 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 168691 0 None - 1 Human 8.1 pIC50 = 8.1 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 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23656922 175635 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 175635 0 None - 1 Human 8.1 pIC50 = 8.1 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 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
23582940 203381 0 None - 1 Human 8.1 pIC50 = 8.1 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 assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 203381 0 None - 1 Human 8.1 pIC50 = 8.1 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 assay in presence of 50% human serumAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
11156698 81076 0 None - 1 Human 8.1 pIC50 = 8.1 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024173 81076 0 None - 1 Human 8.1 pIC50 = 8.1 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 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
11520007 68278 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 68278 0 None - 1 Human 8.1 pIC50 = 8.1 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 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
44570578 185189 0 None - 1 Human 8.1 pIC50 = 8.1 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 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 185189 0 None - 1 Human 8.1 pIC50 = 8.1 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 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11692140 68262 0 None - 1 Human 8.1 pIC50 = 8.1 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 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 68262 0 None - 1 Human 8.1 pIC50 = 8.1 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 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
11432183 81073 0 None - 1 Human 8.1 pIC50 = 8.1 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024170 81073 0 None - 1 Human 8.1 pIC50 = 8.1 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 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
24756767 80566 0 None - 1 Human 8.1 pIC50 = 8.1 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018510 80566 0 None - 1 Human 8.1 pIC50 = 8.1 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 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
59554942 111930 0 None - 1 Human 6.1 pIC50 = 6.1 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 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114468 111930 0 None - 1 Human 6.1 pIC50 = 6.1 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 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11527287 87322 0 None - 1 Human 6.1 pIC50 = 6.1 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 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214829 87322 0 None - 1 Human 6.1 pIC50 = 6.1 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 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46885134 14807 0 None - 1 Human 7.1 pIC50 = 7.1 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 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 14807 0 None - 1 Human 7.1 pIC50 = 7.1 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 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11849025 102260 0 None - 1 Human 6.1 pIC50 = 6.1 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 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 102260 0 None - 1 Human 6.1 pIC50 = 6.1 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 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11848645 104286 0 None - 1 Human 6.1 pIC50 = 6.1 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(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270392 104286 0 None - 1 Human 6.1 pIC50 = 6.1 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(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555055 111953 0 None - 1 Human 7.1 pIC50 = 7.1 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 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114491 111953 0 None - 1 Human 7.1 pIC50 = 7.1 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 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555326 111917 0 None - 1 Human 6.1 pIC50 = 6.1 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 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114455 111917 0 None - 1 Human 6.1 pIC50 = 6.1 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 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11585317 87693 0 None - 1 Human 7.1 pIC50 = 7.1 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 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL215325 87693 0 None - 1 Human 7.1 pIC50 = 7.1 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 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
46885133 14806 0 None - 1 Human 6.1 pIC50 = 6.1 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 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 14806 0 None - 1 Human 6.1 pIC50 = 6.1 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 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
59555012 111940 0 None - 1 Human 7.1 pIC50 = 7.1 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 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114478 111940 0 None - 1 Human 7.1 pIC50 = 7.1 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 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
11548734 205203 0 None - 1 Human 6.1 pIC50 = 6.1 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 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 205203 0 None - 1 Human 6.1 pIC50 = 6.1 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 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44455080 102403 0 None - 1 Human 6.1 pIC50 = 6.1 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 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 102403 0 None - 1 Human 6.1 pIC50 = 6.1 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 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555230 111942 0 None - 1 Human 7.1 pIC50 = 7.1 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 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114480 111942 0 None - 1 Human 7.1 pIC50 = 7.1 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 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
11848646 104285 0 None - 1 Human 7.1 pIC50 = 7.1 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(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270390 104285 0 None - 1 Human 7.1 pIC50 = 7.1 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(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
23656753 98568 0 None - 1 Human 6.0 pIC50 = 6.0 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 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241117 98568 0 None - 1 Human 6.0 pIC50 = 6.0 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 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11706251 205304 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 by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
CHEMBL577957 205304 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 by scintillation proximity assayAntagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
76325057 111924 0 None - 1 Human 6.0 pIC50 = 6.0 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 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114462 111924 0 None - 1 Human 6.0 pIC50 = 6.0 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 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
45487057 204587 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 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 204587 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 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
46885185 14741 0 None - 1 Human 7.0 pIC50 = 7.0 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 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 14741 0 None - 1 Human 7.0 pIC50 = 7.0 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 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11409395 99124 0 None - 1 Human 7.0 pIC50 = 7.0 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 498 5 4 4 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
CHEMBL2430183 99124 0 None - 1 Human 7.0 pIC50 = 7.0 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 498 5 4 4 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc[nH]2)cc2cn[nH]c12 10.1016/j.bmcl.2013.08.031
11849020 101822 0 None - 1 Human 6.0 pIC50 = 6.0 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 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 101822 0 None - 1 Human 6.0 pIC50 = 6.0 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 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44562983 198166 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 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 198166 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 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
59555258 111947 0 None - 1 Human 7.0 pIC50 = 7.0 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
CHEMBL3114485 111947 0 None - 1 Human 7.0 pIC50 = 7.0 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
59555100 111943 0 None - 1 Human 7.0 pIC50 = 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 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114481 111943 0 None - 1 Human 7.0 pIC50 = 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 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
70693851 80551 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018495 80551 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 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11713729 87325 0 None - 1 Human 6.0 pIC50 = 6 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 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL214845 87325 0 None - 1 Human 6.0 pIC50 = 6 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 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
44403860 147841 0 None 75 2 Human 10.1 pKd = 10.1 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL382469 147841 0 None 75 2 Human 10.1 pKd = 10.1 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
56944164 81863 3 None - 1 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to controlAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to control
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 81863 3 None - 1 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to controlAntagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to control
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44403859 140897 0 None - 1 Human 9.1 pKd = 9.1 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL371646 140897 0 None - 1 Human 9.1 pKd = 9.1 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
44403858 79129 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198502 79129 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
44403855 79249 0 None 354 2 Human 6.9 pKd = 6.9 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 79249 0 None 354 2 Human 6.9 pKd = 6.9 Functional
Antagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cellsAntagonistic activity against calcitonin gene related peptide receptor determined by measuring the formation of cyclic AMP in SK-N-MC cells
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
57404496 80976 0 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023191 80976 0 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
25153832 207732 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
CHEMBL601857 207732 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
25153832 207732 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
CHEMBL601857 207732 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 532 5 1 9 3.5 Cc1ncc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)n1C 10.1016/j.bmcl.2010.01.012
46232565 207590 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccc(Cl)cc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600820 207590 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccc(Cl)cc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152370 207633 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 516 4 1 7 3.6 O=C(Cc1nnc(-c2cc(Cl)cc(Br)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601246 207633 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 516 4 1 7 3.6 O=C(Cc1nnc(-c2cc(Cl)cc(Br)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232822 207817 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602475 207817 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152564 207494 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)ccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600010 207494 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)ccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152563 208236 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 440 4 1 7 2.5 O=C(Cc1nnc(-c2cc(F)cc(F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL604955 208236 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 440 4 1 7 2.5 O=C(Cc1nnc(-c2cc(F)cc(F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25110584 207600 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600837 207600 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25154034 208997 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
CHEMBL609757 208997 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
25152560 207767 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602085 207767 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cc(Cl)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232822 207817 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602475 207817 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 552 8 1 7 4.0 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25151968 209055 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL610062 209055 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232591 207902 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cccc(Cl)c2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL603098 207902 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2cccc(Cl)c2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151777 207729 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601854 207729 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232693 206337 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 565 6 1 9 3.7 O=C(Cc1nnc(-c2cc(-c3ccccc3)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592406 206337 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 565 6 1 9 3.7 O=C(Cc1nnc(-c2cc(-c3ccccc3)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232562 208161 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 404 4 1 7 2.2 O=C(Cc1nnc(-c2ccccc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL604539 208161 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 404 4 1 7 2.2 O=C(Cc1nnc(-c2ccccc2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152169 207599 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 514 5 1 7 4.5 O=C(Cc1nnc(-c2cc(Cl)cc(-c3ccccc3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600836 207599 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 514 5 1 7 4.5 O=C(Cc1nnc(-c2cc(Cl)cc(-c3ccccc3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25154034 208997 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
CHEMBL609757 208997 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 529 5 1 8 4.2 Cc1ccc(-c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)cn1 10.1016/j.bmcl.2010.01.012
25152561 207618 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 456 4 1 7 3.0 O=C(Cc1nnc(-c2cc(F)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601034 207618 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 456 4 1 7 3.0 O=C(Cc1nnc(-c2cc(F)cc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152984 207669 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 540 4 1 7 4.2 O=C(Cc1nnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601455 207669 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 540 4 1 7 4.2 O=C(Cc1nnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152985 207768 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 432 4 1 7 2.8 Cc1cc(C)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL602086 207768 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 432 4 1 7 2.8 Cc1cc(C)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152167 207694 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601639 207694 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232593 207819 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2ccc(Cl)c(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602492 207819 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2ccc(Cl)c(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232527 207765 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 442 5 1 5 3.8 COc1ccc(-c2ccccc2)cc1CC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL602075 207765 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 442 5 1 5 3.8 COc1ccc(-c2ccccc2)cc1CC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151968 209055 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL610062 209055 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 549 6 1 8 4.0 CCN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
70685595 80973 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023188 80973 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasmaAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
25154032 206375 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592649 206375 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152766 207571 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 506 4 1 7 3.9 O=C(Cc1nnc(-c2cc(Cl)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600636 207571 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 506 4 1 7 3.9 O=C(Cc1nnc(-c2cc(Cl)cc(C(F)(F)F)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25151777 207729 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601854 207729 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 535 5 1 8 3.6 CN1CCC(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232564 207568 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2cccc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600620 207568 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2cccc(Cl)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152167 207694 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601639 207694 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 536 5 1 9 2.6 CN1CCN(c2cc(Cl)cc(-c3nnc(CC(=O)N4CCC(n5c(=O)[nH]c6ncccc65)CC4)o3)c2)CC1 10.1016/j.bmcl.2010.01.012
46232777 208361 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL605579 208361 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25152981 207617 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 464 6 1 9 2.2 COc1cc(OC)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL601033 207617 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 464 6 1 9 2.2 COc1cc(OC)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
46232777 208361 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL605579 208361 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 525 8 1 9 2.8 CN(C)CCOc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
46232563 207700 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL601657 207700 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 438 4 1 7 2.8 O=C(Cc1nnc(-c2ccccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25110584 207600 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600837 207600 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 523 5 1 9 2.7 O=C(Cc1nnc(-c2cc(Cl)cc(N3CCOCC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
25152765 208952 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 503 5 1 9 2.3 Cc1cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)cc(N2CCOCC2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL609472 208952 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 503 5 1 9 2.3 Cc1cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)cc(N2CCOCC2)c1 10.1016/j.bmcl.2010.01.012
25152367 208234 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 468 5 1 8 2.8 COc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
CHEMBL604949 208234 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 468 5 1 8 2.8 COc1cc(Cl)cc(-c2nnc(CC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)o2)c1 10.1016/j.bmcl.2010.01.012
25154032 206375 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL592649 206375 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in presence of human serum albumin
ChEMBL 585 7 1 8 4.3 O=C(Cc1nnc(-c2cc(Cl)cc(C3CCN(CC(F)F)CC3)c2)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
46232592 207495 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2c(Cl)cccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012
CHEMBL600011 207495 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albuminAntagonist activity at human recombinant CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-stimulated increase of intracellular cAMP level in absence of human serum albumin
ChEMBL 472 4 1 7 3.5 O=C(Cc1nnc(-c2c(Cl)cccc2Cl)o1)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.01.012




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
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
6918509 83817 41 None 131 2 Human 10.6 pEC50 = 10.6 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL207197 83817 41 None 131 2 Human 10.6 pEC50 = 10.6 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
68857312 118725 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 881 12 5 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL3288288 118725 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 881 12 5 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
86298538 118727 0 None - 0 Human 7.0 pEC50 = 7 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 765 12 4 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL3288290 118727 0 None - 0 Human 7.0 pEC50 = 7 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 765 12 4 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
86298539 118726 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 751 12 4 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL3288289 118726 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassayAntagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
ChEMBL 751 12 4 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
6918509 83817 41 None 131 2 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL207197 83817 41 None 131 2 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.05.118
44403861 78798 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL197529 78798 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
6918509 83817 41 None 131 2 Human 10.5 pIC50 = 10.5 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL207197 83817 41 None 131 2 Human 10.5 pIC50 = 10.5 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL3883526 219195 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]hCGRPa from human recombinant CGRP receptor expressed in CHO cells measured after 90 mins by scintillation counting methodDisplacement of [125I]hCGRPa from human recombinant CGRP receptor expressed in CHO cells measured after 90 mins by scintillation counting method
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)[C@@H](C)O)[C@@H](C)O)[C@H](C)O)[C@@H](C)O)C(=O)NCC(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1016/j.bmc.2016.11.014
CHEMBL2369459 216396 0 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm8007618
44403862 164674 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 879 13 5 10 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL408415 164674 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 879 13 5 10 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
44403861 78798 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL197529 78798 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
57404535 80573 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018517 80573 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
57404496 80976 0 None - 1 Human 10.2 pIC50 = 10.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023191 80976 0 None - 1 Human 10.2 pIC50 = 10.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
10416497 80560 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018504 80560 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
57404529 80974 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 612 6 2 6 5.8 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023189 80974 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 612 6 2 6 5.8 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70683493 80975 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 629 6 2 6 5.6 Cc1cc(CC(OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023190 80975 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 629 6 2 6 5.6 Cc1cc(CC(OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696079 80895 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 618 7 2 6 6.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022606 80895 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 618 7 2 6 6.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696075 80890 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022601 80890 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70687597 80563 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 637 8 2 6 4.9 Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018507 80563 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 637 8 2 6 4.9 Cc1cc(CC(CC(=O)N2CCC(n3cc(-c4ccccc4)[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
70681361 80892 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 604 7 2 6 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022603 80892 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 604 7 2 6 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11308219 80561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018505 80561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
44403860 147841 0 None - 1 Human 9.7 pIC50 = 9.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL382469 147841 0 None - 1 Human 9.7 pIC50 = 9.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
57404534 80575 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018519 80575 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11364682 81167 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024603 81167 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696077 80893 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 590 7 2 6 6.0 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022604 80893 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 590 7 2 6 6.0 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70681362 80898 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 586 6 2 5 6.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(-c3ccccc3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022609 80898 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 586 6 2 5 6.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(-c3ccccc3)n[nH]c12 10.1016/j.bmcl.2012.02.065
70689756 80888 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 587 6 2 6 6.3 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(-c3ccncc3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022599 80888 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 587 6 2 6 6.3 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(-c3ccncc3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11308069 80889 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022600 80889 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685595 80973 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023188 80973 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 612 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70681270 80564 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018508 80564 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
24756690 80559 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018503 80559 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
70691910 80887 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 581 6 2 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022598 80887 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 581 6 2 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685565 80896 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Br)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022607 80896 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Br)n[nH]c12 10.1016/j.bmcl.2012.02.065
11169454 80562 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018506 80562 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11786642 81159 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024595 81159 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685566 80897 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 544 5 2 5 5.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Cl)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022608 80897 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 544 5 2 5 5.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Cl)n[nH]c12 10.1016/j.bmcl.2012.02.065
11295951 81163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024599 81163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11215446 81158 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024594 81158 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369463 216398 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL525571 222431 25 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL525571 222431 25 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11467108 81162 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024598 81162 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369463 216398 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11341642 81153 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024589 81153 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696078 80894 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 606 7 2 7 5.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCOCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022605 80894 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 606 7 2 7 5.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCOCC3)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70696080 80899 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(C=O)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022610 80899 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(C=O)n[nH]c12 10.1016/j.bmcl.2012.02.065
11398863 81161 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024597 81161 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11466363 81157 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024593 81157 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369459 216396 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparationBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11192748 81154 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024590 81154 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70693987 80971 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 609 7 2 7 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCOCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023186 80971 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 609 7 2 7 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCOCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369452 216392 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11191890 81075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024172 81075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1 10.1016/j.bmcl.2012.02.065
44403854 78992 0 None - 0 Human 6.0 pIC50 = 6 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198105 78992 0 None - 0 Human 6.0 pIC50 = 6 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL216229 216100 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL267137 217490 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL267182 217491 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL269027 217553 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL405694 219354 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL409205 219531 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL438008 220521 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL438224 220536 0 None - 0 Human 5.0 pIC50 = 5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403917 79069 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 755 15 4 7 4.2 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198311 79069 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 755 15 4 7 4.2 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL2369454 216393 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70689654 80574 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018518 80574 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 7 2 5 4.9 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2369457 216394 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL2369454 216393 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70696076 80891 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 507 5 2 5 5.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022602 80891 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 507 5 2 5 5.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11785754 81151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
CHEMBL2024587 81151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1 10.1016/j.bmcl.2012.02.065
11215412 81164 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024600 81164 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
70685454 80557 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 700 7 2 5 6.3 O=C(C[C@H](Nc1ccc(Br)c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018501 80557 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 700 7 2 5 6.3 O=C(C[C@H](Nc1ccc(Br)c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL216710 216118 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323097 213292 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 494 7 1 5 6.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Oc3ccccc3)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88441 213292 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 494 7 1 5 6.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Oc3ccccc3)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864453 80470 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018356 80470 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44403853 79195 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 745 17 6 6 4.4 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL198762 79195 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 745 17 6 6 4.4 COc1ccccc1CCNC(=O)N[C@@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N[C@H](CCCCN)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL2369742 216445 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL None None None CC(C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(C)C)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL2369457 216394 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70696851 83285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccncc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059903 83285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccncc1)NC2=O 10.1016/j.bmcl.2012.05.118
58864279 80549 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 574 7 2 7 3.2 O=C(C[C@H](Nc1ccncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018493 80549 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 574 7 2 7 3.2 O=C(C[C@H](Nc1ccncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL376040 219020 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2371143 216794 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCN=C(N)N)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)C(N)=O 10.1021/jm970533r
24756769 80570 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018514 80570 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.02.066
24756612 83280 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 4.8 O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.118
CHEMBL2059898 83280 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 4.8 O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.118
CHEMBL406459 219388 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2369464 216399 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL2369464 216399 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL411804 219737 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
70690619 83277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 599 5 2 5 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)Nc1ccccc12 10.1016/j.bmcl.2012.05.118
CHEMBL2059895 83277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 599 5 2 5 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)Nc1ccccc12 10.1016/j.bmcl.2012.05.118
58901616 80555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018499 80555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
11534977 79038 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 714 17 5 5 4.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL198232 79038 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 714 17 5 5 4.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
11578671 78500 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 714 17 5 5 4.9 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm500364u
CHEMBL196582 78500 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 714 17 5 5 4.9 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm500364u
44323001 112958 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 454 5 1 4 5.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(F)c(Cl)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL313797 112958 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 454 5 1 4 5.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(F)c(Cl)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864479 80554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018498 80554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL267406 217498 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
56675112 70111 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
91930235 70111 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL1794015 70111 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
24756768 80568 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018512 80568 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL3350392 218257 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL2369459 216396 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11226747 81160 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024596 81160 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11387141 81166 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024602 81166 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL3037882 217704 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL3037882 217704 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL2369463 216398 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL525571 222431 25 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL2369459 216396 0 None - 1 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
44403860 147841 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL382469 147841 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
86298538 118727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 765 12 4 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL3288290 118727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 765 12 4 10 3.2 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(n2c(=O)[nH]c3ccccc3c2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
21102037 80567 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018511 80567 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
70694804 83282 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 626 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059900 83282 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 626 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2012.05.118
21102224 83287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 615 5 2 6 5.6 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.05.118
CHEMBL2059905 83287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 615 5 2 6 5.6 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1 10.1016/j.bmcl.2012.05.118
CHEMBL2369464 216399 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
44403855 79249 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 79249 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL429765 220325 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL268539 217536 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL2369465 216400 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70684299 83286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1cccnc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059904 83286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1cccnc1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2369457 216394 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL20034 215886 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70681269 80558 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 622 7 2 5 5.5 O=C(C[C@H](Nc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018502 80558 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 622 7 2 5 5.5 O=C(C[C@H](Nc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44403856 77257 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 828 13 4 9 3.7 COc1ccccc1N1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
CHEMBL194631 77257 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 828 13 4 9 3.7 COc1ccccc1N1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
24756611 83278 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 5.4 O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1 10.1016/j.bmcl.2012.05.118
CHEMBL2059896 83278 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 5.4 O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1 10.1016/j.bmcl.2012.05.118
11249157 81155 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024591 81155 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL404977 219316 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL439085 220599 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2369465 216400 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
86298539 118726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 751 12 4 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
CHEMBL3288289 118726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 751 12 4 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc2ccccc2s1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2014.04.033
44403857 77258 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 827 13 4 8 4.8 COc1ccccc1C1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
CHEMBL194632 77258 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 827 13 4 8 4.8 COc1ccccc1C1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1 10.1021/jm0490641
70693851 80551 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018495 80551 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL407774 219462 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL407854 219467 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864407 80543 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 616 7 2 6 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)Oc1ccccc1 10.1016/j.bmcl.2012.02.066
CHEMBL2018487 80543 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 616 7 2 6 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)Oc1ccccc1 10.1016/j.bmcl.2012.02.066
CHEMBL264010 217381 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70694803 83279 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 4.7 O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 10.1016/j.bmcl.2012.05.118
CHEMBL2059897 83279 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 613 5 2 5 4.7 O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 10.1016/j.bmcl.2012.05.118
CHEMBL2369454 216393 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
25034109 185273 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL466555 185273 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.118
70683458 80886 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 535 5 2 6 5.1 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C#N)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022597 80886 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 535 5 2 6 5.1 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C#N)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
11295168 81156 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024592 81156 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
10438558 80565 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018509 80565 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
21102038 80569 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018513 80569 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
11341430 81165 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
CHEMBL2024601 81165 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1 10.1016/j.bmcl.2012.02.065
11238250 80884 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2022595 80884 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL384581 219110 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL407740 219460 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL440990 220653 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70685453 80550 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018494 80550 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL405767 219357 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL2369465 216400 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70686453 83283 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.05.118
CHEMBL2059901 83283 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.05.118
44323139 213093 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 452 5 1 4 6.2 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc3ccccc23)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL87174 213093 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 452 5 1 4 6.2 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc3ccccc23)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL407401 219439 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
11443894 81074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024171 81074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864296 80545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 683 7 3 5 5.4 O=C(Nc1ccc(Cl)cc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018489 80545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 683 7 3 5 5.4 O=C(Nc1ccc(Cl)cc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL405511 219342 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323338 213316 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.4 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2Cl)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88582 213316 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.4 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2Cl)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
70681261 80469 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 8 3 5 4.5 O=C(C[C@H](NCc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018355 80469 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 625 8 3 5 4.5 O=C(C[C@H](NCc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
70688557 83276 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 6 3 6 4.7 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(C2CCNCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2059881 83276 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 6 3 6 4.7 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(C2CCNCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2369742 216445 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lungIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Centigrade in rabbit lung
ChEMBL None None None CC(C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(C)C)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
70687709 80885 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 568 6 2 7 5.0 COC(=O)c1ccnc(C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c1 10.1016/j.bmcl.2012.02.065
CHEMBL2022596 80885 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 568 6 2 7 5.0 COC(=O)c1ccnc(C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c1 10.1016/j.bmcl.2012.02.065
11156698 81076 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
CHEMBL2024173 81076 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1 10.1016/j.bmcl.2012.02.065
44403859 140897 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL371646 140897 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL404978 219317 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44404069 179553 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 713 17 5 5 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
CHEMBL451246 179553 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 713 17 5 5 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm0490641
44323332 119167 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 447 6 1 6 5.0 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc([N+](=O)[O-])c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL329678 119167 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 447 6 1 6 5.0 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc([N+](=O)[O-])c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL269328 217564 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864477 80472 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 636 7 2 5 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2012.02.066
CHEMBL2018358 80472 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 636 7 2 5 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2012.02.066
44403858 79129 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL198502 79129 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
11693761 121243 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 854 12 4 10 4.1 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL3334623 121243 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 854 12 4 10 4.1 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
58864506 80546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 633 7 3 5 4.2 O=C(Nc1ccccc1F)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018490 80546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 633 7 3 5 4.2 O=C(Nc1ccccc1F)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL262749 217326 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C 10.1021/jm970533r
CHEMBL406587 219393 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
58864520 80471 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 594 7 3 6 3.2 O=C(C[C@H](NC1CCC(O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018357 80471 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 594 7 3 6 3.2 O=C(C[C@H](NC1CCC(O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL262961 217333 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
24756770 80572 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 573 5 2 7 3.6 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC4(CC3)OCCO4)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL2018516 80572 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 573 5 2 7 3.6 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC4(CC3)OCCO4)CC2)O1 10.1016/j.bmcl.2012.02.066
CHEMBL274851 217596 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL411078 219640 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL217867 216162 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O 10.1021/jm970533r
62705051 83288 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 5 3 5 5.1 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 10.1016/j.bmcl.2012.05.118
CHEMBL2059906 83288 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 5 3 5 5.1 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1 10.1016/j.bmcl.2012.05.118
24756767 80566 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018510 80566 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL216101 216097 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403914 172999 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 685 15 5 5 5.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)Nc1ccccc1 10.1021/jm0490641
CHEMBL426646 172999 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against human calcitonin gene related peptide receptor (1 uM) expressed in SK-N-MC cells using [125I]-CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 685 15 5 5 5.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)Nc1ccccc1 10.1021/jm0490641
CHEMBL410450 219600 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323095 113738 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(C(F)(F)F)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL314992 113738 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(C(F)(F)F)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
10433192 170204 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Compound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligandCompound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligand
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL419684 170204 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Compound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligandCompound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligand
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
44403860 147841 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL382469 147841 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 853 12 5 10 4.3 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(O)nc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
58864463 80473 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 596 6 2 6 3.8 CC(C)(C)OC(=O)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018359 80473 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 596 6 2 6 3.8 CC(C)(C)OC(=O)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
10433192 170204 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL419684 170204 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
44403861 78798 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
CHEMBL197529 78798 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 867 12 5 8 4.4 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm0490641
70687746 80970 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023185 80970 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
70695974 80576 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018520 80576 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 643 7 2 5 5.1 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2369458 216395 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70685594 80972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 593 7 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2023187 80972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 593 7 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCC3)n[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2369458 216395 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL265906 217448 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL386824 219175 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL415812 219981 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
11753024 81152 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024588 81152 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864272 80468 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 587 8 2 6 3.4 O=C(C[C@H](NCc1ccccn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018354 80468 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 587 8 2 6 3.4 O=C(C[C@H](NCc1ccccn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL428096 220190 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL266666 217471 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44403855 79249 0 None - 1 Rat 4.2 pIC50 = 4.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
CHEMBL198925 79249 0 None - 1 Rat 4.2 pIC50 = 4.2 Binding
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
ChEMBL 787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1 10.1021/jm0490641
58864421 80553 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
CHEMBL2018497 80553 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12 10.1016/j.bmcl.2012.02.066
44323341 213239 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 446 5 1 6 4.8 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL88111 213239 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 446 5 1 6 4.8 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL2369458 216395 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
11432183 81073 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL2024170 81073 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 508 6 2 4 5.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
58864325 80552 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 648 8 3 10 3.0 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc(N)c1[N+](=O)[O-] 10.1016/j.bmcl.2012.02.066
CHEMBL2018496 80552 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 648 8 3 10 3.0 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc(N)c1[N+](=O)[O-] 10.1016/j.bmcl.2012.02.066
CHEMBL265399 217424 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
CHEMBL410354 219593 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
70686454 83284 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 632 6 2 6 4.9 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(C1CCCCC1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL2059902 83284 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 632 6 2 6 4.9 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(C1CCCCC1)NC2=O 10.1016/j.bmcl.2012.05.118
CHEMBL275984 217603 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
70692761 83281 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 5 2 6 4.7 CN1c2ccccc2C(=O)NC12CCN(C(=O)N[C@H](Cc1csc3ccccc13)C(=O)N1CCC(N3CCCCC3)CC1)CC2 10.1016/j.bmcl.2012.05.118
CHEMBL2059899 83281 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 628 5 2 6 4.7 CN1c2ccccc2C(=O)NC12CCN(C(=O)N[C@H](Cc1csc3ccccc13)C(=O)N1CCC(N3CCCCC3)CC1)CC2 10.1016/j.bmcl.2012.05.118
10483468 80571 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018515 80571 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
70695973 80556 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 623 7 2 6 4.9 O=C(C[C@H](Nc1cccc2ncccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018500 80556 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 623 7 2 6 4.9 O=C(C[C@H](Nc1cccc2ncccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2369452 216392 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membraneBinding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
CHEMBL2369452 216392 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig vas deferens membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm00090a003
70694802 83275 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL2059880 83275 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.118
CHEMBL407697 219458 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL2371144 216795 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm970533r
CHEMBL269517 217573 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
ChEMBL None None None None 10.1021/jm970533r
44323110 113926 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 402 5 1 4 5.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccccc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL316211 113926 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 402 5 1 4 5.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccccc2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
58864368 80544 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 683 7 3 5 5.4 O=C(Nc1cccc(Cl)c1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018488 80544 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 683 7 3 5 5.4 O=C(Nc1cccc(Cl)c1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.02.066
58864250 80548 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
CHEMBL2018492 80548 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation countingDisplacement of [125]CGRP from human CGRP receptor expressed in human SK-N-MC cell membrane after 2 hrs by scintillation counting
ChEMBL 608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.02.066
44323180 213405 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc(C(F)(F)F)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
CHEMBL89148 213405 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranesDisplacement of [125I]hCGRP human Calcitonin gene-related peptide type receptor expressed in SK-N-MC neuroblastoma cell membranes
ChEMBL 470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc(C(F)(F)F)c2)nc2ccc(OC)cc12 10.1016/S0960-894X(97)10046-4
56675112 70111 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
91930235 70111 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
CHEMBL1794015 70111 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+iIn vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit porcine c+i
ChEMBL 3187 105 47 49 -19.7 CC(C)C[C@H](NC(=O)COCCOCCNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1016/0960-894X(95)00078-8
6918509 83817 41 None 131 2 Human 10.4 pKd = 10.4 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL207197 83817 41 None 131 2 Human 10.4 pKd = 10.4 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
6918509 83817 41 None 131 2 Human 10.1 pKd = 10.1 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteries
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL207197 83817 41 None 131 2 Human 10.1 pKd = 10.1 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human cerebral arteries
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
11319053 95928 51 None - 1 Human 8.7 pKd = 8.7 Binding
Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compoundReversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 95928 51 None - 1 Human 8.7 pKd = 8.7 Binding
Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compoundReversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 95928 51 None - 1 Human 8.4 pKd = 8.4 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 95928 51 None - 1 Human 8.4 pKd = 8.4 Binding
Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteriesAntagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
6918509 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.04.012
CHEMBL207197 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.04.012
6918509 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/ml300021s
CHEMBL207197 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/ml300021s
6918509 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL207197 83817 41 None 131 2 Human 11.0 pKi = 11 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2013.12.089
11467753 180975 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 626 6 3 5 4.5 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1021/jm800546t
CHEMBL454791 180975 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 626 6 3 5 4.5 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1021/jm800546t
10394458 94448 0 None - 1 Human 11.0 pKi = 11.0 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 646 6 3 5 4.8 O=C(NC(Cc1cc(Cl)c2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336422 94448 0 None - 1 Human 11.0 pKi = 11.0 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 646 6 3 5 4.8 O=C(NC(Cc1cc(Cl)c2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
10077700 94450 0 None - 1 Human 10.9 pKi = 10.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336424 94450 0 None - 1 Human 10.9 pKi = 10.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
44593666 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1021/jm800546t
CHEMBL450668 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1021/jm800546t
44593666 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
CHEMBL450668 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
44593666 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL450668 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
44593666 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
CHEMBL450668 179509 7 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
ChEMBL 644 6 3 5 4.6 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2012.02.065
6918509 83817 41 None 131 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL207197 83817 41 None 131 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
6918509 83817 41 None 131 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.04.105
CHEMBL207197 83817 41 None 131 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.04.105
164614302 192121 0 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 646 5 2 5 4.5 CCn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4859941 192121 0 None - 1 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 646 5 2 5 4.5 CCn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
71569533 94438 0 None - 1 Human 10.8 pKi = 10.8 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 627 6 3 6 3.9 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2nn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336411 94438 0 None - 1 Human 10.8 pKi = 10.8 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 627 6 3 6 3.9 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2nn[nH]c12 10.1016/j.bmcl.2013.01.011
164618286 191324 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 632 4 2 5 4.1 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4848032 191324 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 632 4 2 5 4.1 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
73356952 99254 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 586 4 2 6 3.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431249 99254 0 None - 1 Human 10.8 pKi = 10.8 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 586 4 2 6 3.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
44469664 99251 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 567 2 1 5 4.1 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431246 99251 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 567 2 1 5 4.1 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
164617750 191349 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 618 4 3 4 4.0 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)[nH]c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4848486 191349 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 618 4 3 4 4.0 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)[nH]c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
59555187 111957 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114495 111957 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 692 8 1 6 6.2 CC(C)N1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
164614208 191983 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4857649 191983 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 700 5 2 5 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
25019940 74724 33 None 478 2 Human 10.7 pKi = 10.7 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2013.04.012
CHEMBL1910936 74724 33 None 478 2 Human 10.7 pKi = 10.7 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2013.04.012
25019940 74724 33 None 478 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
CHEMBL1910936 74724 33 None 478 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
44469946 99258 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 569 4 1 5 4.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431253 99258 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 569 4 1 5 4.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
57977594 99261 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 2 5 3.6 CN1C[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
CHEMBL2431256 99261 0 None - 1 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 2 5 3.6 CN1C[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
11377534 94443 0 None - 1 Human 10.6 pKi = 10.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc(Br)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336416 94443 0 None - 1 Human 10.6 pKi = 10.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc(Br)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
53472683 97831 11 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
CHEMBL2397415 97831 11 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
DB15688 97831 11 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 638 6 3 6 3.5 Cc1cc(C[C@@H](NC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCN(C3CCN(C)CC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.04.012
46885183 15110 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092882 15110 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
164628650 193138 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 673 5 2 7 3.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4875327 193138 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 673 5 2 7 3.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)n(CC(F)(F)F)c3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
51049968 89335 47 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
CHEMBL2178422 89335 47 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
DB12457 89335 47 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
CHEMBL2369459 216396 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C 10.1021/jm8007618
76321477 111982 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114676 111982 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
71569375 94445 0 None - 1 Human 10.5 pKi = 10.5 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 660 6 3 5 5.1 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c(Cl)c2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336418 94445 0 None - 1 Human 10.5 pKi = 10.5 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 660 6 3 5 5.1 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c(Cl)c2cn[nH]c12 10.1016/j.bmcl.2013.01.011
25019993 99259 1 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 3 5 3.2 CC1(C)NC[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
CHEMBL2431254 99259 1 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 3 5 3.2 CC1(C)NC[C@@H](c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
45485692 205779 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
CHEMBL585568 205779 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 2 4 4.7 CC1(C)CC[C@@H](c2c(F)cccc2F)N(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2009.07.134
54581910 68290 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
CHEMBL1770729 68290 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1 10.1016/j.bmcl.2010.12.054
52940673 24935 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269644 24935 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
11204595 94444 0 None - 1 Human 10.4 pKi = 10.4 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc(Cl)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336417 94444 0 None - 1 Human 10.4 pKi = 10.4 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc(Cl)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
54586725 68289 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770728 68289 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 608 6 2 7 6.1 CCC(CC)(OC)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
25181509 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL512773 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
54585731 68276 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770715 68276 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 579 5 2 7 4.7 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
57977652 81861 0 None 85 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
CHEMBL2035981 81861 0 None 85 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/ml400199p
25181509 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL512773 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
25181509 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL512773 196144 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
44631920 132617 0 None - 1 Human 10.4 pKi = 10.4 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 534 7 1 4 5.3 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CF nan
CHEMBL3648345 132617 0 None - 1 Human 10.4 pKi = 10.4 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 534 7 1 4 5.3 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CF nan
164627356 193064 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 633 4 2 6 3.5 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ncccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4874157 193064 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 633 4 2 6 3.5 Cn1c(=O)[nH]c2c(Cl)cc3c(c21)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ncccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
44470090 99256 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 5 1 5 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431251 99256 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 571 5 1 5 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
50939479 99253 1 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431248 99253 1 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 585 4 2 5 4.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
17751102 186718 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4746351 186718 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
58864297 94446 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.0 CCc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2c(C)n[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336419 94446 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.0 CCc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2c(C)n[nH]c12 10.1016/j.bmcl.2013.01.011
54580850 68285 1 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770724 68285 1 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 580 4 2 7 5.3 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
54583843 68287 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770726 68287 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 594 5 2 7 5.7 CCOC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
58379673 111095 0 None - 1 Human 10.3 pKi = 10.3 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 568 6 1 4 5.7 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C1(C(F)(F)F)CC1 nan
CHEMBL3099925 111095 0 None - 1 Human 10.3 pKi = 10.3 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 568 6 1 4 5.7 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C1(C(F)(F)F)CC1 nan
56944164 81863 3 None 194 4 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 81863 3 None 194 4 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
11388586 94442 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 755 6 3 6 4.3 O=C(N[C@H](Cc1cc(I)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336415 94442 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 755 6 3 6 4.3 O=C(N[C@H](Cc1cc(I)c2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
50939608 99252 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 559 4 2 5 3.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
CHEMBL2431247 99252 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 559 4 2 5 3.8 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C1(C)C 10.1021/ml400199p
44631936 131957 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 557 3 1 5 5.0 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCc3ccccc32)C1=O nan
CHEMBL3645137 131957 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 557 3 1 5 5.0 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCc3ccccc32)C1=O nan
164619429 192849 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 599 4 2 6 4.0 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4871223 192849 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 599 4 2 6 4.0 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
164627588 193079 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 4 5.2 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4874451 193079 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 4 5.2 N#Cc1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(N2CCc4ccccc4NC2=O)CC1)C3 10.1016/j.bmcl.2021.128077
46179077 131963 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 593 3 1 5 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(=O)C12CCCC2 nan
CHEMBL3645143 131963 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 593 3 1 5 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(=O)C12CCCC2 nan
58379669 132616 0 None - 1 Human 10.2 pKi = 10.2 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 550 7 1 4 5.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CCl nan
CHEMBL3648344 132616 0 None - 1 Human 10.2 pKi = 10.2 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 550 7 1 4 5.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21)C(=O)C(C)(C)CCl nan
51357856 89333 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 560 4 1 7 5.8 [N-]=[N+]=N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
CHEMBL2178420 89333 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 560 4 1 7 5.8 [N-]=[N+]=N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F 10.1021/jm3013147
164620407 193006 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 653 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4873378 193006 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 653 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
46174937 83356 7 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
CHEMBL2063115 83356 7 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
11706981 68281 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770720 68281 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 3 2 6 5.5 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)cnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
59555031 111956 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114494 111956 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
57404496 80976 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1021/ml300021s
CHEMBL2023191 80976 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 602 6 2 8 4.4 Cc1cc(CC(OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c2cc(C(=O)N(C)C)cc(Cl)n2)cc2cn[nH]c12 10.1021/ml300021s
46885299 14980 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092208 14980 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
51357585 89337 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178424 89337 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
23658217 186716 0 None - 1 Human 10.1 pKi = 10.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 575 4 2 6 3.6 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4746329 186716 0 None - 1 Human 10.1 pKi = 10.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 575 4 2 6 3.6 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2020.127624
44468576 99257 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 568 4 1 4 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431252 99257 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 568 4 1 4 5.4 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(C/C=C/c2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
17751102 186718 0 None - 1 Human 10.0 pKi = 10 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4746351 186718 0 None - 1 Human 10.0 pKi = 10 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
59554856 111958 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114496 111958 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
52940932 25025 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 504 4 1 4 5.8 C[C@H](c1ccccc1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
CHEMBL1270291 25025 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 504 4 1 4 5.8 C[C@H](c1ccccc1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
44469523 99096 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 2 1 4 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2429882 99096 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 2 1 4 4.7 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CC#Cc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
69747490 99260 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 3 5 3.4 CC1(C)NC[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
CHEMBL2431255 99260 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 545 4 3 5 3.4 CC1(C)NC[C@@](C)(c2cc(F)cc(F)c2)N(CC(=O)Nc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C1=O 10.1021/ml400199p
52941862 24936 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1ccc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269645 24936 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 4 1 4 5.7 CC(C)(C)C(=O)N(Cc1ccc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
164625304 192984 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 619 4 2 5 4.3 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)oc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4873084 192984 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 619 4 2 5 4.3 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]c(=O)oc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
52942173 25041 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 540 4 1 4 6.0 C[C@H](c1cc(F)cc(F)c1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
CHEMBL1270391 25041 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 540 4 1 4 6.0 C[C@H](c1cc(F)cc(F)c1)N(Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C(=O)C(C)(C)C 10.1016/j.bmcl.2010.08.105
45267476 203063 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL562069 203063 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46885244 14565 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089433 14565 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2010.02.086
164612132 191437 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 6 3.7 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4849710 191437 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 626 4 2 6 3.7 O=C(C[C@@H]1Cc2cc(Cl)c3c(c2CN(CC(F)(F)F)C1=O)C(F)(F)C(=O)N3)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2021.128077
45485605 204433 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
CHEMBL570933 204433 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O 10.1016/j.bmcl.2009.07.134
58379682 111094 0 None - 1 Human 9.9 pKi = 9.9 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 512 5 1 4 5.6 Cc1ccc([C@@H](C)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C(C)(C)C)cc1F nan
CHEMBL3099923 111094 0 None - 1 Human 9.9 pKi = 9.9 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 512 5 1 4 5.6 Cc1ccc([C@@H](C)N(C/C=C/c2cnc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C(C)(C)C)cc1F nan
46178994 131959 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 565 3 2 5 4.9 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CNC12CCCC2 nan
CHEMBL3645139 131959 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 565 3 2 5 4.9 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CNC12CCCC2 nan
11354531 94439 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Br)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336412 94439 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 707 6 3 6 4.5 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Br)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
54580803 68258 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770557 68258 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54581909 68284 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770723 68284 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
52944286 24937 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 1 5 5.1 CC(C)(C)C(=O)N(Cc1cnc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1269646 24937 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 531 4 1 5 5.1 CC(C)(C)C(=O)N(Cc1cnc2nc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21)C[C@@H]1CCc2ccccc21 10.1016/j.bmcl.2010.08.105
54583844 68288 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770727 68288 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 648 5 2 7 6.3 CC(C)(OCC(F)(F)F)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
164609291 191239 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]cnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4846749 191239 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 602 4 2 4 4.8 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]cnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
54583842 68283 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
CHEMBL1770722 68283 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 591 3 2 7 4.9 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)Cn4c(CC(F)(F)F)nnc43)CC2)O1 10.1016/j.bmcl.2010.12.054
23656921 96997 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238276 96997 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 596 6 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCOC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44570616 196993 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL517467 196993 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 538 5 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
46182711 133760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655571 133760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11158071 94447 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.3 CC(C)c1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336420 94447 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 7 3 5 5.3 CC(C)c1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
11977527 186349 0 None - 1 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 588 4 2 4 4.7 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4741882 186349 0 None - 1 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 588 4 2 4 4.7 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
24863333 180959 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL454751 180959 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
44593545 185233 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 185233 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
46905052 17190 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
CHEMBL1162991 17190 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2009.06.057
45485687 204362 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 4 3.6 C[C@H](c1cc(F)cc(F)c1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL570474 204362 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 4 3.6 C[C@H](c1cc(F)cc(F)c1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
24863333 180959 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
CHEMBL454751 180959 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 612 6 3 5 4.2 O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
24863332 83253 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 629 6 3 6 3.7 O=C(N[C@H](Cc1ccc2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059853 83253 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 629 6 3 6 3.7 O=C(N[C@H](Cc1ccc2[nH]c(=O)oc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
46179076 131962 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 531 4 1 5 4.7 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(C)(c2ccccc2)C1=O nan
CHEMBL3645142 131962 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 531 4 1 5 4.7 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(C)(c2ccccc2)C1=O nan
11445240 94440 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Cl)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
CHEMBL2336413 94440 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 663 6 3 6 4.4 O=C(N[C@H](Cc1cc2oc(=O)[nH]c2cc1Cl)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.01.011
45267481 203441 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
CHEMBL564487 203441 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2 10.1016/j.bmcl.2009.06.057
54587762 68286 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770725 68286 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 3 3 7 4.7 CC(C)(O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
23654987 121244 8 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 633 6 2 7 3.9 Cc1cc(C[C@@H](OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCOCC3)CC2)cc(C)c1O 10.1021/jm500364u
CHEMBL3334624 121244 8 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
ChEMBL 633 6 2 7 3.9 Cc1cc(C[C@@H](OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCOCC3)CC2)cc(C)c1O 10.1021/jm500364u
11364735 96484 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237662 96484 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
46178835 25055 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 538 3 1 4 5.8 CC1(C)CC[C@@H](c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2010.08.105
CHEMBL1270484 25055 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 538 3 1 4 5.8 CC1(C)CC[C@@H](c2cc(F)cc(F)c2)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1=O 10.1016/j.bmcl.2010.08.105
46885135 14808 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090848 14808 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11979131 187439 0 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 594 4 2 4 5.3 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755081 187439 0 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 594 4 2 4 5.3 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46178992 131958 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 523 3 1 5 4.9 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCCCC2)C1=O nan
CHEMBL3645138 131958 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 523 3 1 5 4.9 CC(C)N1C(=O)N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C2(CCCCCC2)C1=O nan
23582940 203381 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 203381 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
54580838 68275 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770714 68275 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
54586710 68280 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770719 68280 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 4 2 6 4.8 COC(C)(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
164626848 193279 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 617 5 3 6 3.3 NC(=O)c1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
CHEMBL4877386 193279 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 617 5 3 6 3.3 NC(=O)c1c[nH]c2c(Cl)cc3c(c12)CN(CC(F)(F)F)C(=O)[C@H](CC(=O)N1CCC(n2c(=O)[nH]c4ncccc42)CC1)C3 10.1016/j.bmcl.2021.128077
11979011 187484 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 576 4 2 4 5.2 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755588 187484 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 576 4 2 4 5.2 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46885185 14741 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1090515 14741 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2010.02.086
58379670 132618 0 None - 1 Human 9.4 pKi = 9.4 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 495 5 1 3 4.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C nan
CHEMBL3648346 132618 0 None - 1 Human 9.4 pKi = 9.4 Binding
Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.Native Receptor Binding Assay: Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.
ChEMBL 495 5 1 3 4.6 C[C@H](c1cc(F)cc(F)c1)N(C/C=C/c1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C nan
164612882 191683 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 603 4 2 5 4.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]nnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4853137 191683 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 603 4 2 5 4.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]nnc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
54584803 68282 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770721 68282 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
46179163 131964 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
CHEMBL3645144 131964 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
44468711 99255 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 570 5 1 4 5.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
CHEMBL2431250 99255 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 570 5 1 4 5.3 CN1C[C@@](C)(c2cc(F)cc(F)c2)N(CCCc2ccc3c(c2)C[C@@]2(C3)C(=O)Nc3ncccc32)C(=O)C12CCCC2 10.1021/ml400199p
23657089 153758 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392634 153758 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11192602 153763 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392636 153763 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
59554895 111952 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114490 111952 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44593545 185233 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
CHEMBL466192 185233 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 3 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2 10.1016/j.bmcl.2008.10.106
25227362 180512 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL453643 180512 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2008.10.019
25227362 180512 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL453643 180512 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2 10.1016/j.bmcl.2010.02.086
46885243 15100 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1092838 15100 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11977643 187425 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 585 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3ccccc3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4754995 187425 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 585 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3ccccc3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
24863323 83273 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 613 6 3 6 3.6 O=C(N[C@H](Cc1ccc2[nH]nnc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059878 83273 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 613 6 3 6 3.6 O=C(N[C@H](Cc1ccc2[nH]nnc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
70694802 83275 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059880 83275 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 614 6 2 6 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
45485640 204169 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 498 5 2 4 3.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL569340 204169 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 498 5 2 4 3.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
46885242 15099 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
CHEMBL1092837 15099 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1 10.1016/j.bmcl.2010.02.086
25034109 185273 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
CHEMBL466555 185273 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cellsDisplacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
ChEMBL 628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1021/jm800546t
54587752 68277 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770716 68277 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 574 3 2 5 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
44570579 197610 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL518422 197610 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
54581897 68279 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770718 68279 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
11520007 68278 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
CHEMBL1770717 68278 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 600 3 2 5 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3(C(F)(F)F)CC3)cnc21)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2010.12.054
70690615 83234 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 730 6 3 6 5.0 O=C(N[C@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059794 83234 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 730 6 3 6 5.0 O=C(N[C@H](Cc1cc(Br)c(O)c(Br)c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
24863334 83272 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 627 6 3 5 3.8 O=C1Cc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2N1 10.1016/j.bmcl.2012.05.074
CHEMBL2059877 83272 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 627 6 3 5 3.8 O=C1Cc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2N1 10.1016/j.bmcl.2012.05.074
51357855 89334 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178421 89334 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@H](c2cccc(F)c2F)[C@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
11606400 68269 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770568 68269 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 549 4 2 6 5.0 CC(C)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
52943413 25010 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 526 4 1 4 5.5 CC(C)(C)C(=O)N(Cc1cc(F)cc(F)c1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1270197 25010 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 526 4 1 4 5.5 CC(C)(C)C(=O)N(Cc1cc(F)cc(F)c1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
11432931 168691 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL415263 168691 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
11979133 186233 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 573 4 2 4 5.4 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4740622 186233 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 573 4 2 4 5.4 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2013.04.012
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2013.04.012
46178995 131960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 564 3 1 4 6.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCC12CCCC2 nan
CHEMBL3645140 131960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 564 3 1 4 6.3 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCC12CCCC2 nan
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human CGRP receptorBinding affinity to human CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm500364u
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/ml400199p
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cellsDisplacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/ml400199p
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1021/jm070668p
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.09.066
11319053 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
CHEMBL236593 95928 51 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 566 4 2 6 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncccc32)CC1 10.1016/j.bmcl.2009.06.057
45485677 205613 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL583679 205613 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
164626466 193072 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 601 4 2 3 5.4 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ccc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
CHEMBL4874351 193072 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysisDisplacement of [125I]CGRP from human CGRP receptor in human SK-N-MC cells measured after 2 hrs by scintillation counting analysis
ChEMBL 601 4 2 3 5.4 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ccc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2021.128077
44570614 184380 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464078 184380 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
46179164 131965 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2ccc3nc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
CHEMBL3645145 131965 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 579 3 2 5 5.3 O=C1N(Cc2ccc3nc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)[C@H](c2cc(F)cc(F)c2)CCNC12CCCC2 nan
11284233 96662 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237849 96662 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 548 5 2 5 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11387595 153760 1 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392635 153760 1 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 575 5 2 6 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(Cc2ccccn2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555048 111948 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114486 111948 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11628603 188499 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 597 4 3 4 4.9 O=C(N[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4777037 188499 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 597 4 3 4 4.9 O=C(N[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
54582783 68257 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770556 68257 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 548 4 2 7 4.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(C3CC3)nnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59554993 111951 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114489 111951 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
59555066 111955 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114493 111955 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
76332330 111983 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114677 111983 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 706 7 1 6 6.6 CC(C)(C)CCN1C(=O)[C@H](CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)S[C@H]1c1cccc(F)c1N1CCN(C(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
11541560 68267 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770566 68267 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11721278 68268 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770567 68268 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11512928 148449 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
CHEMBL385454 148449 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1 10.1016/j.bmcl.2006.07.044
11692628 204404 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL570746 204404 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 567 3 2 5 4.3 O=C1Nc2ncccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
45271754 201833 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL549503 201833 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570580 184226 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL463880 184226 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
45485646 204552 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 514 5 2 4 3.5 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571797 204552 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 514 5 2 4 3.5 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(F)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
23582940 203381 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564088 203381 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
46179074 131961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 547 3 1 5 5.4 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(c2ccccc2Cl)=NC12CCCC2 nan
CHEMBL3645141 131961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 547 3 1 5 5.4 O=C1N(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C(c2ccccc2Cl)=NC12CCCC2 nan
52947106 24992 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 490 4 1 4 5.2 CC(C)(C)C(=O)N(Cc1ccccc1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
CHEMBL1270088 24992 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 490 4 1 4 5.2 CC(C)(C)C(=O)N(Cc1ccccc1)Cc1cnc2cc3c(cc2c1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.08.105
46885245 14619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089772 14619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2 10.1016/j.bmcl.2010.02.086
11753021 96485 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237663 96485 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11752904 154129 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL392937 154129 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 530 5 2 5 3.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCF)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
45271740 203325 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
CHEMBL563727 203325 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23 10.1016/j.bmcl.2009.06.057
46885134 14807 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
CHEMBL1090847 14807 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21 10.1016/j.bmcl.2010.02.086
11979010 190229 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 577 3 3 4 4.7 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4798946 190229 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 577 3 3 4 4.7 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
46885186 14805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090841 14805 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2 10.1016/j.bmcl.2010.02.086
45485645 204522 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571580 204522 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(F)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45254467 133761 0 None - 1 Human 8.8 pKi = 8.8 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 597 5 3 5 4.0 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655572 133761 0 None - 1 Human 8.8 pKi = 8.8 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 597 5 3 5 4.0 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11180666 153872 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL392730 153872 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
44570615 184381 9 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL464079 184381 9 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
44593445 198308 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
CHEMBL519421 198308 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.106
44593445 198308 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
CHEMBL519421 198308 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 5 2 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)N(C)C 10.1016/j.bmcl.2008.10.019
11584808 204467 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
CHEMBL571203 204467 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 551 3 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)C(=O)Nc1ncccc12 10.1016/j.bmcl.2009.09.066
45485664 204117 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 496 5 2 4 3.4 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL568920 204117 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 496 5 2 4 3.4 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45485625 204558 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL571823 204558 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2010.08.105
45485625 204558 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571823 204558 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44563052 192814 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
CHEMBL487068 192814 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 3 7 0.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(N)=O 10.1016/j.bmcl.2008.10.019
25019940 74724 33 None -478 2 Rat 8.0 pKi = 8 Binding
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/jm500364u
CHEMBL1910936 74724 33 None -478 2 Rat 8.0 pKi = 8 Binding
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1021/jm500364u
59555258 111947 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114485 111947 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
25019940 74724 33 None -478 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL1910936 74724 33 None -478 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 557 4 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44420250 143706 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374251 143706 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11432505 204412 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570793 204412 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 527 4 2 4 3.3 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccn[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
44562938 185873 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471705 185873 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45487023 205598 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 526 4 2 3 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccc[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL583547 205598 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 526 4 2 3 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2ccc[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
44416442 87352 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 593 4 2 7 3.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214950 87352 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 593 4 2 7 3.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2006.07.044
44420286 91030 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221160 91030 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44417049 175598 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL437718 175598 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11848968 101980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255967 101980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11570753 176346 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3cccnc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL443577 176346 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3cccnc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44420290 91402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL222198 91402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44416513 148660 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 619 5 3 7 4.0 NC(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386714 148660 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 619 5 3 7 4.0 NC(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
71569532 94441 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 6 3 7 3.6 N#Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2oc(=O)[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336414 94441 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 654 6 3 7 3.6 N#Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2oc(=O)[nH]c12 10.1016/j.bmcl.2013.01.011
11168000 160962 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398575 160962 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11628731 87168 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214507 87168 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44416912 87632 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215274 87632 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11707040 87853 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215499 87853 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 602 5 2 6 5.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
11519899 148265 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL384408 148265 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 584 5 2 8 3.5 COC(=O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
23656751 98516 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 3 3 5 2.4 Cc1ccc(C2CC[C@@H](NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)C(=O)NC2)cc1 10.1021/jm070668p
CHEMBL240903 98516 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 3 3 5 2.4 Cc1ccc(C2CC[C@@H](NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)C(=O)NC2)cc1 10.1021/jm070668p
11549001 148657 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386701 148657 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
59554867 111987 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114681 111987 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
59555008 111933 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114471 111933 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F 10.1016/j.bmcl.2013.12.089
11978769 189153 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 563 4 3 4 4.2 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785088 189153 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 563 4 3 4 4.2 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
52945887 24991 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)[C@]12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1270087 24991 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)[C@]12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
44420256 91722 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223756 91722 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44563026 193422 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL488065 193422 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
59555056 111922 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114460 111922 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11713849 205668 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 564 3 2 3 4.6 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)Cc1ccccc1NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL584311 205668 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 564 3 2 3 4.6 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)Cc1ccccc1NC2=O 10.1016/j.bmcl.2009.09.066
70685988 81865 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 606 4 3 6 4.0 C[C@@]1(c2cc(F)c(Cl)c(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035985 81865 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 606 4 3 6 4.0 C[C@@]1(c2cc(F)c(Cl)c(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44570499 199175 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL520778 199175 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44562897 185845 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471530 185845 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563126 195712 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL508016 195712 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44570461 186025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2cccnc2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL472829 186025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2cccnc2)NC1=O 10.1016/j.bmcl.2008.10.106
45254662 133758 0 None - 1 Human 6.9 pKi = 6.9 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cccnc2)NC1=O nan
CHEMBL3655569 133758 0 None - 1 Human 6.9 pKi = 6.9 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cccnc2)NC1=O nan
25119464 189323 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 529 4 3 4 3.7 CC(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4787479 189323 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 529 4 3 4 3.7 CC(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
59555055 111953 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114491 111953 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2cc(F)ccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59554934 111954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114492 111954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
45485631 204492 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccccc3F)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL571350 204492 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccccc3F)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44455457 101985 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255998 101985 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487059 204466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 502 3 2 3 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CCNC2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL571185 204466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 502 3 2 3 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CCNC2=O)CC1 10.1016/j.bmcl.2009.09.066
70690614 83233 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 2 6 3.8 COc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059793 83233 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 2 6 3.8 COc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
44416437 148572 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386204 148572 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2006.07.044
44420245 90779 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
CHEMBL220715 90779 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1 10.1016/j.bmcl.2006.09.045
44562939 185874 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL471706 185874 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563025 199274 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL520905 199274 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
44455043 102501 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258329 102501 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11444589 86564 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL211931 86564 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1 10.1016/j.bmcl.2006.07.044
70690616 83242 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 611 6 2 6 4.3 Cn1cc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.074
CHEMBL2059802 83242 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 611 6 2 6 4.3 Cn1cc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.074
44570498 190819 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL482178 190819 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
45254661 133759 0 None - 1 Human 6.8 pKi = 6.8 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccncc2)NC1=O nan
CHEMBL3655570 133759 0 None - 1 Human 6.8 pKi = 6.8 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccncc2)NC1=O nan
44455041 177376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL445069 177376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
56944164 81863 3 None -194 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 81863 3 None -194 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
11849025 102260 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL257252 102260 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 548 4 2 6 4.3 O=C(Nc1cc(-c2cccc(F)c2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44420261 144061 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375224 144061 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46885132 14943 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 490 3 1 7 2.8 CN1C(=O)NC(=O)[C@]12Cc1cc3ccc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1091903 14943 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 490 3 1 7 2.8 CN1C(=O)NC(=O)[C@]12Cc1cc3ccc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11977970 187811 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 544 5 3 5 2.6 CN(C)CCN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4759318 187811 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 544 5 3 5 2.6 CN(C)CCN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11848963 162213 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL403765 162213 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
23656750 98505 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 478 4 3 6 2.1 COc1ccccc1C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240902 98505 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 478 4 3 6 2.1 COc1ccccc1C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11848753 165677 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 522 4 2 8 2.4 Cn1cc(-c2ccc(S(C)(=O)=O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL409535 165677 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 522 4 2 8 2.4 Cn1cc(-c2ccc(S(C)(=O)=O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59554936 111939 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114477 111939 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1 10.1016/j.bmcl.2013.12.089
70685987 81864 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 592 4 3 6 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)c(Cl)c(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035984 81864 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 592 4 3 6 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)c(Cl)c(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44562982 192820 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487076 192820 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2 10.1016/j.bmcl.2008.10.019
59554947 111949 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114487 111949 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
16745090 14539 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 491 3 1 8 2.2 CN1C(=O)NC(=O)C12Cc1cc3ncc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089207 14539 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 491 3 1 8 2.2 CN1C(=O)NC(=O)C12Cc1cc3ncc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
59554857 111920 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114458 111920 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11571094 148668 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386757 148668 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
56944164 81863 3 None -218 4 Mouse 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from mouse CGRP receptorDisplacement of [125I]CGRP from mouse CGRP receptor
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035983 81863 3 None -218 4 Mouse 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from mouse CGRP receptorDisplacement of [125I]CGRP from mouse CGRP receptor
ChEMBL 572 4 3 6 3.3 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
70686451 83236 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 615 7 3 6 3.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059797 83236 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 615 7 3 6 3.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
11848798 102444 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 446 3 2 8 1.7 Cn1cc(-c2ncccn2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258069 102444 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 446 3 2 8 1.7 Cn1cc(-c2ncccn2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555157 111936 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114474 111936 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1 10.1016/j.bmcl.2013.12.089
24853164 111938 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114476 111938 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555074 111946 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114484 111946 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 632 7 1 6 5.2 CN1CCN(c2ccccc2[C@H]2S[C@@H](CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
59555331 111950 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114488 111950 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
44563050 193426 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488082 193426 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 505 5 2 8 1.3 COC(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
52949562 24971 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3ccc(CN(Cc4ccccc4)C(=O)C(C)(C)C)nc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1269977 24971 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3ccc(CN(Cc4ccccc4)C(=O)C(C)(C)C)nc3cc1C2 10.1016/j.bmcl.2010.08.105
54581838 68263 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770562 68263 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
44563200 181269 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL455458 181269 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 502 3 2 7 1.2 CN1C(=O)CCCn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
45269221 203436 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
CHEMBL564466 203436 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2009.06.057
44570578 185189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL465934 185189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
11375693 96661 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237848 96661 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
54583774 68264 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770563 68264 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CO)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
70688552 83231 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 574 6 3 6 3.5 O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059790 83231 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 574 6 3 6 3.5 O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
11225752 96486 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL237664 96486 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
44563028 201345 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
CHEMBL530116 201345 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 447 3 2 6 1.6 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2C 10.1016/j.bmcl.2008.10.019
54583775 68266 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770565 68266 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59555100 111943 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114481 111943 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1ccncc1 10.1016/j.bmcl.2013.12.089
44420240 90250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL220101 90250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420235 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL223156 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
44420240 90250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220101 90250 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420235 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL223156 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
11505361 148266 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccn3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384409 148266 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccn3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11678456 86995 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 556 5 3 7 3.2 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(CO)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213717 86995 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 556 5 3 7 3.2 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(CO)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44416516 87865 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2nc(O)n(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c12 10.1016/j.bmcl.2006.07.044
CHEMBL215549 87865 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2nc(O)n(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c12 10.1016/j.bmcl.2006.07.044
59555245 111931 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114469 111931 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
59555102 111986 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114680 111986 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11650307 87293 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL214800 87293 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
11849024 162062 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402887 162062 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 502 4 3 7 2.7 O=C(Nc1cc(-c2ccn[nH]2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455188 168021 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 1.4 Cn1cc(C2C=NC=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL411896 168021 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 1.4 Cn1cc(C2C=NC=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44420235 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL223156 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44420235 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL223156 91549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563051 193454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
CHEMBL488255 193454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21 10.1016/j.bmcl.2008.10.019
70692757 83232 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 3 6 3.9 O=C(N[C@H](CCc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059792 83232 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 588 7 3 6 3.9 O=C(N[C@H](CCc1ccc(O)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
44455078 102363 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257732 102363 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
162666990 189187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 564 4 3 5 3.6 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785645 189187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 564 4 3 5 3.6 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(Cc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
11351794 97755 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL239630 97755 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555230 111942 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114480 111942 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 611 7 1 5 6.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-c1cccnc1 10.1016/j.bmcl.2013.12.089
11421827 164383 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL408093 164383 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2008.10.106
44563123 195665 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL507339 195665 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
11848645 104286 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270392 104286 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccccc2O)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11365194 147513 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2008.10.106
CHEMBL381798 147513 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2008.10.106
11365194 147513 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL381798 147513 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 576 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2006.07.044
11848800 162051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL402844 162051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11421827 164383 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL408093 164383 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2006.07.044
45485600 204601 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 487 5 2 5 2.6 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(C#N)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL572225 204601 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 487 5 2 5 2.6 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3cccc(C#N)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44562984 192821 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL487077 192821 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1ccc2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
70692759 83238 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059799 83238 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
44570375 185148 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 468 4 3 7 1.5 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL465279 185148 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 468 4 3 7 1.5 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2008.10.106
45487037 204378 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 603 5 2 4 4.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2cc(-c3ccccc3)n[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570626 204378 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 603 5 2 4 4.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(c2cc(-c3ccccc3)n[nH]c2=O)CC1 10.1016/j.bmcl.2009.09.066
70696845 83228 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 524 6 2 5 3.6 CC(C)C[C@@H](NC(=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059786 83228 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 524 6 2 5 3.6 CC(C)C[C@@H](NC(=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1)C(=O)N1CCC(N2CCCCC2)CC1 10.1016/j.bmcl.2012.05.074
44420255 144663 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL376292 144663 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
45485609 205223 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 3.7 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(C(F)(F)F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL577304 205223 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 3.7 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(C(F)(F)F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
45254862 133752 0 None - 1 Human 7.6 pKi = 7.6 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 534 5 2 8 3.3 O=C(Cn1c(=O)n(-c2nccs2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655563 133752 0 None - 1 Human 7.6 pKi = 7.6 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 534 5 2 8 3.3 O=C(Cn1c(=O)n(-c2nccs2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
70682194 83240 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 634 7 2 5 5.4 O=C(N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059800 83240 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 634 7 2 5 5.4 O=C(N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
70690617 83252 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 612 6 3 5 4.2 O=C(N[C@@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059852 83252 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 612 6 3 5 4.2 O=C(N[C@@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2012.05.074
44563027 193423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL488066 193423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2 10.1016/j.bmcl.2008.10.019
135461116 148331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384799 148331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2nc(-c3ccccc3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44562937 185872 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471704 185872 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
44563089 192939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
CHEMBL487240 192939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O 10.1016/j.bmcl.2008.10.019
59554942 111930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114468 111930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 541 6 1 5 4.7 O=C(CC1SC(c2ccccc2)N(Cc2cccnc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416514 162514 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405544 162514 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44570462 190704 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(C2CC2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL481382 190704 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(C2CC2)NC1=O 10.1016/j.bmcl.2008.10.106
45254859 133754 0 None - 1 Human 5.6 pKi = 5.6 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(C2CC2)NC1=O nan
CHEMBL3655565 133754 0 None - 1 Human 5.6 pKi = 5.6 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 492 5 2 7 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(C2CC2)NC1=O nan
71569374 94449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(C[C@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
CHEMBL2336423 94449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CGRP receptor (unknown origin)Binding affinity to CGRP receptor (unknown origin)
ChEMBL 626 6 3 5 4.5 Cc1cc(C[C@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12 10.1016/j.bmcl.2013.01.011
11541725 148164 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL383872 148164 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1 10.1016/j.bmcl.2006.07.044
44417050 148287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384539 148287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1 10.1016/j.bmcl.2006.07.044
11848647 162142 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL403373 162142 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11576078 185149 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 453 4 2 6 2.4 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCNC1=O)C2 10.1016/j.bmcl.2008.10.106
CHEMBL465280 185149 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 453 4 2 6 2.4 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCNC1=O)C2 10.1016/j.bmcl.2008.10.106
44570421 184529 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 6 2.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCCNC1=O)C2 10.1016/j.bmcl.2008.10.106
CHEMBL464264 184529 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 6 2.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(CCCNC1=O)C2 10.1016/j.bmcl.2008.10.106
24863246 83274 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 626 6 3 5 4.5 Cc1nc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2[nH]1 10.1016/j.bmcl.2012.05.074
CHEMBL2059879 83274 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 626 6 3 5 4.5 Cc1nc2cc(C[C@@H](NC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N3CCC(N4CCCCC4)CC3)ccc2[nH]1 10.1016/j.bmcl.2012.05.074
10340395 91770 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL223805 91770 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
11238717 148658 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386706 148658 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
76310551 111984 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114678 111984 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416824 87058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
CHEMBL213976 87058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2006.07.044
44420231 143821 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374666 143821 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46182711 133760 0 None - 1 Human 7.5 pKi = 7.5 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655571 133760 0 None - 1 Human 7.5 pKi = 7.5 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 583 5 3 5 3.8 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11978083 189671 0 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 556 3 4 5 2.8 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(C2CCNCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4792127 189671 0 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 556 3 4 5 2.8 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(C2CCNCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
11671386 148197 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 570 5 3 7 3.4 O=C(O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL384091 148197 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 570 5 3 7 3.4 O=C(O)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
11456102 86820 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL212942 86820 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
76325057 111924 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114462 111924 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 554 6 1 4 5.8 CC(c1ccccc1)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
59555036 111944 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114482 111944 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1 10.1016/j.bmcl.2013.12.089
46885184 15111 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
CHEMBL1092883 15111 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2010.02.086
11691938 68259 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770558 68259 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11678239 68261 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770560 68261 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 537 4 3 7 3.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CO)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
23658195 188153 0 None - 1 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 574 4 2 5 4.2 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4763305 188153 0 None - 1 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 574 4 2 5 4.2 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2020.127624
6918509 83817 41 None -131 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
CHEMBL207197 83817 41 None -131 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat CGRP receptorBinding affinity to rat CGRP receptor
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1021/jm500364u
57977652 81861 0 None -85 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035981 81861 0 None -85 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 571 4 3 5 3.9 C[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
6918509 83817 41 None -131 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.04.105
CHEMBL207197 83817 41 None -131 2 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma countingDisplacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma counting
ChEMBL 867 12 5 8 4.4 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCN(c2ccncc2)CC1 10.1016/j.bmcl.2012.04.105
11526993 204371 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
CHEMBL570531 204371 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 565 3 2 4 4.1 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c2cccnc2N1 10.1016/j.bmcl.2009.09.066
11397560 96483 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL237661 96483 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11562434 186106 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
CHEMBL473445 186106 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2008.10.106
45485654 204364 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL570488 204364 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 480 5 2 4 2.9 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)CN(Cc3ccc(F)cc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
11699891 68260 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770559 68260 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
59555277 111934 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114472 111934 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F 10.1016/j.bmcl.2013.12.089
11548734 205203 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577110 205203 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
70690613 83229 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 558 6 2 5 3.8 O=C(N[C@H](Cc1ccccc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059787 83229 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 558 6 2 5 3.8 O=C(N[C@H](Cc1ccccc1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59554876 111923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114461 111923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
10340456 90284 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL220336 90284 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
44563124 195850 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 476 6 3 7 0.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL509718 195850 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 476 6 3 7 0.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
10483685 83243 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(NC(Cc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059803 83243 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(NC(Cc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59554982 111919 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114457 111919 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
24853374 111985 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114679 111985 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
44562936 185715 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL470321 185715 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11330786 145166 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL377252 145166 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46884948 14587 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
57774187 14587 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089497 14587 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
11520022 87339 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214904 87339 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 604 5 2 4 4.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccccc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44570422 197490 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2ccccc2)NC1=O 10.1016/j.bmcl.2008.10.106
CHEMBL518236 197490 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@@]1(C2)N=C(c2ccccc2)NC1=O 10.1016/j.bmcl.2008.10.106
45487016 204564 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CCC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL571861 204564 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CCC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
44455348 162063 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1ccc(-c2ccccc2)n(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL402888 162063 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1ccc(-c2ccccc2)n(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
23627980 24972 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
CHEMBL1269978 24972 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant CGRP receptorBinding affinity to human recombinant CGRP receptor
ChEMBL 470 4 1 4 3.8 CN1C(=O)NC(=O)C12Cc1cc3cc(CN(Cc4ccccc4)C(=O)C(C)(C)C)cnc3cc1C2 10.1016/j.bmcl.2010.08.105
44570536 190652 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
CHEMBL480999 190652 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.106
45254663 133757 0 None - 1 Human 7.5 pKi = 7.5 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
CHEMBL3655568 133757 0 None - 1 Human 7.5 pKi = 7.5 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 528 5 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccc2)NC1=O nan
11157626 173215 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL427743 173215 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44563125 180606 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL453865 180606 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 504 6 2 7 0.9 CN(C)C(=O)CCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
23656918 98569 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241118 98569 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
44563091 199319 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL521076 199319 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11977861 189986 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 487 2 3 4 2.7 CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4795912 189986 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 487 2 3 4 2.7 CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
44416436 87330 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214873 87330 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1 10.1016/j.bmcl.2006.07.044
70692303 81862 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 558 4 3 6 3.2 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035982 81862 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 558 4 3 6 3.2 O=C(CN1C(=O)C2(CCCC2)NC[C@H]1c1cc(F)cc(F)c1)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
44420228 91012 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL221009 91012 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2008.10.019
11599531 205225 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
CHEMBL577320 205225 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 578 4 2 3 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)CC(c1ccccc1)NC2=O 10.1016/j.bmcl.2009.09.066
44416488 144469 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 644 4 2 6 5.9 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL375872 144469 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 644 4 2 6 5.9 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2006.07.044
44454954 102160 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL256813 102160 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
45487042 204370 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)CC(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL570527 204370 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 530 3 2 4 2.8 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)CC(=O)N1 10.1016/j.bmcl.2009.09.066
11692140 68262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
CHEMBL1770561 68262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2 10.1016/j.bmcl.2010.12.054
23656920 95923 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL236590 95923 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 528 5 3 6 2.1 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCO)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
51357854 89336 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
CHEMBL2178423 89336 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysisDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis
ChEMBL 535 3 2 7 4.5 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](O)c2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm3013147
44563090 193427 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
CHEMBL488083 193427 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1 10.1016/j.bmcl.2008.10.019
45485666 204200 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 4.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(Cl)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL569588 204200 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 530 5 2 4 4.0 CN1C(=O)NC(=O)[C@@]12Cc1ccc(NC(=O)CN(Cc3cc(Cl)cc(Cl)c3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
44563162 181356 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL455674 181356 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2 10.1016/j.bmcl.2008.10.019
25119463 187833 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 543 3 3 4 4.1 CC(C)(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4759604 187833 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 543 3 3 4 4.1 CC(C)(C)CN1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
23656922 175635 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
CHEMBL438120 175635 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 555 6 2 6 2.7 CN(C)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O 10.1021/jm070668p
59554885 111941 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
CHEMBL3114479 111941 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1 10.1016/j.bmcl.2013.12.089
11848908 102220 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257094 102220 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44562896 185822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL471359 185822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45487057 204587 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
CHEMBL572114 204587 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2009.09.066
11848966 102177 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256901 102177 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2cccc(F)c2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
44455153 104243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270175 104243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11215322 148556 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL386113 148556 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccnc32)CC1 10.1016/j.bmcl.2006.07.044
11848646 104285 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270390 104285 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 460 3 3 7 2.7 Cn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44420228 91012 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL221009 91012 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
23656586 161173 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2ccccn2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL398779 161173 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2ccccn2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
59555326 111917 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114455 111917 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 504 6 1 4 4.5 O=C(CC1SC(c2ccccc2)N(CC2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45485590 204463 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 492 6 2 5 2.7 COc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
CHEMBL571137 204463 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 492 6 2 5 2.7 COc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
11555955 204504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571459 204504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
11706251 205304 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
CHEMBL577957 205304 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 517 3 3 4 2.0 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)N1 10.1016/j.bmcl.2009.09.066
23656749 98355 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240686 98355 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
23656752 98520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
CHEMBL240904 98520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1 10.1021/jm070668p
11410749 172608 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL424864 172608 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
44420287 90214 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL219782 90214 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
11848755 102154 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
CHEMBL256802 102154 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1 10.1016/j.bmcl.2007.11.042
11495985 102445 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL258070 102445 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
44562895 185821 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
CHEMBL471358 185821 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1 10.1016/j.bmcl.2008.10.019
54582784 68265 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
CHEMBL1770564 68265 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-CGRP from human recombinant CGRP receptorDisplacement of [125I]-CGRP from human recombinant CGRP receptor
ChEMBL 564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2010.12.054
11977972 188670 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 586 5 3 6 2.4 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCN2CCOCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4779094 188670 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 586 5 3 6 2.4 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCN2CCOCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
45487060 204406 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 449 3 2 3 2.8 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(O)CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570750 204406 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 449 3 2 3 2.8 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(O)CC1 10.1016/j.bmcl.2009.09.066
11454113 152530 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL391660 152530 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11786529 146309 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL379548 146309 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1 10.1016/j.bmcl.2006.07.044
45487055 205738 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 531 3 2 4 2.3 CN1C(=O)NC(=O)C12CCN(C(=O)N[C@@H]1CC[C@@H](c3cccc(F)c3F)CN(CC(F)(F)F)C1=O)CC2 10.1016/j.bmcl.2009.09.066
CHEMBL585017 205738 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 531 3 2 4 2.3 CN1C(=O)NC(=O)C12CCN(C(=O)N[C@@H]1CC[C@@H](c3cccc(F)c3F)CN(CC(F)(F)F)C1=O)CC2 10.1016/j.bmcl.2009.09.066
59555260 111937 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114475 111937 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1 10.1016/j.bmcl.2013.12.089
44416824 87058 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2008.10.106
CHEMBL213976 87058 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 542 4 2 5 2.5 O=C1CN(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)C(=O)N1 10.1016/j.bmcl.2008.10.106
44570463 196423 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 501 4 2 6 3.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ccccc21 10.1016/j.bmcl.2008.10.106
CHEMBL515087 196423 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 501 4 2 6 3.8 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ccccc21 10.1016/j.bmcl.2008.10.106
11570464 148440 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 568 5 2 6 4.8 CC(C)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL385399 148440 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 568 5 2 6 4.8 CC(C)c1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
59554953 111932 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114470 111932 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F 10.1016/j.bmcl.2013.12.089
11848965 173478 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL428247 173478 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
46884946 15153 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)c(F)c1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1093189 15153 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)c(F)c1C2 10.1016/j.bmcl.2010.02.086
59554924 111929 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114467 111929 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45485676 204113 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
CHEMBL568880 204113 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.3 C[C@@H](c1ccccc1)N(CC(=O)Nc1ccc2c(c1)C[C@@]1(C2)C(=O)NC(=O)N1C)C(=O)C(C)(C)C 10.1016/j.bmcl.2009.07.134
46179165 131966 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 493 3 2 5 3.4 O=C1NCCN(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1c1ccc(F)cc1 nan
CHEMBL3645146 131966 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Receptor binding assay.Binding Assay: Receptor binding assay.
ChEMBL 493 3 2 5 3.4 O=C1NCCN(Cc2cnc3cc4c(cc3c2)C[C@@]2(C4)C(=O)Nc3ncccc32)C1c1ccc(F)cc1 nan
58432803 133753 0 None - 1 Human 6.2 pKi = 6.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccn2)NC1=O nan
CHEMBL3655564 133753 0 None - 1 Human 6.2 pKi = 6.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 529 5 2 8 2.6 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2ccccn2)NC1=O nan
11713729 87325 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
CHEMBL214845 87325 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 551 4 2 7 3.6 N#Cc1cn(C2CCN(C(=O)N[C@@H]3N=C(c4ccccc4)c4ccccc4N(CC(F)(F)F)C3=O)CC2)c(O)n1 10.1016/j.bmcl.2006.07.044
11692206 86984 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL213670 86984 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1 10.1016/j.bmcl.2006.07.044
24782724 188174 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 515 3 3 4 3.4 CC(C)N1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4763543 188174 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 515 3 3 4 3.4 CC(C)N1Cc2c(ccc3[nH]ncc23)C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
59555152 111935 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
CHEMBL3114473 111935 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F 10.1016/j.bmcl.2013.12.089
59731892 187470 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 591 4 2 4 5.5 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
CHEMBL4755474 187470 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 591 4 2 4 5.5 CC(C)(C)CN1Cc2c(cc(Cl)c3[nH]ncc23)C[C@@H](CC(=O)N2CCC(c3cc4cccc(F)c4[nH]c3=O)CC2)C1=O 10.1016/j.bmcl.2020.127624
11977740 189199 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 603 4 2 4 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3cccc(F)c3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4785845 189199 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 603 4 2 4 5.1 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(c2cc3cccc(F)c3[nH]c2=O)CC1 10.1016/j.bmcl.2020.127624
11585317 87693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
CHEMBL215325 87693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 616 5 2 6 5.7 Cc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1 10.1016/j.bmcl.2006.07.044
45487036 204405 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
CHEMBL570748 204405 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 541 4 2 4 3.6 Cc1cc(C2CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)c(=O)[nH]n1 10.1016/j.bmcl.2009.09.066
44420241 143490 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL374064 143490 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
70683851 81866 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 586 5 3 6 3.7 CC[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
CHEMBL2035986 81866 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrsDisplacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
ChEMBL 586 5 3 6 3.7 CC[C@@]1(c2cc(F)cc(F)c2)CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21 10.1016/j.bmcl.2012.04.105
46884999 14498 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 1 8 2.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)oc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1088906 14498 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 480 3 1 8 2.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)oc3cc1C2 10.1016/j.bmcl.2010.02.086
10453991 144658 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL376263 144658 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
23656753 98568 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL241117 98568 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 462 4 3 5 2.2 O=C1NCC(Cc2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
11444699 87280 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214751 87280 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
44562983 198166 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
CHEMBL519242 198166 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C 10.1016/j.bmcl.2008.10.019
45254858 133756 0 None - 1 Human 6.2 pKi = 6.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 530 5 2 9 2.0 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cnccn2)NC1=O nan
CHEMBL3655567 133756 0 None - 1 Human 6.2 pKi = 6.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 530 5 2 9 2.0 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)N=C(c2cnccn2)NC1=O nan
11849023 101933 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255755 101933 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
59554855 111918 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114456 111918 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
11215639 148295 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384565 148295 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2006.07.044
45254860 133755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 494 6 2 7 3.0 CCCC1=NC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 nan
CHEMBL3655566 133755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).Recombinant Receptor Binding Assay: Recombinant receptor binding assay using human CL receptor/RAMP1 (CGRP).
ChEMBL 494 6 2 7 3.0 CCCC1=NC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 nan
45487061 204418 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 582 4 2 5 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2009.09.066
CHEMBL570860 204418 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 582 4 2 5 2.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3c2ccc[n+]3[O-])CC1 10.1016/j.bmcl.2009.09.066
46884948 14587 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
57774187 14587 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089497 14587 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 7 2.1 CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2 10.1016/j.bmcl.2010.02.086
24862842 83244 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 598 6 3 6 3.6 O=C(NC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059804 83244 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 598 6 3 6 3.6 O=C(NC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
59555024 111926 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114464 111926 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
11330650 168716 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL415453 168716 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3cnccc32)CC1 10.1016/j.bmcl.2006.07.044
11157609 148195 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2c1nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384080 148195 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 590 4 2 6 5.2 Cc1cccc2c1nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
11848857 101986 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL255999 101986 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
59555012 111940 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114478 111940 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1ccnc1 10.1016/j.bmcl.2013.12.089
162649395 186951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 578 5 3 5 3.7 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4749085 186951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 578 5 3 5 3.7 O=C(N[C@@H]1Cc2ccc3[nH]ncc3c2CN(CCc2ccncc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2020.127624
46905052 17190 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
CHEMBL1162991 17190 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 488 3 2 7 0.7 Cc1cc2c3c(c1)n(CC(=O)Nc1ccc4c(c1)C[C@]1(C4)C(=O)NC(=O)N1C)c(=O)n3CC(=O)N2C 10.1016/j.bmcl.2008.10.106
44563161 180513 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
CHEMBL453644 180513 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32 10.1016/j.bmcl.2008.10.019
70682193 83237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059798 83237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 608 6 2 5 4.9 O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
45485665 204118 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.0 Cc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
CHEMBL568921 204118 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 476 5 2 4 3.0 Cc1cccc(CN(CC(=O)Nc2ccc3c(c2)CC2(C3)C(=O)NC(=O)N2C)C(=O)C(C)(C)C)c1 10.1016/j.bmcl.2009.07.134
44455080 102403 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257902 102403 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11527287 87322 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL214829 87322 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 605 5 2 5 4.1 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CC(c3ccncc3)NC2=O)CC1 10.1016/j.bmcl.2006.07.044
46884947 14586 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1cc(F)c(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1089496 14586 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 500 4 2 7 2.0 CN1C(=O)NC(=O)[C@]12Cc1cc(F)c(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2 10.1016/j.bmcl.2010.02.086
11848855 104364 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL270796 104364 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
11848750 102362 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257731 102362 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
70684297 83235 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 573 6 3 6 3.3 Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
CHEMBL2059796 83235 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 573 6 3 6 3.3 Nc1ccc(C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.05.074
59555274 111921 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114459 111921 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
23656587 96996 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL238275 96996 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
9978597 148420 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
CHEMBL385322 148420 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21 10.1016/j.bmcl.2006.09.045
59554975 111945 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114483 111945 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1 10.1016/j.bmcl.2013.12.089
44420236 144367 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL375533 144367 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
46885133 14806 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
CHEMBL1090846 14806 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2 10.1016/j.bmcl.2010.02.086
11849147 102028 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL256203 102028 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1 10.1016/j.bmcl.2007.11.042
45485621 205275 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
CHEMBL577737 205275 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 462 5 2 4 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN(Cc3ccccc3)C(=O)C(C)(C)C)cc1C2 10.1016/j.bmcl.2009.07.134
59555236 111928 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114466 111928 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44416512 162513 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL405543 162513 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2006.07.044
11453687 174233 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL429803 174233 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
70696847 83241 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
CHEMBL2059801 83241 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrsDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs
ChEMBL 597 6 3 5 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.074
11342207 148317 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL384723 148317 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 577 4 2 7 4.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccncc32)CC1 10.1016/j.bmcl.2006.07.044
11497403 172855 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL425807 172855 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1 10.1016/j.bmcl.2006.07.044
59555111 111916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114454 111916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
44420227 90207 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
CHEMBL219721 90207 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O 10.1016/j.bmcl.2006.09.045
24853163 111925 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
CHEMBL3114463 111925 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1 10.1016/j.bmcl.2013.12.089
45487056 204474 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 518 3 2 5 2.4 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
CHEMBL571236 204474 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation countingDisplacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting
ChEMBL 518 3 2 5 2.4 O=C1NC(=O)C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1 10.1016/j.bmcl.2009.09.066
76310534 111927 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
CHEMBL3114465 111927 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation countingDisplacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
ChEMBL 520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1 10.1016/j.bmcl.2013.12.089
23658240 188031 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 620 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3cccc(F)c3NC2=O)CC1 10.1016/j.bmcl.2020.127624
CHEMBL4761776 188031 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human CGRP receptorAntagonist activity at human CGRP receptor
ChEMBL 620 4 2 4 4.9 O=C(C[C@@H]1Cc2cc(Cl)c3[nH]ncc3c2CN(CC(F)(F)F)C1=O)N1CCC(N2CCc3cccc(F)c3NC2=O)CC1 10.1016/j.bmcl.2020.127624
44420260 90255 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
CHEMBL220146 90255 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
ChEMBL 483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2 10.1016/j.bmcl.2006.09.045
44562985 192941 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
CHEMBL487244 192941 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2 10.1016/j.bmcl.2008.10.019
44563160 181354 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
CHEMBL455670 181354 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cellsDisplacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
ChEMBL 518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21 10.1016/j.bmcl.2008.10.019
45273525 202465 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
CHEMBL556703 202465 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
ChEMBL 479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32 10.1016/j.bmcl.2009.06.057
11848698 102195 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 4 3 7 2.7 Cn1cc(-c2ccc(C(=O)O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
CHEMBL257004 102195 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 488 4 3 7 2.7 Cn1cc(-c2ccc(C(=O)O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O 10.1016/j.bmcl.2007.11.042
23656919 161524 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL400020 161524 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
70694861 83357 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 519 3 1 6 5.0 O=C(O[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
CHEMBL2063116 83357 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cellsDisplacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells
ChEMBL 519 3 1 6 5.0 O=C(O[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/ml300021s
11848964 101979 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255966 101979 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11849020 101822 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
CHEMBL255136 101822 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1Displacement of [125I]CGRP from human recombinant CL receptor /RAMP1
ChEMBL 528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1016/j.bmcl.2007.11.042
11532845 184528 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 7 2.0 O=C1CC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 10.1016/j.bmcl.2008.10.106
CHEMBL464263 184528 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
ChEMBL 467 4 2 7 2.0 O=C1CC2(Cc3ccc(NC(=O)Cn4c(=O)n(-c5ccccn5)c5ccccc54)cc3C2)C(=O)N1 10.1016/j.bmcl.2008.10.106
11261842 87838 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL215424 87838 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ncccc3NC2=O)CC1 10.1016/j.bmcl.2006.07.044
11215502 172914 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
CHEMBL426142 172914 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CGRP from human recombinant CGRP receptorDisplacement of [125I]CGRP from human recombinant CGRP receptor
ChEMBL 594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2006.07.044
23656588 98354 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2cccnc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
CHEMBL240685 98354 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cellsDisplacement of [125I]CGPR from human CL receptor expressed in HEK293 cells
ChEMBL 449 3 3 6 1.5 O=C1NCC(c2cccnc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1 10.1021/jm070668p
68748835 224529 0 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
CHEMBL2364638 224529 0 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
DB15328 224529 0 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 549 4 2 5 3.5 C[C@@H]1[C@@H](C[C@H](NC(=O)C2=CN=C3C[C@]4(CC3=C2)C(=O)NC2=NC=CC=C42)C(=O)N1CC(F)(F)F)C1=CC=CC=C1 None
51049968 89335 47 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F None
CHEMBL2178422 89335 47 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F None
DB12457 89335 47 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 534 3 2 7 4.5 N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F None