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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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Assay Type Assay Description Source Mol
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H don H acc LogP Smiles DOI
11467753 173350 0 CALRL calcitonin receptor-like receptor 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 173350 0 CALRL calcitonin receptor-like receptor 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
6918509 76451 28 CALRL calcitonin receptor-like receptor 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 76451 28 CALRL calcitonin receptor-like receptor 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
44593666 171885 1 CALRL calcitonin receptor-like receptor 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 171885 1 CALRL calcitonin receptor-like receptor 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 81912 30 CALRL calcitonin receptor-like receptor 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 81912 30 CALRL calcitonin receptor-like receptor 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
68857312 111217 0 CALRL calcitonin receptor-like receptor 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 111217 0 CALRL calcitonin receptor-like receptor 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
CHEMBL412994 206551 0 CALRL calcitonin receptor-like receptor 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
86298538 111219 0 CALRL calcitonin receptor-like receptor 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 111219 0 CALRL calcitonin receptor-like receptor 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
24756611 75911 0 CALRL calcitonin receptor-like receptor 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 75911 0 CALRL calcitonin receptor-like receptor 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 75915 0 CALRL calcitonin receptor-like receptor 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 75915 0 CALRL calcitonin receptor-like receptor 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 75913 0 CALRL calcitonin receptor-like receptor 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 75913 0 CALRL calcitonin receptor-like receptor 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 75912 0 CALRL calcitonin receptor-like receptor 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 75912 0 CALRL calcitonin receptor-like receptor 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 75921 0 CALRL calcitonin receptor-like receptor 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 75921 0 CALRL calcitonin receptor-like receptor 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 75920 0 CALRL calcitonin receptor-like receptor 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 75920 0 CALRL calcitonin receptor-like receptor 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
86298539 111218 0 CALRL calcitonin receptor-like receptor 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 111218 0 CALRL calcitonin receptor-like receptor 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
11621504 172617 0 CALRL calcitonin receptor-like receptor 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 172617 0 CALRL calcitonin receptor-like receptor 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 186141 0 CALRL calcitonin receptor-like receptor 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 186141 0 CALRL calcitonin receptor-like receptor 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 186117 0 CALRL calcitonin receptor-like receptor 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 186117 0 CALRL calcitonin receptor-like receptor 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 73215 0 CALRL calcitonin receptor-like receptor 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 73215 0 CALRL calcitonin receptor-like receptor 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 73532 0 CALRL calcitonin receptor-like receptor 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 73532 0 CALRL calcitonin receptor-like receptor 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 171289 0 CALRL calcitonin receptor-like receptor 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 171289 0 CALRL calcitonin receptor-like receptor 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
6918509 76451 28 CALRL calcitonin receptor-like receptor 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 76451 28 CALRL calcitonin receptor-like receptor 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
11549159 171922 0 CALRL calcitonin receptor-like receptor 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 171922 0 CALRL calcitonin receptor-like receptor 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 171885 1 CALRL calcitonin receptor-like receptor 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 171885 1 CALRL calcitonin receptor-like receptor 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
44403861 71445 0 CALRL calcitonin receptor-like receptor 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 71445 0 CALRL calcitonin receptor-like receptor 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 76451 28 CALRL calcitonin receptor-like receptor 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 76451 28 CALRL calcitonin receptor-like receptor 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 205929 0 CALRL calcitonin receptor-like receptor 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
70696079 73537 0 CALRL calcitonin receptor-like receptor 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 73537 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369459 203140 0 CALRL calcitonin receptor-like receptor 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
11657395 185708 0 CALRL calcitonin receptor-like receptor 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 185708 0 CALRL calcitonin receptor-like receptor 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 73205 0 CALRL calcitonin receptor-like receptor 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 73205 0 CALRL calcitonin receptor-like receptor 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
44403862 157077 0 CALRL calcitonin receptor-like receptor 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 157077 0 CALRL calcitonin receptor-like receptor 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
11599798 185559 0 CALRL calcitonin receptor-like receptor 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 185559 0 CALRL calcitonin receptor-like receptor 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 172495 0 CALRL calcitonin receptor-like receptor 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 172495 0 CALRL calcitonin receptor-like receptor 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
44403861 71445 0 CALRL calcitonin receptor-like receptor 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 71445 0 CALRL calcitonin receptor-like receptor 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 73215 0 CALRL calcitonin receptor-like receptor 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 73215 0 CALRL calcitonin receptor-like receptor 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
11512851 186133 0 CALRL calcitonin receptor-like receptor 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 186133 0 CALRL calcitonin receptor-like receptor 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 73616 0 CALRL calcitonin receptor-like receptor 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 73616 0 CALRL calcitonin receptor-like receptor 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 73202 0 CALRL calcitonin receptor-like receptor 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 73202 0 CALRL calcitonin receptor-like receptor 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 185748 0 CALRL calcitonin receptor-like receptor 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 185748 0 CALRL calcitonin receptor-like receptor 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
57404496 73618 0 CALRL calcitonin receptor-like receptor 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 73618 0 CALRL calcitonin receptor-like receptor 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 73202 0 CALRL calcitonin receptor-like receptor 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 73202 0 CALRL calcitonin receptor-like receptor 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
46885183 8073 0 CALRL calcitonin receptor-like receptor 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 8073 0 CALRL calcitonin receptor-like receptor 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
57404529 73616 0 CALRL calcitonin receptor-like receptor 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 73616 0 CALRL calcitonin receptor-like receptor 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
11422298 91661 0 CALRL calcitonin receptor-like receptor 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 91661 0 CALRL calcitonin receptor-like receptor 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 73217 0 CALRL calcitonin receptor-like receptor 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 73217 0 CALRL calcitonin receptor-like receptor 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 73203 0 CALRL calcitonin receptor-like receptor 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 73203 0 CALRL calcitonin receptor-like receptor 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
70683493 73617 0 CALRL calcitonin receptor-like receptor 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 73617 0 CALRL calcitonin receptor-like receptor 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 73537 0 CALRL calcitonin receptor-like receptor 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 73537 0 CALRL calcitonin receptor-like receptor 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
50939479 91806 0 CALRL calcitonin receptor-like receptor 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 91806 0 CALRL calcitonin receptor-like receptor 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 73531 0 CALRL calcitonin receptor-like receptor 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 73531 0 CALRL calcitonin receptor-like receptor 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 73534 0 CALRL calcitonin receptor-like receptor 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 73534 0 CALRL calcitonin receptor-like receptor 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
70696075 73532 0 CALRL calcitonin receptor-like receptor 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 73532 0 CALRL calcitonin receptor-like receptor 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
70681270 73206 0 CALRL calcitonin receptor-like receptor 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 73206 0 CALRL calcitonin receptor-like receptor 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 192591 0 CALRL calcitonin receptor-like receptor 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 192591 0 CALRL calcitonin receptor-like receptor 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 91663 0 CALRL calcitonin receptor-like receptor 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 91663 0 CALRL calcitonin receptor-like receptor 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 186088 0 CALRL calcitonin receptor-like receptor 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 186088 0 CALRL calcitonin receptor-like receptor 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
70687597 73205 0 CALRL calcitonin receptor-like receptor 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 73205 0 CALRL calcitonin receptor-like receptor 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 73534 0 CALRL calcitonin receptor-like receptor 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 73534 0 CALRL calcitonin receptor-like receptor 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
44583379 185583 0 CALRL calcitonin receptor-like receptor 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 185583 0 CALRL calcitonin receptor-like receptor 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
11308219 73203 0 CALRL calcitonin receptor-like receptor 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 73203 0 CALRL calcitonin receptor-like receptor 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
11204498 91671 0 CALRL calcitonin receptor-like receptor 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 91671 0 CALRL calcitonin receptor-like receptor 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
44403860 140262 0 CALRL calcitonin receptor-like receptor 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 140262 0 CALRL calcitonin receptor-like receptor 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 73217 0 CALRL calcitonin receptor-like receptor 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 73217 0 CALRL calcitonin receptor-like receptor 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
54581910 60966 0 CALRL calcitonin receptor-like receptor 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 60966 0 CALRL calcitonin receptor-like receptor 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
11364682 73808 0 CALRL calcitonin receptor-like receptor 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 73808 0 CALRL calcitonin receptor-like receptor 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
46174937 75990 4 CALRL calcitonin receptor-like receptor 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 75990 4 CALRL calcitonin receptor-like receptor 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 91660 0 CALRL calcitonin receptor-like receptor 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 91660 0 CALRL calcitonin receptor-like receptor 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 74501 1 CALRL calcitonin receptor-like receptor 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 74501 1 CALRL calcitonin receptor-like receptor 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 60961 1 CALRL calcitonin receptor-like receptor 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 60961 1 CALRL calcitonin receptor-like receptor 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
70696077 73535 0 CALRL calcitonin receptor-like receptor 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 73535 0 CALRL calcitonin receptor-like receptor 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 73540 0 CALRL calcitonin receptor-like receptor 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 73540 0 CALRL calcitonin receptor-like receptor 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
54586725 60965 0 CALRL calcitonin receptor-like receptor 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 60965 0 CALRL calcitonin receptor-like receptor 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 91659 0 CALRL calcitonin receptor-like receptor 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 91659 0 CALRL calcitonin receptor-like receptor 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 179073 0 CALRL calcitonin receptor-like receptor 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 179073 0 CALRL calcitonin receptor-like receptor 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
70689756 73530 0 CALRL calcitonin receptor-like receptor 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 73530 0 CALRL calcitonin receptor-like receptor 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
11364682 73808 0 CALRL calcitonin receptor-like receptor 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 73808 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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
11308069 73531 0 CALRL calcitonin receptor-like receptor 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 73531 0 CALRL calcitonin receptor-like receptor 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 73615 0 CALRL calcitonin receptor-like receptor 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 73615 0 CALRL calcitonin receptor-like receptor 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
59555187 104463 0 CALRL calcitonin receptor-like receptor 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 104463 0 CALRL calcitonin receptor-like receptor 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
70681270 73206 0 CALRL calcitonin receptor-like receptor 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 73206 0 CALRL calcitonin receptor-like receptor 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
54585731 60952 0 CALRL calcitonin receptor-like receptor 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 60952 0 CALRL calcitonin receptor-like receptor 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 60963 0 CALRL calcitonin receptor-like receptor 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 60963 0 CALRL calcitonin receptor-like receptor 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
24756690 73201 0 CALRL calcitonin receptor-like receptor 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 73201 0 CALRL calcitonin receptor-like receptor 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 73529 0 CALRL calcitonin receptor-like receptor 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 73529 0 CALRL calcitonin receptor-like receptor 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 73538 0 CALRL calcitonin receptor-like receptor 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 73538 0 CALRL calcitonin receptor-like receptor 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
70685595 73615 0 CALRL calcitonin receptor-like receptor 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 73615 0 CALRL calcitonin receptor-like receptor 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 74501 1 CALRL calcitonin receptor-like receptor 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 74501 1 CALRL calcitonin receptor-like receptor 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 73204 0 CALRL calcitonin receptor-like receptor 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 73204 0 CALRL calcitonin receptor-like receptor 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
11169454 73204 0 CALRL calcitonin receptor-like receptor 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 73204 0 CALRL calcitonin receptor-like receptor 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 60934 0 CALRL calcitonin receptor-like receptor 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 60934 0 CALRL calcitonin receptor-like receptor 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 91668 0 CALRL calcitonin receptor-like receptor 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 91668 0 CALRL calcitonin receptor-like receptor 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
11786642 73800 0 CALRL calcitonin receptor-like receptor 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 73800 0 CALRL calcitonin receptor-like receptor 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
50939479 91806 0 CALRL calcitonin receptor-like receptor 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 91806 0 CALRL calcitonin receptor-like receptor 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 91670 0 CALRL calcitonin receptor-like receptor 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 91670 0 CALRL calcitonin receptor-like receptor 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 91672 0 CALRL calcitonin receptor-like receptor 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 91672 0 CALRL calcitonin receptor-like receptor 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
70685566 73539 0 CALRL calcitonin receptor-like receptor 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 73539 0 CALRL calcitonin receptor-like receptor 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
11706981 60957 0 CALRL calcitonin receptor-like receptor 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 60957 0 CALRL calcitonin receptor-like receptor 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 60965 0 CALRL calcitonin receptor-like receptor 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 60965 0 CALRL calcitonin receptor-like receptor 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 91664 0 CALRL calcitonin receptor-like receptor 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 91664 0 CALRL calcitonin receptor-like receptor 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 73800 0 CALRL calcitonin receptor-like receptor 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 73800 0 CALRL calcitonin receptor-like receptor 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
11295951 73804 0 CALRL calcitonin receptor-like receptor 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 73804 0 CALRL calcitonin receptor-like receptor 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 73799 0 CALRL calcitonin receptor-like receptor 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 73799 0 CALRL calcitonin receptor-like receptor 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 203142 0 CALRL calcitonin receptor-like receptor 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 207745 20 CALRL calcitonin receptor-like receptor 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
46885244 7530 0 CALRL calcitonin receptor-like receptor 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 7530 0 CALRL calcitonin receptor-like receptor 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 104464 0 CALRL calcitonin receptor-like receptor 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 104464 0 CALRL calcitonin receptor-like receptor 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
CHEMBL525571 207745 20 CALRL calcitonin receptor-like receptor 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
54581909 60960 0 CALRL calcitonin receptor-like receptor 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 60960 0 CALRL calcitonin receptor-like receptor 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 60952 0 CALRL calcitonin receptor-like receptor 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 60952 0 CALRL calcitonin receptor-like receptor 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 189878 0 CALRL calcitonin receptor-like receptor 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 189878 0 CALRL calcitonin receptor-like receptor 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 60945 0 CALRL calcitonin receptor-like receptor 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 60945 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 191244 0 CALRL calcitonin receptor-like receptor 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 191244 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 186520 0 CALRL calcitonin receptor-like receptor 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 60951 0 CALRL calcitonin receptor-like receptor 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 60951 0 CALRL calcitonin receptor-like receptor 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 60961 1 CALRL calcitonin receptor-like receptor 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 60961 1 CALRL calcitonin receptor-like receptor 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 73804 0 CALRL calcitonin receptor-like receptor 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 73804 0 CALRL calcitonin receptor-like receptor 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 91673 0 CALRL calcitonin receptor-like receptor 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 91673 0 CALRL calcitonin receptor-like receptor 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 60964 0 CALRL calcitonin receptor-like receptor 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 60964 0 CALRL calcitonin receptor-like receptor 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 7943 0 CALRL calcitonin receptor-like receptor 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 7943 0 CALRL calcitonin receptor-like receptor 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 73201 0 CALRL calcitonin receptor-like receptor 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 73201 0 CALRL calcitonin receptor-like receptor 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 60966 0 CALRL calcitonin receptor-like receptor 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 60966 0 CALRL calcitonin receptor-like receptor 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 91679 0 CALRL calcitonin receptor-like receptor 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 91679 0 CALRL calcitonin receptor-like receptor 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 60956 0 CALRL calcitonin receptor-like receptor 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 60956 0 CALRL calcitonin receptor-like receptor 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 73799 0 CALRL calcitonin receptor-like receptor 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 73799 0 CALRL calcitonin receptor-like receptor 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
11467108 73803 0 CALRL calcitonin receptor-like receptor 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 73803 0 CALRL calcitonin receptor-like receptor 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
54583842 60959 0 CALRL calcitonin receptor-like receptor 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 60959 0 CALRL calcitonin receptor-like receptor 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 91662 0 CALRL calcitonin receptor-like receptor 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 91662 0 CALRL calcitonin receptor-like receptor 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 60962 0 CALRL calcitonin receptor-like receptor 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 60962 0 CALRL calcitonin receptor-like receptor 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 8062 0 CALRL calcitonin receptor-like receptor 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 8062 0 CALRL calcitonin receptor-like receptor 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 187087 0 CALRL calcitonin receptor-like receptor 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 187087 0 CALRL calcitonin receptor-like receptor 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 91676 0 CALRL calcitonin receptor-like receptor 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 91676 0 CALRL calcitonin receptor-like receptor 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 10140 0 CALRL calcitonin receptor-like receptor 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 10140 0 CALRL calcitonin receptor-like receptor 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 177603 0 CALRL calcitonin receptor-like receptor 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 177603 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369463 203142 0 CALRL calcitonin receptor-like receptor 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
71819577 144498 0 CALRL calcitonin receptor-like receptor 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 144498 0 CALRL calcitonin receptor-like receptor 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 60953 0 CALRL calcitonin receptor-like receptor 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 60953 0 CALRL calcitonin receptor-like receptor 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 73794 0 CALRL calcitonin receptor-like receptor 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 73794 0 CALRL calcitonin receptor-like receptor 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 91674 0 CALRL calcitonin receptor-like receptor 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 91674 0 CALRL calcitonin receptor-like receptor 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 73803 0 CALRL calcitonin receptor-like receptor 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 73803 0 CALRL calcitonin receptor-like receptor 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 104488 0 CALRL calcitonin receptor-like receptor 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 104488 0 CALRL calcitonin receptor-like receptor 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 89551 0 CALRL calcitonin receptor-like receptor 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 89551 0 CALRL calcitonin receptor-like receptor 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
11341642 73794 0 CALRL calcitonin receptor-like receptor 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 73794 0 CALRL calcitonin receptor-like receptor 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
46885185 7706 0 CALRL calcitonin receptor-like receptor 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 7706 0 CALRL calcitonin receptor-like receptor 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
70696078 73536 0 CALRL calcitonin receptor-like receptor 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 73536 0 CALRL calcitonin receptor-like receptor 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
54583842 60959 0 CALRL calcitonin receptor-like receptor 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 60959 0 CALRL calcitonin receptor-like receptor 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 73795 0 CALRL calcitonin receptor-like receptor 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 73795 0 CALRL calcitonin receptor-like receptor 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 190255 0 CALRL calcitonin receptor-like receptor 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 190255 0 CALRL calcitonin receptor-like receptor 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 7530 0 CALRL calcitonin receptor-like receptor 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 7530 0 CALRL calcitonin receptor-like receptor 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
70696080 73541 0 CALRL calcitonin receptor-like receptor 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 73541 0 CALRL calcitonin receptor-like receptor 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
11520007 60954 0 CALRL calcitonin receptor-like receptor 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 60954 0 CALRL calcitonin receptor-like receptor 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 60956 0 CALRL calcitonin receptor-like receptor 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 60956 0 CALRL calcitonin receptor-like receptor 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 73801 0 CALRL calcitonin receptor-like receptor 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 73801 0 CALRL calcitonin receptor-like receptor 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
11398863 73802 0 CALRL calcitonin receptor-like receptor 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 73802 0 CALRL calcitonin receptor-like receptor 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
54587762 60962 0 CALRL calcitonin receptor-like receptor 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 60962 0 CALRL calcitonin receptor-like receptor 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 7943 0 CALRL calcitonin receptor-like receptor 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 7943 0 CALRL calcitonin receptor-like receptor 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
11466363 73798 0 CALRL calcitonin receptor-like receptor 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 73798 0 CALRL calcitonin receptor-like receptor 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
54582783 60933 0 CALRL calcitonin receptor-like receptor 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 60933 0 CALRL calcitonin receptor-like receptor 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 91665 0 CALRL calcitonin receptor-like receptor 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 91665 0 CALRL calcitonin receptor-like receptor 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 187181 0 CALRL calcitonin receptor-like receptor 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 187181 0 CALRL calcitonin receptor-like receptor 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 60955 0 CALRL calcitonin receptor-like receptor 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 60955 0 CALRL calcitonin receptor-like receptor 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 60960 0 CALRL calcitonin receptor-like receptor 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 60960 0 CALRL calcitonin receptor-like receptor 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 91658 0 CALRL calcitonin receptor-like receptor 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 91658 0 CALRL calcitonin receptor-like receptor 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 7773 0 CALRL calcitonin receptor-like receptor 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 7773 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369459 203140 0 CALRL calcitonin receptor-like receptor 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
11599135 185622 0 CALRL calcitonin receptor-like receptor 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 185622 0 CALRL calcitonin receptor-like receptor 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
11192748 73795 0 CALRL calcitonin receptor-like receptor 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 73795 0 CALRL calcitonin receptor-like receptor 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
54580838 60951 0 CALRL calcitonin receptor-like receptor 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 60951 0 CALRL calcitonin receptor-like receptor 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 73798 0 CALRL calcitonin receptor-like receptor 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 73798 0 CALRL calcitonin receptor-like receptor 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 91675 0 CALRL calcitonin receptor-like receptor 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 91675 0 CALRL calcitonin receptor-like receptor 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
70693987 73613 0 CALRL calcitonin receptor-like receptor 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 73613 0 CALRL calcitonin receptor-like receptor 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
44563028 188237 0 CALRL calcitonin receptor-like receptor 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 188237 0 CALRL calcitonin receptor-like receptor 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 104454 0 CALRL calcitonin receptor-like receptor 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 104454 0 CALRL calcitonin receptor-like receptor 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 146182 0 CALRL calcitonin receptor-like receptor 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 146182 0 CALRL calcitonin receptor-like receptor 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 146549 0 CALRL calcitonin receptor-like receptor 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 146549 0 CALRL calcitonin receptor-like receptor 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 183164 0 CALRL calcitonin receptor-like receptor 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 183164 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369452 203136 0 CALRL calcitonin receptor-like receptor 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 73716 0 CALRL calcitonin receptor-like receptor 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 73716 0 CALRL calcitonin receptor-like receptor 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
44416824 79637 0 CALRL calcitonin receptor-like receptor 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 79637 0 CALRL calcitonin receptor-like receptor 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 140752 0 CALRL calcitonin receptor-like receptor 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 140752 0 CALRL calcitonin receptor-like receptor 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 73189 0 CALRL calcitonin receptor-like receptor 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 73189 0 CALRL calcitonin receptor-like receptor 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
44403854 71639 0 CALRL calcitonin receptor-like receptor 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 71639 0 CALRL calcitonin receptor-like receptor 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
23656587 89550 0 CALRL calcitonin receptor-like receptor 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 89550 0 CALRL calcitonin receptor-like receptor 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
CHEMBL216229 202844 0 CALRL calcitonin receptor-like receptor 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 204226 0 CALRL calcitonin receptor-like receptor 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 204227 0 CALRL calcitonin receptor-like receptor 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 204289 0 CALRL calcitonin receptor-like receptor 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 206088 0 CALRL calcitonin receptor-like receptor 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 206265 0 CALRL calcitonin receptor-like receptor 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 207253 0 CALRL calcitonin receptor-like receptor 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 207268 0 CALRL calcitonin receptor-like receptor 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
11848908 94761 0 CALRL calcitonin receptor-like receptor 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 94761 0 CALRL calcitonin receptor-like receptor 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
44403917 71716 0 CALRL calcitonin receptor-like receptor 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 71716 0 CALRL calcitonin receptor-like receptor 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
11848647 154556 0 CALRL calcitonin receptor-like receptor 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 154556 0 CALRL calcitonin receptor-like receptor 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 80209 0 CALRL calcitonin receptor-like receptor 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 80209 0 CALRL calcitonin receptor-like receptor 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 96518 0 CALRL calcitonin receptor-like receptor 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 96518 0 CALRL calcitonin receptor-like receptor 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 94986 0 CALRL calcitonin receptor-like receptor 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 94986 0 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 73216 0 CALRL calcitonin receptor-like receptor 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 73216 0 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 191182 0 CALRL calcitonin receptor-like receptor 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 191182 0 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 88483 38 CALRL calcitonin receptor-like receptor 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 191182 0 CALRL calcitonin receptor-like receptor 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 191182 0 CALRL calcitonin receptor-like receptor 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 191278 0 CALRL calcitonin receptor-like receptor 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 191278 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369454 203137 0 CALRL calcitonin receptor-like receptor 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 73216 0 CALRL calcitonin receptor-like receptor 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 73216 0 CALRL calcitonin receptor-like receptor 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 203138 0 CALRL calcitonin receptor-like receptor 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
44420228 83584 0 CALRL calcitonin receptor-like receptor 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 83584 0 CALRL calcitonin receptor-like receptor 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 137094 0 CALRL calcitonin receptor-like receptor 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 137094 0 CALRL calcitonin receptor-like receptor 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 151789 0 CALRL calcitonin receptor-like receptor 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 151789 0 CALRL calcitonin receptor-like receptor 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 191223 0 CALRL calcitonin receptor-like receptor 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 191223 0 CALRL calcitonin receptor-like receptor 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 140977 0 CALRL calcitonin receptor-like receptor 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 140977 0 CALRL calcitonin receptor-like receptor 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 94717 0 CALRL calcitonin receptor-like receptor 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 94717 0 CALRL calcitonin receptor-like receptor 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 94526 0 CALRL calcitonin receptor-like receptor 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 94526 0 CALRL calcitonin receptor-like receptor 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 173645 0 CALRL calcitonin receptor-like receptor 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 173645 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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 60937 0 CALRL calcitonin receptor-like receptor 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 60937 0 CALRL calcitonin receptor-like receptor 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 60941 0 CALRL calcitonin receptor-like receptor 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 60941 0 CALRL calcitonin receptor-like receptor 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 60939 0 CALRL calcitonin receptor-like receptor 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 60939 0 CALRL calcitonin receptor-like receptor 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 60940 0 CALRL calcitonin receptor-like receptor 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 60940 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369454 203137 0 CALRL calcitonin receptor-like receptor 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 73533 0 CALRL calcitonin receptor-like receptor 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 73533 0 CALRL calcitonin receptor-like receptor 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 73792 0 CALRL calcitonin receptor-like receptor 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 73792 0 CALRL calcitonin receptor-like receptor 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 73805 0 CALRL calcitonin receptor-like receptor 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 73805 0 CALRL calcitonin receptor-like receptor 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
44563125 172981 0 CALRL calcitonin receptor-like receptor 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 172981 0 CALRL calcitonin receptor-like receptor 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 73195 0 CALRL calcitonin receptor-like receptor 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 73195 0 CALRL calcitonin receptor-like receptor 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 91669 0 CALRL calcitonin receptor-like receptor 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 91669 0 CALRL calcitonin receptor-like receptor 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 90308 0 CALRL calcitonin receptor-like receptor 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 90308 0 CALRL calcitonin receptor-like receptor 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 192036 0 CALRL calcitonin receptor-like receptor 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 192036 0 CALRL calcitonin receptor-like receptor 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
70685454 73199 0 CALRL calcitonin receptor-like receptor 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 73199 0 CALRL calcitonin receptor-like receptor 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
44420228 83584 0 CALRL calcitonin receptor-like receptor 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 83584 0 CALRL calcitonin receptor-like receptor 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 83584 0 CALRL calcitonin receptor-like receptor 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 83584 0 CALRL calcitonin receptor-like receptor 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 178073 0 CALRL calcitonin receptor-like receptor 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 178073 0 CALRL calcitonin receptor-like receptor 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 187516 0 CALRL calcitonin receptor-like receptor 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 187516 0 CALRL calcitonin receptor-like receptor 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 188237 0 CALRL calcitonin receptor-like receptor 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 188237 0 CALRL calcitonin receptor-like receptor 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 8074 0 CALRL calcitonin receptor-like receptor 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 8074 0 CALRL calcitonin receptor-like receptor 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
CHEMBL216710 202862 0 CALRL calcitonin receptor-like receptor 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 200058 0 CALRL calcitonin receptor-like receptor 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 200058 0 CALRL calcitonin receptor-like receptor 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
11706251 192115 0 CALRL calcitonin receptor-like receptor 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 192115 0 CALRL calcitonin receptor-like receptor 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 104428 0 CALRL calcitonin receptor-like receptor 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 104428 0 CALRL calcitonin receptor-like receptor 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 183820 0 CALRL calcitonin receptor-like receptor 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 183820 0 CALRL calcitonin receptor-like receptor 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 173645 0 CALRL calcitonin receptor-like receptor 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 173645 0 CALRL calcitonin receptor-like receptor 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 60964 0 CALRL calcitonin receptor-like receptor 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 60964 0 CALRL calcitonin receptor-like receptor 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 73716 0 CALRL calcitonin receptor-like receptor 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 73716 0 CALRL calcitonin receptor-like receptor 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 10140 0 CALRL calcitonin receptor-like receptor 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 10140 0 CALRL calcitonin receptor-like receptor 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 191216 0 CALRL calcitonin receptor-like receptor 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 191216 0 CALRL calcitonin receptor-like receptor 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 191215 0 CALRL calcitonin receptor-like receptor 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 191215 0 CALRL calcitonin receptor-like receptor 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 177603 0 CALRL calcitonin receptor-like receptor 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 177603 0 CALRL calcitonin receptor-like receptor 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 183824 0 CALRL calcitonin receptor-like receptor 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 183824 0 CALRL calcitonin receptor-like receptor 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 187534 0 CALRL calcitonin receptor-like receptor 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 187534 0 CALRL calcitonin receptor-like receptor 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
58864453 73112 0 CALRL calcitonin receptor-like receptor 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 73112 0 CALRL calcitonin receptor-like receptor 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 71841 0 CALRL calcitonin receptor-like receptor 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 71841 0 CALRL calcitonin receptor-like receptor 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
59555245 104437 0 CALRL calcitonin receptor-like receptor 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 104437 0 CALRL calcitonin receptor-like receptor 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 161111 0 CALRL calcitonin receptor-like receptor 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 161111 0 CALRL calcitonin receptor-like receptor 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 104455 0 CALRL calcitonin receptor-like receptor 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 104455 0 CALRL calcitonin receptor-like receptor 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 165309 0 CALRL calcitonin receptor-like receptor 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 165309 0 CALRL calcitonin receptor-like receptor 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 140738 0 CALRL calcitonin receptor-like receptor 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 140738 0 CALRL calcitonin receptor-like receptor 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 80429 0 CALRL calcitonin receptor-like receptor 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 80429 0 CALRL calcitonin receptor-like receptor 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 173732 0 CALRL calcitonin receptor-like receptor 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 173732 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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 187317 0 CALRL calcitonin receptor-like receptor 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 73805 0 CALRL calcitonin receptor-like receptor 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 73805 0 CALRL calcitonin receptor-like receptor 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 89038 0 CALRL calcitonin receptor-like receptor 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 89038 0 CALRL calcitonin receptor-like receptor 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 7773 0 CALRL calcitonin receptor-like receptor 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 7773 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369742 203189 0 CALRL calcitonin receptor-like receptor 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 203138 0 CALRL calcitonin receptor-like receptor 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
44563052 183820 0 CALRL calcitonin receptor-like receptor 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 183820 0 CALRL calcitonin receptor-like receptor 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
70696851 75918 0 CALRL calcitonin receptor-like receptor 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 75918 0 CALRL calcitonin receptor-like receptor 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 73191 0 CALRL calcitonin receptor-like receptor 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 73191 0 CALRL calcitonin receptor-like receptor 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
44420286 83602 0 CALRL calcitonin receptor-like receptor 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 83602 0 CALRL calcitonin receptor-like receptor 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
CHEMBL376040 205754 0 CALRL calcitonin receptor-like receptor 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
44455153 96778 0 CALRL calcitonin receptor-like receptor 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 96778 0 CALRL calcitonin receptor-like receptor 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 154476 0 CALRL calcitonin receptor-like receptor 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 154476 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2371143 203538 0 CALRL calcitonin receptor-like receptor 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
54582784 60941 0 CALRL calcitonin receptor-like receptor 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 60941 0 CALRL calcitonin receptor-like receptor 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 88478 0 CALRL calcitonin receptor-like receptor 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 88478 0 CALRL calcitonin receptor-like receptor 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 89217 0 CALRL calcitonin receptor-like receptor 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 89217 0 CALRL calcitonin receptor-like receptor 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
24756769 73212 0 CALRL calcitonin receptor-like receptor 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 73212 0 CALRL calcitonin receptor-like receptor 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
44562982 183823 0 CALRL calcitonin receptor-like receptor 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 183823 0 CALRL calcitonin receptor-like receptor 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 187534 0 CALRL calcitonin receptor-like receptor 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 187534 0 CALRL calcitonin receptor-like receptor 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 183970 0 CALRL calcitonin receptor-like receptor 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 183970 0 CALRL calcitonin receptor-like receptor 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 91121 0 CALRL calcitonin receptor-like receptor 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 91121 0 CALRL calcitonin receptor-like receptor 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
24756612 75913 0 CALRL calcitonin receptor-like receptor 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 75913 0 CALRL calcitonin receptor-like receptor 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
122238743 159934 0 CALRL calcitonin receptor-like receptor 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 159934 0 CALRL calcitonin receptor-like receptor 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 183966 0 CALRL calcitonin receptor-like receptor 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 183966 0 CALRL calcitonin receptor-like receptor 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 104493 0 CALRL calcitonin receptor-like receptor 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 104493 0 CALRL calcitonin receptor-like receptor 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 94694 0 CALRL calcitonin receptor-like receptor 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 94694 0 CALRL calcitonin receptor-like receptor 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 140686 0 CALRL calcitonin receptor-like receptor 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 140686 0 CALRL calcitonin receptor-like receptor 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 139936 0 CALRL calcitonin receptor-like receptor 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 139936 0 CALRL calcitonin receptor-like receptor 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
CHEMBL406459 206122 0 CALRL calcitonin receptor-like receptor 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
23656922 168017 0 CALRL calcitonin receptor-like receptor 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 168017 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369464 203143 0 CALRL calcitonin receptor-like receptor 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
59555260 104443 0 CALRL calcitonin receptor-like receptor 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 104443 0 CALRL calcitonin receptor-like receptor 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 182996 0 CALRL calcitonin receptor-like receptor 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 182996 0 CALRL calcitonin receptor-like receptor 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 94761 0 CALRL calcitonin receptor-like receptor 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 94761 0 CALRL calcitonin receptor-like receptor 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
CHEMBL2369464 203143 0 CALRL calcitonin receptor-like receptor 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
59555152 104441 0 CALRL calcitonin receptor-like receptor 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 104441 0 CALRL calcitonin receptor-like receptor 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 96899 0 CALRL calcitonin receptor-like receptor 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 96899 0 CALRL calcitonin receptor-like receptor 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 82826 0 CALRL calcitonin receptor-like receptor 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 82826 0 CALRL calcitonin receptor-like receptor 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
CHEMBL411804 206471 0 CALRL calcitonin receptor-like receptor 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 75910 0 CALRL calcitonin receptor-like receptor 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 75910 0 CALRL calcitonin receptor-like receptor 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 73197 0 CALRL calcitonin receptor-like receptor 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 73197 0 CALRL calcitonin receptor-like receptor 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 71685 0 CALRL calcitonin receptor-like receptor 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 71685 0 CALRL calcitonin receptor-like receptor 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 71148 0 CALRL calcitonin receptor-like receptor 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 71148 0 CALRL calcitonin receptor-like receptor 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 105460 0 CALRL calcitonin receptor-like receptor 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 105460 0 CALRL calcitonin receptor-like receptor 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
11785754 73792 0 CALRL calcitonin receptor-like receptor 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 73792 0 CALRL calcitonin receptor-like receptor 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 94801 0 CALRL calcitonin receptor-like receptor 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 94801 0 CALRL calcitonin receptor-like receptor 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 104438 0 CALRL calcitonin receptor-like receptor 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 104438 0 CALRL calcitonin receptor-like receptor 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
58864479 73196 0 CALRL calcitonin receptor-like receptor 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 73196 0 CALRL calcitonin receptor-like receptor 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
44420231 136255 0 CALRL calcitonin receptor-like receptor 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 136255 0 CALRL calcitonin receptor-like receptor 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 90908 0 CALRL calcitonin receptor-like receptor 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 90908 0 CALRL calcitonin receptor-like receptor 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
CHEMBL267406 204234 0 CALRL calcitonin receptor-like receptor 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
11261842 80414 0 CALRL calcitonin receptor-like receptor 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 80414 0 CALRL calcitonin receptor-like receptor 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 94944 0 CALRL calcitonin receptor-like receptor 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 94944 0 CALRL calcitonin receptor-like receptor 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
56675112 62783 0 CALRL calcitonin receptor-like receptor 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 62783 0 CALRL calcitonin receptor-like receptor 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<