Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL454791 calrl_human Human No 10.8 EC50 = 0.0 nM Funct
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
626 6 3 5 4.5 Cc1cc(C[C@@H](NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL207197 calrl_human Human Yes 10.6 EC50 = 0.0 nM Bind
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
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
CHEMBL450668 calrl_human Human Yes 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL2178422 calrl_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL3288288 calrl_human Human No 9.8 EC50 = 0.2 nM Bind
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
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
CHEMBL412994 calrl_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL3288290 calrl_human Human No 7.0 EC50 = 100 nM Bind
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
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
CHEMBL2059896 calrl_human Human No 7.9 EC50 = 12 nM Funct
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
613 5 2 5 5.4 O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1
CHEMBL2059900 calrl_human Human No 7.9 EC50 = 13 nM Funct
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
626 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O
CHEMBL2059898 calrl_human Human No 6.9 EC50 = 130 nM Funct
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
613 5 2 5 4.8 O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21
CHEMBL2059897 calrl_human Human No 7.8 EC50 = 15 nM Funct
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
613 5 2 5 4.7 O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1
CHEMBL2059906 calrl_human Human No 8.5 EC50 = 3 nM Funct
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
614 5 3 5 5.1 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1
CHEMBL2059905 calrl_human Human No 7.5 EC50 = 31 nM Funct
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
615 5 2 6 5.6 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1
CHEMBL3288289 calrl_human Human No 7.0 EC50 = 96 nM Bind
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
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
CHEMBL452966 calrl_human Human No 11.0 IC50 = 0.0 nM Funct
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
627 6 2 6 4.9 Cc1cc(C[C@@H](OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL508453 calrl_human Human No 11.0 IC50 = 0.0 nM Funct
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
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
CHEMBL508215 calrl_human Human No 10.8 IC50 = 0.0 nM Funct
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
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
CHEMBL2018517 calrl_human Human No 10.7 IC50 = 0.0 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
625 7 2 5 4.9 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2022601 calrl_human Human No 10.7 IC50 = 0.0 nM Funct
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
607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL447297 calrl_human Human No 10.7 IC50 = 0.0 nM Funct
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
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
CHEMBL207197 calrl_human Human Yes 10.7 IC50 = 0.0 nM Bind
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
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
CHEMBL451164 calrl_human Human No 10.7 IC50 = 0.0 nM Funct
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
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
CHEMBL450668 calrl_human Human Yes 10.6 IC50 = 0.0 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL197529 calrl_human Human No 10.5 IC50 = 0.0 nM Bind
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
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
CHEMBL207197 calrl_human Human Yes 10.5 IC50 = 0.0 nM Bind
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
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
CHEMBL3883526 calrl_human Human No 10.5 IC50 = 0.0 nM Bind
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
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
CHEMBL2022606 calrl_human Human No 10.4 IC50 = 0.0 nM Funct
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
618 7 2 6 6.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2369459 calrl_human Human No 10.4 IC50 = 0.0 nM Bind
Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor
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
CHEMBL501603 calrl_human Human No 10.4 IC50 = 0.0 nM Funct
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
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
CHEMBL2018507 calrl_human Human No 10.3 IC50 = 0.0 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL408415 calrl_human Human No 10.3 IC50 = 0.1 nM Bind
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
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
CHEMBL499488 calrl_human Human No 10.3 IC50 = 0.1 nM Funct
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
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
CHEMBL452686 calrl_human Human No 10.2 IC50 = 0.1 nM Funct
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
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
CHEMBL197529 calrl_human Human No 10.2 IC50 = 0.1 nM Bind
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
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
CHEMBL2018517 calrl_human Human No 10.2 IC50 = 0.1 nM Bind
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
625 7 2 5 4.9 Cc1cc(C[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL508349 calrl_human Human No 10.2 IC50 = 0.1 nM Funct
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
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
CHEMBL2023189 calrl_human Human No 10.2 IC50 = 0.1 nM Funct
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
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
CHEMBL2018504 calrl_human Human No 10.2 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
625 7 2 5 4.9 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL502243 calrl_human Human No 10.2 IC50 = 0.1 nM Funct
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
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
CHEMBL2023191 calrl_human Human No 10.2 IC50 = 0.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
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
CHEMBL2018504 calrl_human Human No 10.1 IC50 = 0.1 nM Bind
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
625 7 2 5 4.9 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL1092882 calrl_human Human No 10.1 IC50 = 0.1 nM Funct
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
488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1
CHEMBL2023189 calrl_human Human No 10.1 IC50 = 0.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
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
CHEMBL2430167 calrl_human Human No 10.1 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
637 7 3 6 6.0 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)cc(Cl)n1
CHEMBL2018519 calrl_human Human No 10.1 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL2018505 calrl_human Human No 10.1 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
643 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2023190 calrl_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
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
CHEMBL2022606 calrl_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
618 7 2 6 6.8 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2431248 calrl_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assayAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay
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
CHEMBL2022600 calrl_human Human No 10.0 IC50 = 0.1 nM Funct
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
621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2022603 calrl_human Human No 10.0 IC50 = 0.1 nM Funct
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
604 7 2 6 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2022601 calrl_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2018508 calrl_human Human No 9.9 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL585568 calrl_human Human No 9.9 IC50 = 0.1 nM Funct
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
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
CHEMBL2430169 calrl_human Human No 9.9 IC50 = 0.1 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
603 7 3 6 5.3 Cc1cc(Cn2ccnc2C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)ccn1
CHEMBL507893 calrl_human Human No 9.9 IC50 = 0.1 nM Funct
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
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
CHEMBL2018507 calrl_human Human No 9.8 IC50 = 0.2 nM Bind
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
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
CHEMBL2022603 calrl_human Human No 9.8 IC50 = 0.2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
604 7 2 6 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL499810 calrl_human Human No 9.7 IC50 = 0.2 nM Funct
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
608 6 1 6 5.8 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4cn3)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2018505 calrl_human Human No 9.7 IC50 = 0.2 nM Bind
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
643 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2430177 calrl_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
644 7 3 5 6.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(C(C)(C)C)cc2)cc2cn[nH]c12
CHEMBL382469 calrl_human Human No 9.7 IC50 = 0.2 nM Bind
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
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
CHEMBL2018519 calrl_human Human No 9.7 IC50 = 0.2 nM Bind
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
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
CHEMBL1770729 calrl_human Human No 9.7 IC50 = 0.2 nM Funct
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
592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1
CHEMBL2024603 calrl_human Human No 9.7 IC50 = 0.2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12
CHEMBL2063115 calrl_human Human Yes 9.7 IC50 = 0.2 nM Funct
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
519 3 1 6 5.0 O=C(O[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2430166 calrl_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
633 6 2 7 6.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(C2CCCCC2)C3)cc2cn[nH]c12
CHEMBL2035983 calrl_human Human Yes 9.6 IC50 = 0.2 nM Funct
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
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
CHEMBL1770724 calrl_human Human Yes 9.6 IC50 = 0.2 nM Funct
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
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
CHEMBL2022604 calrl_human Human No 9.6 IC50 = 0.2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
590 7 2 6 6.0 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCCC3)ccn2)cc2cn[nH]c12
CHEMBL2022609 calrl_human Human No 9.6 IC50 = 0.2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
586 6 2 5 6.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(-c3ccccc3)n[nH]c12
CHEMBL1770728 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
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
CHEMBL2430165 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
641 7 2 7 6.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCN(Cc2ccccc2)C3)cc2cn[nH]c12
CHEMBL4746351 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
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
CHEMBL2022599 calrl_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
587 6 2 6 6.3 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(-c3ccncc3)ccn2)cc2cn[nH]c12
CHEMBL2024603 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C=O)ccn2)cc2cn[nH]c12
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL2022600 calrl_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
621 6 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N3CCCCC3)ccn2)cc2cn[nH]c12
CHEMBL2023188 calrl_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
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
CHEMBL3114495 calrl_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL2018508 calrl_human Human No 9.5 IC50 = 0.3 nM Bind
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
622 7 2 5 5.1 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL1770715 calrl_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL1770726 calrl_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL2018503 calrl_human Human No 9.5 IC50 = 0.3 nM Bind
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
612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2022598 calrl_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
581 6 2 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)N(C)C)ccn2)cc2cn[nH]c12
CHEMBL2022607 calrl_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Br)n[nH]c12
CHEMBL2023188 calrl_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL2035983 calrl_human Human Yes 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.3 nM Bind
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
611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
611 6 3 5 4.6 Cc1cc(CC(CC(=O)N2CCC3(CC2)NC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL1770557 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
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
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
CHEMBL2430174 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
620 7 3 5 6.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(C)n2Cc2cccc(F)c2)cc2cn[nH]c12
CHEMBL2024595 calrl_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12
CHEMBL2431248 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
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
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
CHEMBL2430176 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
702 7 3 5 6.7 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)cn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12
CHEMBL2430178 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
624 7 3 5 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cc(F)cc(F)c2)cc2cn[nH]c12
CHEMBL2022608 calrl_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
544 5 2 5 5.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(Cl)n[nH]c12
CHEMBL1770720 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
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
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
CHEMBL1770728 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
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
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
CHEMBL2430170 calrl_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccnc2)cc2cn[nH]c12
CHEMBL2024595 calrl_human Human No 9.3 IC50 = 0.5 nM Funct
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
588 5 2 5 6.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12
CHEMBL2024599 calrl_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12
CHEMBL2024594 calrl_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12
CHEMBL2369463 calrl_human Human No 9.3 IC50 = 0.5 nM Bind
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.
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
CHEMBL525571 calrl_human Human Yes 9.3 IC50 = 0.5 nM Bind
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.
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
CHEMBL1089433 calrl_human Human No 9.3 IC50 = 0.5 nM Funct
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
487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2
CHEMBL3114496 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
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
CHEMBL525571 calrl_rat Rat Yes 9.2 IC50 = 0.6 nM Bind
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
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
CHEMBL1770723 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12
CHEMBL1770715 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
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
CHEMBL562069 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL1770568 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
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
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL570933 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
516 3 3 6 2.7 NCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@]1(C4)C(=O)Nc3ncccc31)C2=O
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
480 3 3 7 1.8 O=C(Cn1c(=O)n2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL1770714 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770724 calrl_human Human Yes 9.2 IC50 = 0.6 nM Funct
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
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
CHEMBL2024599 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
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
560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12
CHEMBL2430179 calrl_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2cccc(F)c2)cc2cn[nH]c12
CHEMBL1770727 calrl_human Human No 9.2 IC50 = 0.7 nM Funct
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
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
CHEMBL1092208 calrl_human Human No 9.2 IC50 = 0.7 nM Funct
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
501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2
CHEMBL2018503 calrl_human Human No 9.2 IC50 = 0.7 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
612 6 2 6 5.0 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL1770729 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
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
592 3 2 7 5.5 CC1(c2cnc3n2C[C@H](c2cccc(F)c2F)CC[C@H]3NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)CCCO1
CHEMBL2430185 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
588 7 3 5 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2)cc2cn[nH]c12
CHEMBL1770719 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
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
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
CHEMBL2024594 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
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
587 5 3 4 5.5 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(Br)n2)cc2cn[nH]c12
CHEMBL2024598 calrl_human Human No 9.1 IC50 = 0.8 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12
CHEMBL1770722 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
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
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
CHEMBL2430168 calrl_human Human No 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccncc2)cc2cn[nH]c12
CHEMBL1770725 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
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
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
CHEMBL1092837 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
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
473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1
CHEMBL517467 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
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
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
CHEMBL2430182 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
602 8 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2CCc2ccccc2)cc2cn[nH]c12
CHEMBL1162991 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
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
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
CHEMBL466192 calrl_human Human No 9.1 IC50 = 0.9 nM Funct
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
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
CHEMBL2369463 calrl_rat Rat No 9.1 IC50 = 0.9 nM Bind
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
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
CHEMBL3913150 calrl_human Human No 9.0 IC50 = 0.9 nM Funct
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).
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
CHEMBL1770716 calrl_human Human No 9.0 IC50 = 0.9 nM Funct
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
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
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 0.9 nM Funct
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
536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12
CHEMBL2430180 calrl_human Human No 9.0 IC50 = 1.0 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccc(F)cc2)cc2cn[nH]c12
CHEMBL2024598 calrl_human Human No 9.0 IC50 = 1 nM Funct
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
559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc3ccccc3cn2)cc2cn[nH]c12
CHEMBL3114676 calrl_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL238276 calrl_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
536 7 2 5 4.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(C=O)cn2)cc2cn[nH]c12
CHEMBL1090515 calrl_human Human No 8.9 IC50 = 1.2 nM Funct
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
502 2 1 7 2.8 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32
CHEMBL2022605 calrl_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
606 7 2 7 5.2 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2cc(CN3CCOCC3)ccn2)cc2cn[nH]c12
CHEMBL1770722 calrl_human Human No 8.9 IC50 = 1.3 nM Funct
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
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
CHEMBL2024590 calrl_human Human No 8.9 IC50 = 1.3 nM Funct
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
605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12
CHEMBL564487 calrl_human Human No 8.9 IC50 = 1.3 nM Funct
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
479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2
CHEMBL1089433 calrl_human Human No 8.9 IC50 = 1.3 nM Funct
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
487 2 2 5 4.2 CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2
CHEMBL2022610 calrl_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
538 6 2 6 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(C=O)n[nH]c12
CHEMBL1770717 calrl_human Human No 8.9 IC50 = 1.4 nM Funct
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
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
CHEMBL1770719 calrl_human Human No 8.9 IC50 = 1.4 nM Funct
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
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
CHEMBL2024596 calrl_human Human No 8.9 IC50 = 1.4 nM Funct
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
559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12
CHEMBL2024597 calrl_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12
CHEMBL1770725 calrl_human Human No 8.8 IC50 = 1.5 nM Funct
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
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
CHEMBL1092208 calrl_human Human No 8.8 IC50 = 1.5 nM Funct
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
501 3 2 5 4.6 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2
CHEMBL2024593 calrl_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL1770556 calrl_human Human No 8.8 IC50 = 1.6 nM Funct
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
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
CHEMBL2430171 calrl_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
589 7 3 6 5.0 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccn2)cc2cn[nH]c12
CHEMBL518422 calrl_human Human No 8.8 IC50 = 1.6 nM Funct
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
503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL1770718 calrl_human Human No 8.8 IC50 = 1.7 nM Funct
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
536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12
CHEMBL1770723 calrl_human Human No 8.8 IC50 = 1.7 nM Funct
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
552 4 2 7 4.6 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)OC(=O)Nc1ncccc12
CHEMBL2430164 calrl_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
579 6 2 7 5.0 CCN1CCn2c(cnc2C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C1
CHEMBL1090848 calrl_human Human No 8.8 IC50 = 1.7 nM Funct
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
468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2
CHEMBL2369459 calrl_human Human No 8.8 IC50 = 1.7 nM Bind
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
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
CHEMBL500384 calrl_human Human No 8.7 IC50 = 1.8 nM Funct
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
541 5 2 5 4.7 Cc1cc(C[C@@H](OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12
CHEMBL2024590 calrl_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
605 8 2 5 6.0 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CN3CCCCC3)cn2)cc2cn[nH]c12
CHEMBL1770714 calrl_human Human No 8.7 IC50 = 1.9 nM Funct
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
551 5 2 7 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2024593 calrl_human Human No 8.7 IC50 = 1.9 nM Funct
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
510 5 2 5 5.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL2430181 calrl_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
606 7 3 5 5.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2Cc2ccccc2F)cc2cn[nH]c12
CHEMBL2023186 calrl_human Human No 8.7 IC50 = 1.9 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
609 7 2 7 5.0 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCOCC3)n[nH]c12
CHEMBL530116 calrl_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL3114486 calrl_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL392635 calrl_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL392937 calrl_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL482178 calrl_human Human No 8.0 IC50 = 10 nM Funct
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
483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2
CHEMBL2369452 calrl_rat Rat No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL2024172 calrl_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1
CHEMBL213976 calrl_human Human No 7.0 IC50 = 100 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL384799 calrl_human Human No 7.0 IC50 = 100 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL2018491 calrl_human Human No 7.0 IC50 = 100 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
649 7 3 5 4.7 O=C(Nc1ccccc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1
CHEMBL198105 calrl_human Human No 6.0 IC50 = 1000 nM Bind
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
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
CHEMBL238275 calrl_human Human No 6.0 IC50 = 1000 nM Funct
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
464 3 4 6 1.8 O=C1NCC(c2ccc(O)cc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL216229 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL267137 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL267182 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL269027 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL405694 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL409205 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL438008 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL438224 calrl_human Human No 5.0 IC50 = 10000 nM Bind
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.
None None None None
CHEMBL257094 calrl_human Human No 6.0 IC50 = 1004 nM Funct
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
524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL198311 calrl_human Human No 5.0 IC50 = 10300 nM Bind
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
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
CHEMBL403373 calrl_human Human No 6.0 IC50 = 1066 nM Funct
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
445 3 2 7 2.4 Cn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL215274 calrl_human Human No 7.0 IC50 = 107 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL268420 calrl_human Human No 7.0 IC50 = 107.2 nM Funct
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
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
CHEMBL258070 calrl_human Human No 5.0 IC50 = 10900 nM Funct
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
444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 nM Funct
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
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
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 nM Funct
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
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
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
625 7 2 5 4.9 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 nM Funct
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
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
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 nM Funct
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
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
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 nM Funct
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
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
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL571203 calrl_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL2369454 calrl_rat Rat No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 nM Bind
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
625 7 2 5 4.9 Cc1cc(C[C@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)cc2cn[nH]c12
CHEMBL2369457 calrl_human Human No 8.0 IC50 = 11.2 nM Bind
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
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
CHEMBL221009 calrl_human Human No 7.0 IC50 = 110 nM Funct
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
405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2
CHEMBL376292 calrl_human Human No 7.0 IC50 = 110 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ncccn4)c4ccccc43)cc1C2
CHEMBL3971889 calrl_human Human No 6.0 IC50 = 1100 nM Funct
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).
503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL570793 calrl_human Human No 7.0 IC50 = 112 nM Funct
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
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
CHEMBL386113 calrl_human Human No 6.0 IC50 = 1135 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL256901 calrl_human Human No 6.9 IC50 = 119 nM Funct
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
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
CHEMBL255999 calrl_human Human No 5.9 IC50 = 1190 nM Funct
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
489 6 2 8 2.5 COCCn1cc(-c2cccnc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL455458 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL1770560 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL1770564 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770562 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770563 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL2369454 calrl_human Human No 7.9 IC50 = 12 nM Bind
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.
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
CHEMBL2022602 calrl_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
507 5 2 5 5.4 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL2024587 calrl_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12
CHEMBL453865 calrl_human Human No 6.9 IC50 = 120 nM Funct
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
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
CHEMBL2018497 calrl_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12
CHEMBL2430175 calrl_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
512 5 4 4 4.4 Cc1c[nH]c(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1
CHEMBL239630 calrl_human Human No 6.9 IC50 = 120 nM Funct
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
466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL577320 calrl_human Human No 6.9 IC50 = 120 nM Funct
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
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
CHEMBL2018501 calrl_human Human No 6.9 IC50 = 120 nM Bind
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
700 7 2 5 6.3 O=C(C[C@H](Nc1ccc(Br)c2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL221009 calrl_human Human No 6.9 IC50 = 120 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2
CHEMBL221009 calrl_human Human No 5.9 IC50 = 1200 nM Funct
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
405 3 3 5 1.0 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccccc43)cc1C2
CHEMBL470321 calrl_human Human No 5.9 IC50 = 1200 nM Funct
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
423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2
CHEMBL520905 calrl_human Human No 5.9 IC50 = 1200 nM Funct
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
423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(F)cc43)cc1C2
CHEMBL530116 calrl_human Human No 5.9 IC50 = 1200 nM Funct
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
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
CHEMBL1092883 calrl_human Human No 5.9 IC50 = 1200 nM Funct
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
482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32
CHEMBL216710 calrl_human Human No 5.9 IC50 = 1200 nM Bind
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.
None None None None
CHEMBL88441 calrl_human Human No 4.9 IC50 = 12000 nM Bind
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
494 7 1 5 6.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Oc3ccccc3)cc2)nc2ccc(OC)cc12
CHEMBL577957 calrl_human Human No 6.9 IC50 = 122 nM Funct
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
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
CHEMBL3114460 calrl_human Human No 5.9 IC50 = 1220 nM Funct
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
508 7 1 5 3.7 COCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL487068 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL455458 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL1770727 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL2024172 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
536 7 2 4 5.6 CCc1ccnc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)c1
CHEMBL1162991 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL570748 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL570746 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL466192 calrl_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL487077 calrl_human Human No 6.9 IC50 = 130 nM Funct
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
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
CHEMBL521076 calrl_human Human No 6.9 IC50 = 130 nM Funct
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
462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2
CHEMBL2018356 calrl_human Human No 6.9 IC50 = 130 nM Bind
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
626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL198762 calrl_human Human No 4.9 IC50 = 13000 nM Bind
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
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
CHEMBL3114469 calrl_human Human No 5.9 IC50 = 1370 nM Funct
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
555 7 1 5 4.7 O=C(CC1SC(c2ccccc2)N(CCc2ccccn2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL415453 calrl_human Human No 5.9 IC50 = 1381 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL3114487 calrl_human Human No 4.9 IC50 = 13900 nM Funct
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
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
CHEMBL426142 calrl_human Human No 5.9 IC50 = 1396 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL384723 calrl_human Human No 5.9 IC50 = 1398 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL215499 calrl_human Human No 7.9 IC50 = 14 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL455674 calrl_human Human No 7.9 IC50 = 14 nM Funct
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
488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2
CHEMBL519421 calrl_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 14 nM Funct
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
585 6 3 4 6.4 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cccc(-c3ccccc3)n2)cc2cn[nH]c12
CHEMBL237661 calrl_human Human No 7.9 IC50 = 14 nM Funct
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
484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1090848 calrl_human Human No 7.9 IC50 = 14 nM Funct
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
468 2 2 7 1.4 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2
CHEMBL2369742 calrl_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL2369457 calrl_human Human No 7.8 IC50 = 14.5 nM Bind
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.
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
CHEMBL487068 calrl_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL2059903 calrl_human Human No 5.9 IC50 = 1400 nM Bind
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
627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccncc1)NC2=O
CHEMBL2018493 calrl_human Human No 5.9 IC50 = 1400 nM Bind
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
574 7 2 7 3.2 O=C(C[C@H](Nc1ccncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL221160 calrl_human Human No 5.9 IC50 = 1400 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
406 3 2 6 1.3 CN1C(=O)NC(=O)C12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2
CHEMBL376040 calrl_human Human No 4.9 IC50 = 14000 nM Bind
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.
None None None None
CHEMBL270175 calrl_human Human No 6.9 IC50 = 142 nM Funct
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
460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL402887 calrl_human Human No 5.9 IC50 = 1421 nM Funct
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
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
CHEMBL2371143 calrl_human Human No 6.8 IC50 = 146 nM Bind
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.
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
CHEMBL1770564 calrl_human Human No 7.8 IC50 = 15 nM Funct
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
564 6 3 7 3.6 CNCCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL236590 calrl_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL237849 calrl_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL2018514 calrl_human Human No 7.8 IC50 = 15 nM Bind
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
598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1
CHEMBL487076 calrl_human Human No 6.8 IC50 = 150 nM Funct
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
423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(F)ccc43)cc1C2
CHEMBL521076 calrl_human Human No 6.8 IC50 = 150 nM Funct
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
462 5 3 7 -0.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CC(N)=O)c4ccccc43)cc1C2
CHEMBL488082 calrl_human Human No 6.8 IC50 = 150 nM Funct
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
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
CHEMBL241118 calrl_human Human No 6.8 IC50 = 150 nM Funct
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
466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2059898 calrl_human Human No 6.8 IC50 = 150 nM Bind
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
613 5 2 5 4.8 O=C1NCC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc21
CHEMBL4114031 calrl_human Human No 6.8 IC50 = 150 nM Funct
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).
487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL488065 calrl_human Human No 5.8 IC50 = 1500 nM Funct
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
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
CHEMBL3114681 calrl_human Human No 5.8 IC50 = 1500 nM Funct
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
492 5 1 4 4.5 CC(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL256802 calrl_human Human No 5.8 IC50 = 1528 nM Funct
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
474 4 2 7 3.0 COc1ccc(-c2cc(NC(=O)N3CCC(n4c(=O)[nH]c5ncccc54)CC3)c(=O)n(C)c2)cc1
CHEMBL384408 calrl_human Human No 6.8 IC50 = 156 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL381798 calrl_human Human No 5.8 IC50 = 1583 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL406459 calrl_human Human No 6.8 IC50 = 159 nM Bind
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.
None None None None
CHEMBL438120 calrl_human Human No 7.8 IC50 = 16 nM Funct
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
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
CHEMBL2369464 calrl_human Human No 7.8 IC50 = 16 nM Bind
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.
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
CHEMBL3114475 calrl_human Human No 6.8 IC50 = 160 nM Funct
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
619 7 1 6 5.3 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCOCC1
CHEMBL480999 calrl_human Human No 6.8 IC50 = 160 nM Funct
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
474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2
CHEMBL257094 calrl_human Human No 6.8 IC50 = 164 nM Funct
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
524 6 2 7 3.3 COCCn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL2369464 calrl_rat Rat No 7.8 IC50 = 17.9 nM Bind
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
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
CHEMBL3114473 calrl_human Human No 6.8 IC50 = 170 nM Funct
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
570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1c(F)cccc1F
CHEMBL270796 calrl_human Human No 6.8 IC50 = 170 nM Funct
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
504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL220101 calrl_human Human No 6.8 IC50 = 170 nM Funct
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
475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2
CHEMBL411804 calrl_human Human No 6.8 IC50 = 170 nM Bind
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.
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
CHEMBL2059895 calrl_human Human No 6.8 IC50 = 170 nM Bind
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
599 5 2 5 5.0 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)Nc1ccccc12
CHEMBL2018499 calrl_human Human No 6.8 IC50 = 170 nM Bind
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
612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL198232 calrl_human Human No 4.8 IC50 = 17000 nM Bind
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
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
CHEMBL196582 calrl_human Human No 4.8 IC50 = 17000 nM Bind
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
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
CHEMBL313797 calrl_human Human No 4.8 IC50 = 17000 nM Bind
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
454 5 1 4 5.9 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(F)c(Cl)c2)nc2ccc(OC)cc12
CHEMBL2024587 calrl_human Human No 7.8 IC50 = 18 nM Funct
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
522 6 2 4 5.3 Cc1ccc(C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)Cc2cc(C)c3[nH]ncc3c2)nc1
CHEMBL257252 calrl_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL3114470 calrl_human Human No 6.8 IC50 = 180 nM Funct
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
552 6 1 4 5.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1F
CHEMBL2018498 calrl_human Human No 6.8 IC50 = 180 nM Bind
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
611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL374666 calrl_human Human No 6.8 IC50 = 180 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
517 4 2 6 2.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cc(F)cc(F)c4)c4ccccc43)cc1C2
CHEMBL240686 calrl_human Human No 5.8 IC50 = 1800 nM Funct
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
454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL267406 calrl_human Human No 4.8 IC50 = 18000 nM Bind
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.
None None None None
CHEMBL215424 calrl_human Human No 5.7 IC50 = 1837 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL257902 calrl_human Human No 6.7 IC50 = 184 nM Funct
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
434 3 2 8 2.3 Cn1cc(C2C=CN=N2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL1794015 calrl_human Human No 6.7 IC50 = 185 nM Bind
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
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
CHEMBL428247 calrl_human Human No 6.7 IC50 = 186 nM Funct
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
530 4 2 6 4.1 O=C(Nc1cc(-c2ccccc2F)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770558 calrl_human Human No 7.7 IC50 = 19 nM Funct
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
507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL3114488 calrl_human Human No 7.7 IC50 = 19 nM Funct
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
646 7 1 6 5.3 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL2018512 calrl_human Human No 7.7 IC50 = 19 nM Bind
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
529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12
CHEMBL3114472 calrl_human Human No 6.7 IC50 = 190 nM Funct
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
570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccc(F)cc1F
CHEMBL3971889 calrl_human Human No 5.7 IC50 = 1900 nM Funct
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).
503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL3350392 calrl_human Human No 4.7 IC50 = 19000 nM Bind
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.
None None None CC(C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O
CHEMBL214800 calrl_human Human No 6.7 IC50 = 193 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
632 6 2 7 5.4 COc1ccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)cc1
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 nM Funct
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
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
CHEMBL1770720 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
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
CHEMBL3114494 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
678 8 1 6 5.8 CCN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL2018511 calrl_human Human No 8.7 IC50 = 2 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12
CHEMBL237662 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL237663 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL392635 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
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
CHEMBL415263 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
558 6 2 6 3.5 CSCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL392636 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL562069 calrl_human Human No 8.7 IC50 = 2 nM Funct
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
463 3 3 5 3.2 O=C(Cn1cc2c3c(cccc31)NC(=O)C2)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 nM Funct
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
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
CHEMBL2369459 calrl_human Human No 8.7 IC50 = 2 nM Bind
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
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
CHEMBL2024596 calrl_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
559 5 3 4 5.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12
CHEMBL3037882 calrl_human Human No 8.7 IC50 = 2 nM Bind
In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)In vitro ability to displace [125 I]CGRP from Calcitonin gene-related peptide type receptor at 4 degrees Celsius in rabbit lung; value ranges from (2-5)
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL3037882 calrl_human Human No 8.7 IC50 = 2 nM Bind
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
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2.1 nM Funct
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
540 6 3 6 4.7 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(CO)ccn2)cc2cn[nH]c12
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 nM Funct
Antagonist activity against human CGRP receptor by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor by cell based cAMP accumulation assay
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
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 nM Funct
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
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
CHEMBL1092838 calrl_human Human No 8.7 IC50 = 2.2 nM Funct
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
467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.3 nM Funct
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
575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12
CHEMBL2369463 calrl_human Human No 8.6 IC50 = 2.3 nM Bind
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
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
CHEMBL525571 calrl_human Human Yes 8.6 IC50 = 2.3 nM Bind
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
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
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 nM Funct
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
460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2
CHEMBL1770556 calrl_human Human No 8.6 IC50 = 2.4 nM Funct
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
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
CHEMBL236593 calrl_human Human Yes 8.6 IC50 = 2.4 nM Funct
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
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
CHEMBL564088 calrl_human Human No 8.6 IC50 = 2.4 nM Funct
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
465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 nM Funct
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
460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2
CHEMBL466192 calrl_human Human No 8.6 IC50 = 2.4 nM Funct
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
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
CHEMBL2369459 calrl_rat Rat No 8.6 IC50 = 2.4 nM Bind
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
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
CHEMBL1092882 calrl_human Human No 8.6 IC50 = 2.5 nM Funct
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
488 2 2 7 2.7 O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1
CHEMBL464078 calrl_human Human No 8.6 IC50 = 2.5 nM Funct
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
525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL1770566 calrl_human Human No 8.6 IC50 = 2.6 nM Funct
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
583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770557 calrl_human Human No 8.6 IC50 = 2.6 nM Funct
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
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
CHEMBL382469 calrl_human Human No 8.6 IC50 = 2.7 nM Bind
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
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
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.7 nM Funct
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
575 3 2 6 4.4 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(CC(F)(F)F)nnc21)N1CCC2(CC1)C(=O)Nc1ncccc12
CHEMBL570746 calrl_human Human No 8.6 IC50 = 2.7 nM Funct
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
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
CHEMBL3288290 calrl_human Human No 8.6 IC50 = 2.7 nM Bind
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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
CHEMBL2018511 calrl_human Human No 8.6 IC50 = 2.7 nM Bind
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
556 6 2 4 4.7 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(C)CC2)cc2cn[nH]c12
CHEMBL1770726 calrl_human Human No 8.5 IC50 = 2.9 nM Funct
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
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
CHEMBL2430163 calrl_human Human No 8.5 IC50 = 2.9 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
551 5 3 7 4.3 Cc1cc(CC(OC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ncc3n2CCNC3)cc2cn[nH]c12
CHEMBL2024171 calrl_human Human No 7.7 IC50 = 20 nM Funct
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
526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL2059900 calrl_human Human No 7.7 IC50 = 20 nM Bind
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
626 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1ccccc1)NC2=O
CHEMBL2059905 calrl_human Human No 7.7 IC50 = 20 nM Bind
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
615 5 2 6 5.6 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1
CHEMBL2369464 calrl_human Human No 7.7 IC50 = 20.2 nM Bind
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
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
CHEMBL198925 calrl_human Human No 6.7 IC50 = 200 nM Bind
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
787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1
CHEMBL429765 calrl_human Human No 6.7 IC50 = 200 nM Bind
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.
None None None None
CHEMBL471530 calrl_human Human No 5.7 IC50 = 2000 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2
CHEMBL268539 calrl_human Human No 6.7 IC50 = 205 nM Bind
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.
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C
CHEMBL255966 calrl_human Human No 6.7 IC50 = 209 nM Funct
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
512 4 2 6 4.0 O=C(Nc1cc(-c2ccccc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL455674 calrl_human Human No 7.7 IC50 = 21 nM Funct
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
488 3 3 7 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)CCC4)cc1C2
CHEMBL237663 calrl_human Human No 7.7 IC50 = 21 nM Funct
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
538 5 2 5 3.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL570748 calrl_human Human No 7.7 IC50 = 21 nM Funct
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
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
CHEMBL2369465 calrl_human Human No 7.7 IC50 = 21.9 nM Bind
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.
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL3114471 calrl_human Human No 6.7 IC50 = 210 nM Funct
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
570 6 1 4 5.8 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1cccc(F)c1F
CHEMBL2059904 calrl_human Human No 6.7 IC50 = 210 nM Bind
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
627 6 2 7 3.8 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)N=C(c1cccnc1)NC2=O
CHEMBL237661 calrl_human Human No 7.7 IC50 = 22 nM Funct
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
484 3 3 5 2.4 O=C1NC[C@H](c2cccc(F)c2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL237664 calrl_human Human No 7.7 IC50 = 22 nM Funct
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
498 3 2 5 2.8 CN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL2369457 calrl_rat Rat No 7.7 IC50 = 22 nM Bind
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
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
CHEMBL3943580 calrl_human Human No 7.7 IC50 = 22 nM Funct
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).
487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL3985425 calrl_human Human No 7.7 IC50 = 22 nM Funct
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).
555 3 2 5 5.2 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)[C@@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL405544 calrl_human Human No 6.7 IC50 = 220 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
654 5 2 8 4.3 CS(=O)(=O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1
CHEMBL453644 calrl_human Human No 6.7 IC50 = 220 nM Funct
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
474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32
CHEMBL391660 calrl_human Human No 6.7 IC50 = 220 nM Funct
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
466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1162991 calrl_human Human No 6.7 IC50 = 220 nM Funct
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
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
CHEMBL520778 calrl_human Human No 6.7 IC50 = 220 nM Funct
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
505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2
CHEMBL20034 calrl_human Human No 6.7 IC50 = 220 nM Bind
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.
None None None None
CHEMBL2018502 calrl_human Human No 6.7 IC50 = 220 nM Bind
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
622 7 2 5 5.5 O=C(C[C@H](Nc1cccc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL427743 calrl_human Human No 6.7 IC50 = 224 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccncc3NC2=O)CC1
CHEMBL194631 calrl_human Human No 6.7 IC50 = 226 nM Bind
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
828 13 4 9 3.7 COc1ccccc1N1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1
CHEMBL471358 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
433 3 3 5 1.6 Cc1cc(C)c2[nH]c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c2c1
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL236590 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL549503 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL577110 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
577 4 2 4 3.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CC(F)(F)F)C1=O)N1CCC2(CC1)N=C(c1ccccc1)NC2=O
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL2059896 calrl_human Human No 7.6 IC50 = 23 nM Bind
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
613 5 2 5 5.4 O=C1CC2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)c2ccccc2N1
CHEMBL2018499 calrl_human Human No 6.6 IC50 = 230 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
612 7 3 6 4.2 O=C(C[C@H](Nc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL455670 calrl_human Human No 7.6 IC50 = 24 nM Funct
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
518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21
CHEMBL564088 calrl_human Human No 7.6 IC50 = 24 nM Funct
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
465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL464078 calrl_human Human No 7.6 IC50 = 24 nM Funct
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
525 4 2 7 3.9 O=C(Cn1c(=O)n(C2CCSCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL2024591 calrl_human Human No 7.6 IC50 = 24 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL375533 calrl_human Human No 7.6 IC50 = 24 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccs4)c4ccccc43)cc1C2
CHEMBL404977 calrl_human Human No 4.6 IC50 = 24000 nM Bind
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.
None None None None
CHEMBL439085 calrl_human Human No 4.6 IC50 = 24000 nM Bind
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.
None None None None
CHEMBL2369465 calrl_human Human No 7.6 IC50 = 25 nM Bind
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
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL3288289 calrl_human Human No 7.6 IC50 = 25 nM Bind
Displacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-hCGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
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
CHEMBL194632 calrl_human Human No 6.6 IC50 = 250 nM Bind
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
827 13 4 8 4.8 COc1ccccc1C1CCN(C(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1
CHEMBL3114465 calrl_human Human No 6.6 IC50 = 250 nM Funct
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
520 5 1 4 5.1 CC(C)(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL241118 calrl_human Human No 6.6 IC50 = 250 nM Funct
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
466 3 3 5 2.3 O=C1NCC(c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL391660 calrl_human Human No 6.6 IC50 = 250 nM Funct
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
466 3 3 5 2.3 O=C1NC[C@H](c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2018495 calrl_human Human No 6.6 IC50 = 250 nM Bind
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
648 7 3 8 3.7 O=C(C[C@H](Nc1nc(Cl)nc2[nH]ncc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL488083 calrl_human Human No 7.6 IC50 = 26 nM Funct
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
510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1
CHEMBL1770560 calrl_human Human No 7.6 IC50 = 26 nM Funct
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
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
CHEMBL471704 calrl_human Human No 6.6 IC50 = 260 nM Funct
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
435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C
CHEMBL520778 calrl_human Human No 7.6 IC50 = 27 nM Funct
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
505 4 2 7 2.5 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCSCC4)c4ccccc43)cc1C2
CHEMBL463880 calrl_human Human No 7.6 IC50 = 27 nM Funct
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
495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL407774 calrl_human Human No 5.6 IC50 = 2700 nM Bind
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.
None None None None
CHEMBL1770561 calrl_human Human No 7.6 IC50 = 28 nM Funct
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
521 3 2 6 4.2 Cc1cn2c(n1)[C@H](NC(=O)N1CCC(n3c(=O)[nH]c4ncccc43)CC1)CC[C@@H](c1cccc(F)c1F)C2
CHEMBL2022595 calrl_human Human No 7.6 IC50 = 28 nM Funct
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
554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12
CHEMBL507339 calrl_human Human No 6.6 IC50 = 280 nM Funct
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
490 5 2 7 0.5 CN(C)C(=O)Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21
CHEMBL270796 calrl_human Human No 6.6 IC50 = 280 nM Funct
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
504 6 3 8 2.8 COCCn1cc(-c2ccc(O)cc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL407854 calrl_human Human No 6.6 IC50 = 280 nM Bind
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.
None None None None
CHEMBL2018487 calrl_human Human No 6.6 IC50 = 280 nM Bind
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
616 7 2 6 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)Oc1ccccc1
CHEMBL255136 calrl_human Human No 6.6 IC50 = 282 nM Funct
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
528 4 3 7 3.7 O=C(Nc1cc(-c2ccc(O)cc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL211931 calrl_human Human No 6.5 IC50 = 286 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3nccnc32)CC1
CHEMBL264010 calrl_human Human No 7.5 IC50 = 29 nM Bind
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.
None None None None
CHEMBL2059897 calrl_human Human No 7.5 IC50 = 29 nM Bind
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
613 5 2 5 4.7 O=C1Cc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1
CHEMBL3928622 calrl_human Human No 6.5 IC50 = 290 nM Funct
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).
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
CHEMBL220336 calrl_human Human No 5.5 IC50 = 2900 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
392 3 3 6 0.9 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O
CHEMBL3114466 calrl_human Human No 5.5 IC50 = 2940 nM Funct
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
526 5 1 4 5.3 O=C(CC1SC(c2ccccc2)N(c2ccccc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL3114490 calrl_human Human No 8.5 IC50 = 3 nM Funct
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
664 7 1 6 5.4 CN1CCN(c2c(F)cccc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL392636 calrl_human Human No 8.5 IC50 = 3 nM Funct
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
590 6 2 7 2.2 CS(=O)(=O)CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL237662 calrl_human Human No 8.5 IC50 = 3 nM Funct
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
542 6 2 6 2.8 COCCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL392634 calrl_human Human No 8.5 IC50 = 3 nM Funct
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
597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL549503 calrl_human Human No 8.5 IC50 = 3 nM Funct
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
479 3 3 5 3.3 O=C(CN1CC2CCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL2369454 calrl_human Human No 8.5 IC50 = 3 nM Bind
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
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
CHEMBL466555 calrl_human Human No 8.5 IC50 = 3 nM Bind
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
628 6 2 5 5.5 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL2022597 calrl_human Human No 8.5 IC50 = 3 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
535 5 2 6 5.1 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C#N)ccn2)cc2cn[nH]c12
CHEMBL2024592 calrl_human Human No 8.5 IC50 = 3.1 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL1770568 calrl_human Human No 8.5 IC50 = 3.2 nM Funct
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
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
CHEMBL2018509 calrl_human Human No 8.5 IC50 = 3.2 nM Bind
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
600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12
CHEMBL571203 calrl_human Human No 8.5 IC50 = 3.3 nM Funct
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
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
CHEMBL2024601 calrl_human Human No 8.5 IC50 = 3.4 nM Funct
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
523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1
CHEMBL1770567 calrl_human Human No 8.4 IC50 = 3.6 nM Funct
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
590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2018513 calrl_human Human No 8.4 IC50 = 3.7 nM Bind
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
542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12
CHEMBL2024601 calrl_human Human No 8.4 IC50 = 3.8 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
523 5 3 4 5.1 Cc1cccc(C(Cc2cc(C)c3[nH]ncc3c2)NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)n1
CHEMBL455670 calrl_human Human No 7.5 IC50 = 30 nM Funct
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
518 7 2 7 1.3 CN(C)C(=O)CCCn1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2ccccc21
CHEMBL2024591 calrl_human Human No 7.5 IC50 = 30 nM Funct
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
505 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(c3cc4ccccc4[nH]c3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL237848 calrl_human Human No 7.5 IC50 = 30 nM Funct
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
512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL2022595 calrl_human Human No 7.5 IC50 = 30 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
554 6 3 6 4.9 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2cc(C(=O)O)ccn2)cc2cn[nH]c12
CHEMBL2018356 calrl_human Human No 6.5 IC50 = 300 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
626 8 3 6 3.9 O=C(C[C@H](NCc1ccc2[nH]ncc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL384581 calrl_human Human No 6.5 IC50 = 300 nM Bind
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.
None None None CC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C
CHEMBL407740 calrl_human Human No 5.5 IC50 = 3000 nM Bind
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.
None None None None
CHEMBL440990 calrl_human Human No 5.5 IC50 = 3000 nM Bind
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.
None None None None
CHEMBL403765 calrl_human Human No 6.5 IC50 = 302 nM Funct
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
484 5 2 6 3.8 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL255998 calrl_human Human No 6.5 IC50 = 307 nM Funct
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
478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL453644 calrl_human Human No 7.5 IC50 = 31 nM Funct
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
474 3 2 7 0.4 CN1C(=O)Cn2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3cccc1c32
CHEMBL1162991 calrl_human Human No 7.5 IC50 = 31 nM Funct
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
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
CHEMBL425807 calrl_human Human No 5.5 IC50 = 3100 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
528 4 2 4 3.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2CCNC2=O)CC1
CHEMBL2018494 calrl_human Human No 7.5 IC50 = 32 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL2018494 calrl_human Human No 7.5 IC50 = 32 nM Bind
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
651 8 2 7 4.9 O=C(C[C@H](Nc1ccc(Cl)cc1[N+](=O)[O-])C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL3114456 calrl_human Human No 6.5 IC50 = 320 nM Funct
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
506 7 1 4 4.9 CCCCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL2018515 calrl_human Human No 6.5 IC50 = 320 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
586 6 2 6 3.5 O=C(CC(Cc1ccc2[nH]ncc2c1)C(=O)N1CCC2(CC1)OCCO2)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL405767 calrl_human Human No 4.5 IC50 = 32000 nM Bind
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.
None None None None
CHEMBL1770559 calrl_human Human No 7.5 IC50 = 33 nM Funct
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
589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL3114489 calrl_human Human No 7.5 IC50 = 33 nM Funct
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
632 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1
CHEMBL1092883 calrl_human Human No 7.5 IC50 = 33 nM Funct
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
482 2 1 7 1.4 CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32
CHEMBL2369465 calrl_rat Rat No 7.5 IC50 = 33 nM Bind
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
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL257731 calrl_human Human No 6.5 IC50 = 330 nM Funct
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
450 3 2 7 3.0 Cn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL2059901 calrl_human Human No 6.5 IC50 = 330 nM Bind
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
628 6 2 6 4.4 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL376263 calrl_human Human No 5.5 IC50 = 3300 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
406 3 3 6 1.3 O=C(Cn1c(=O)oc2ccccc21)Nc1ccc2c(c1)CCC1(C2)NC(=O)NC1=O
CHEMBL87174 calrl_human Human No 4.5 IC50 = 33000 nM Bind
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
452 5 1 4 6.2 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc3ccccc23)nc2ccc(OC)cc12
CHEMBL258329 calrl_human Human No 6.5 IC50 = 337 nM Funct
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
462 3 2 6 3.1 Cn1cc(-c2cccc(F)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL424864 calrl_human Human No 7.5 IC50 = 34 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
590 4 2 4 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL1770566 calrl_human Human No 7.5 IC50 = 34 nM Funct
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
583 4 2 6 5.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3ccccc3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2018512 calrl_human Human No 7.5 IC50 = 34 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
529 5 2 5 4.5 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCCCC2)cc2cn[nH]c12
CHEMBL400020 calrl_human Human No 6.5 IC50 = 340 nM Funct
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
466 3 3 5 2.3 O=C1NCC(c2cccc(F)c2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL398575 calrl_human Human No 6.5 IC50 = 340 nM Funct
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
502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL407401 calrl_human Human No 5.5 IC50 = 3400 nM Bind
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.
None None None None
CHEMBL255967 calrl_human Human No 6.5 IC50 = 345 nM Funct
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
518 4 2 7 4.0 O=C(Nc1cc(-c2ccsc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL518422 calrl_human Human No 7.5 IC50 = 35 nM Funct
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
503 4 2 8 2.6 O=C(Cn1c(=O)n(-c2ccncn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL2024171 calrl_human Human No 7.5 IC50 = 35 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
526 6 2 4 5.2 Cc1cc(CC(CC(=O)N2CCC(N3Cc4cccc(F)c4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL219782 calrl_human Human No 6.5 IC50 = 350 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
406 3 2 6 1.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)oc4ccccc43)cc1C2
CHEMBL2371945 calrl_human Human No 5.5 IC50 = 3548.1 nM Funct
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
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)NN(C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL3114483 calrl_human Human No 7.4 IC50 = 36 nM Funct
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
662 9 2 7 4.6 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCN(CCO)CC1
CHEMBL2018489 calrl_human Human No 7.4 IC50 = 36 nM Bind
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
683 7 3 5 5.4 O=C(Nc1ccc(Cl)cc1Cl)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1
CHEMBL256203 calrl_human Human No 6.4 IC50 = 360 nM Funct
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
509 6 2 5 5.0 O=C(Nc1cc(-c2ccccc2)cn(CC2CC2)c1=O)N1CCC(n2cc(-c3ccccc3)[nH]c2=O)CC1
CHEMBL405511 calrl_human Human No 6.4 IC50 = 360 nM Bind
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.
None None None None
CHEMBL384539 calrl_human Human No 6.4 IC50 = 369 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
626 4 2 6 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c4ccccc4ccc32)CC1
CHEMBL383872 calrl_human Human No 7.4 IC50 = 37 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
603 5 2 7 4.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccccn3)nc2O)CC1
CHEMBL556703 calrl_human Human No 7.4 IC50 = 37 nM Funct
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
479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32
CHEMBL564466 calrl_human Human No 7.4 IC50 = 37 nM Funct
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
493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL530116 calrl_human Human No 6.4 IC50 = 370 nM Funct
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
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
CHEMBL3114457 calrl_human Human No 6.4 IC50 = 370 nM Funct
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
506 6 1 4 4.7 CC(C)CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL3114679 calrl_human Human No 6.4 IC50 = 370 nM Funct
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
520 7 1 4 5.1 CC(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL88582 calrl_human Human No 4.4 IC50 = 37000 nM Bind
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
470 5 1 4 6.4 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2Cl)nc2ccc(OC)cc12
CHEMBL214873 calrl_human Human No 6.4 IC50 = 373 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
594 4 2 6 5.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(F)cccc32)CC1
CHEMBL398575 calrl_human Human No 7.4 IC50 = 38 nM Funct
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
502 5 2 5 3.3 O=C(N[C@@H]1CC[C@@H](c2ccccc2)CN(CC2CC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL240904 calrl_human Human No 6.4 IC50 = 380 nM Funct
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
414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1
CHEMBL2018355 calrl_human Human No 6.4 IC50 = 380 nM Bind
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
625 8 3 5 4.5 O=C(C[C@H](NCc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL3974762 calrl_human Human No 6.4 IC50 = 380 nM Funct
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).
537 3 2 5 4.7 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL415186 calrl_human Human No 6.4 IC50 = 380.2 nM Funct
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
1196 28 12 14 -1.7 CC(C)[C@H](NC(=O)N(CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL464079 calrl_human Human Yes 7.4 IC50 = 39 nM Funct
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
494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL374064 calrl_human Human No 7.4 IC50 = 39 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
488 4 2 8 1.9 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnsc4)c4ccccc43)cc1C2
CHEMBL255998 calrl_human Human No 6.4 IC50 = 394 nM Funct
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
478 6 3 8 1.8 COCCn1cc(-c2ccn[nH]2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL1770716 calrl_human Human No 8.4 IC50 = 4 nM Funct
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
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
CHEMBL207197 calrl_human Human Yes 8.4 IC50 = 4 nM Funct
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
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
CHEMBL3114484 calrl_human Human No 8.4 IC50 = 4 nM Funct
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
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
CHEMBL392634 calrl_human Human No 8.4 IC50 = 4 nM Funct
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
597 6 2 7 2.5 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)CN(CCN2CCOCC2)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2059881 calrl_human Human No 8.4 IC50 = 4 nM Bind
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
614 6 3 6 4.7 O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCC(C2CCNCC2)CC1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL2369742 calrl_human Human No 8.4 IC50 = 4 nM Bind
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
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
CHEMBL1770562 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
521 3 2 6 4.2 Cc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL1770565 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2024592 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
509 5 3 4 4.8 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2cn[nH]c12
CHEMBL563727 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23
CHEMBL1092837 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
473 2 2 5 4.1 O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1
CHEMBL517467 calrl_human Human No 8.4 IC50 = 4.1 nM Funct
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
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
CHEMBL1770718 calrl_human Human No 8.4 IC50 = 4.3 nM Funct
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
536 4 2 6 4.0 COCc1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc12
CHEMBL2022596 calrl_human Human No 8.4 IC50 = 4.4 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
568 6 2 7 5.0 COC(=O)c1ccnc(C(Cc2cc(C)c3[nH]ncc3c2)OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c1
CHEMBL2024173 calrl_human Human No 8.4 IC50 = 4.4 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
522 6 2 4 5.3 Cc1cccnc1C(CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)Cc1cc(C)c2[nH]ncc2c1
CHEMBL4113356 calrl_human Human No 8.4 IC50 = 4.5 nM Funct
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).
537 3 2 5 4.7 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL2018520 calrl_human Human No 8.3 IC50 = 4.6 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
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
CHEMBL371646 calrl_human Human No 8.3 IC50 = 4.7 nM Bind
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
855 13 5 8 3.9 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(N(C(N)=O)c2ccccc2)CC1)C(=O)N1CCN(c2ccncc2)CC1
CHEMBL1090847 calrl_human Human No 8.3 IC50 = 4.7 nM Funct
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
446 2 1 4 4.1 O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21
CHEMBL2024597 calrl_human Human No 8.3 IC50 = 4.8 nM Funct
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
560 5 2 5 6.4 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc3ccccc3n2)cc2cn[nH]c12
CHEMBL2430172 calrl_human Human No 8.3 IC50 = 4.8 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
654 5 4 4 5.6 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nc(Br)c(Br)[nH]2)cc2cn[nH]c12
CHEMBL2430184 calrl_human Human No 8.3 IC50 = 4.8 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
512 5 3 5 4.1 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2nccn2C)cc2cn[nH]c12
CHEMBL3114476 calrl_human Human No 7.4 IC50 = 40 nM Funct
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
632 7 1 6 5.2 CN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL404978 calrl_human Human No 5.4 IC50 = 4000 nM Bind
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.
None None None None
CHEMBL451246 calrl_human Human No 4.4 IC50 = 40000 nM Bind
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
713 17 5 5 4.8 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1
CHEMBL487240 calrl_human Human No 5.4 IC50 = 4100 nM Funct
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
491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O
CHEMBL329678 calrl_human Human No 4.4 IC50 = 41000 nM Bind
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
447 6 1 6 5.0 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2cccc([N+](=O)[O-])c2)nc2ccc(OC)cc12
CHEMBL471530 calrl_human Human No 7.4 IC50 = 42 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(Cl)cccc43)cc1C2
CHEMBL465934 calrl_human Human No 6.4 IC50 = 420 nM Funct
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
502 4 2 7 3.2 O=C(Cn1c(=O)n(-c2ccccn2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL488083 calrl_human Human No 6.4 IC50 = 426 nM Funct
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
510 4 2 7 2.5 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2-c1ccccn1
CHEMBL269328 calrl_human Human No 5.4 IC50 = 4275 nM Bind
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.
None None None None
CHEMBL508016 calrl_human Human No 7.4 IC50 = 43 nM Funct
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
490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2
CHEMBL1090841 calrl_human Human No 7.4 IC50 = 43 nM Funct
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
453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2
CHEMBL379548 calrl_human Human No 6.4 IC50 = 430 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
578 4 2 8 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3ncncc32)CC1
CHEMBL2018358 calrl_human Human No 6.4 IC50 = 430 nM Bind
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
636 7 2 5 4.0 O=C(N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)c1ccc(F)c(F)c1
CHEMBL219721 calrl_human Human No 6.4 IC50 = 430 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
467 4 3 6 2.1 O=C(Cn1c(=O)n(-c2ccccc2)c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O
CHEMBL437718 calrl_human Human No 6.4 IC50 = 431 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
686 6 2 7 6.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)(F)F)cc3)nc2O)CC1
CHEMBL198502 calrl_human Human No 7.4 IC50 = 44 nM Bind
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
854 12 4 10 4.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1
CHEMBL3334623 calrl_human Human No 7.4 IC50 = 44 nM Bind
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
854 12 4 10 4.1 NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)oc3ccccc32)CC1)C(=O)N1CCN(c2ccncc2)CC1
CHEMBL487240 calrl_human Human No 7.4 IC50 = 44 nM Funct
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
491 5 3 7 1.2 Cc1cc(C)c2c(c1)n(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)NC(=O)N1C)c(=O)n2CC(=O)O
CHEMBL3114477 calrl_human Human No 7.4 IC50 = 44 nM Funct
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
633 7 2 6 5.5 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCC(O)CC1
CHEMBL3114482 calrl_human Human No 7.4 IC50 = 44 nM Funct
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
674 10 1 6 6.4 CCCCN1CCN(c2ccccc2C2SC(CC(=O)N3CCC(N4Cc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL570793 calrl_human Human No 7.4 IC50 = 44 nM Funct
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
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
CHEMBL1089772 calrl_human Human No 7.4 IC50 = 44 nM Funct
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
481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2
CHEMBL471704 calrl_human Human No 5.4 IC50 = 4400 nM Funct
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
435 4 3 6 1.0 COc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C
CHEMBL386204 calrl_human Human No 6.4 IC50 = 446 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
610 4 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(O)nc3c(Cl)cccc32)CC1
CHEMBL374579 calrl_human Human No 5.4 IC50 = 4466.8 nM Funct
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
949 23 11 12 -2.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCCN1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL3114680 calrl_human Human No 5.4 IC50 = 4470 nM Funct
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
464 4 1 4 3.7 CN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL2018490 calrl_human Human No 7.4 IC50 = 45 nM Bind
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
633 7 3 5 4.2 O=C(Nc1ccccc1F)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1
CHEMBL386701 calrl_human Human No 6.4 IC50 = 450 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
616 6 2 6 5.3 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(Cc3ccccc3)nc2O)CC1
CHEMBL488066 calrl_human Human No 6.4 IC50 = 450 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cccc(Cl)c43)cc1C2
CHEMBL519242 calrl_human Human No 5.4 IC50 = 4500 nM Funct
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
435 4 3 6 1.0 COc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C
CHEMBL262749 calrl_human Human No 5.4 IC50 = 4500 nM Bind
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.
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O)C(C)C
CHEMBL406587 calrl_human Human No 5.4 IC50 = 4500 nM Bind
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.
None None None None
CHEMBL2018357 calrl_human Human No 5.4 IC50 = 4500 nM Bind
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
594 7 3 6 3.2 O=C(C[C@H](NC1CCC(O)CC1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL262961 calrl_human Human No 4.4 IC50 = 45000 nM Bind
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.
None None None None
CHEMBL3114459 calrl_human Human No 5.3 IC50 = 4540 nM Funct
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
532 5 1 4 4.6 O=C(CC1SC(c2ccccc2)N(CC(F)(F)F)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL214507 calrl_human Human No 7.3 IC50 = 46 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
620 5 2 6 5.5 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3cccc(F)c3)nc2O)CC1
CHEMBL3114677 calrl_human Human No 7.3 IC50 = 46 nM Funct
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
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
CHEMBL2018492 calrl_human Human No 7.3 IC50 = 46 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
608 7 2 7 3.8 O=C(C[C@H](Nc1cc(Cl)ncn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL2018516 calrl_human Human No 6.3 IC50 = 460 nM Bind
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
573 5 2 7 3.6 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC4(CC3)OCCO4)CC2)O1
CHEMBL4114031 calrl_human Human No 5.3 IC50 = 4600 nM Funct
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).
487 3 2 5 4.1 O=C(NC1CC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL274851 calrl_human Human No 6.3 IC50 = 470 nM Bind
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.
None None None None
CHEMBL257732 calrl_human Human No 6.3 IC50 = 477 nM Funct
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
462 3 2 6 3.1 Cn1cc(-c2ccccc2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL411078 calrl_human Human No 5.3 IC50 = 4790 nM Bind
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.
None None None None
CHEMBL3971889 calrl_human Human No 6.3 IC50 = 480 nM Funct
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).
503 3 2 6 3.6 O=C(NC1COC(c2ccccc2)Cc2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL3114461 calrl_human Human No 5.3 IC50 = 4880 nM Funct
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
549 9 1 5 4.4 CCN(CC)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL408093 calrl_human Human No 7.3 IC50 = 49 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL408093 calrl_human Human No 7.3 IC50 = 49 nM Funct
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
577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL471706 calrl_human Human No 6.3 IC50 = 490 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2
CHEMBL217867 calrl_human Human No 6.3 IC50 = 490 nM Bind
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.
None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)[C@@H](C)O
CHEMBL258070 calrl_human Human No 6.3 IC50 = 495 nM Funct
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
444 3 2 6 3.0 Cn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL237849 calrl_human Human No 8.3 IC50 = 5 nM Funct
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
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
CHEMBL392937 calrl_human Human No 8.3 IC50 = 5 nM Funct
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
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
CHEMBL392730 calrl_human Human No 8.3 IC50 = 5 nM Funct
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
574 6 2 6 2.5 C[S+]([O-])CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL2059906 calrl_human Human No 8.3 IC50 = 5 nM Bind
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
614 5 3 5 5.1 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@H](Cc3csc4ccccc34)C(=O)N3CCC(N4CCCCC4)CC3)CC2)N1
CHEMBL385454 calrl_human Human No 8.3 IC50 = 5.1 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
632 6 2 7 5.4 COc1cccc(-c2cn(C3CCN(C(=O)N[C@@H]4N=C(c5ccccc5)c5ccccc5N(CC(F)(F)F)C4=O)CC3)c(O)n2)c1
CHEMBL463880 calrl_human Human No 8.3 IC50 = 5.2 nM Funct
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
495 4 2 7 2.8 O=C(Cn1c(=O)n(C2CCOC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL564088 calrl_human Human No 8.3 IC50 = 5.3 nM Funct
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
465 3 3 5 3.0 O=C(CN1CC2CC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL453643 calrl_human Human No 8.3 IC50 = 5.4 nM Funct
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
460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2
CHEMBL453643 calrl_human Human No 8.3 IC50 = 5.4 nM Funct
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
460 3 3 7 0.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n4c5c(cccc53)NC(=O)C4)cc1C2
CHEMBL466192 calrl_human Human No 8.3 IC50 = 5.4 nM Funct
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
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
CHEMBL488082 calrl_human Human No 8.3 IC50 = 5.6 nM Funct
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
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
CHEMBL464079 calrl_human Human Yes 8.2 IC50 = 5.7 nM Funct
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
494 3 2 5 3.1 O=C(CN1C(=O)C2(CCOCC2)c2ccccc21)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL2018509 calrl_human Human No 8.2 IC50 = 5.8 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
600 6 2 6 3.8 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12
CHEMBL2018510 calrl_human Human No 8.2 IC50 = 5.9 nM Bind
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
587 5 2 7 3.9 Cc1cc(CC(CC(=O)N2CCC3(CC2)OC(=O)Nc2ccccc23)C(=O)N2CCC3(CC2)OCCO3)cc2cn[nH]c12
CHEMBL1090846 calrl_human Human No 7.3 IC50 = 50 nM Funct
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
426 2 1 4 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2
CHEMBL220146 calrl_human Human No 7.3 IC50 = 50 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cncnc4)c4ccccc43)cc1C2
CHEMBL374251 calrl_human Human No 7.3 IC50 = 50 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
551 4 2 8 2.3 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4nccc(C(F)(F)F)n4)c4ccccc43)cc1C2
CHEMBL216101 calrl_human Human No 5.3 IC50 = 5000 nM Bind
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.
None None None None
CHEMBL426646 calrl_human Human No 4.3 IC50 = 50000 nM Bind
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
685 15 5 5 5.1 NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)Nc1ccccc1
CHEMBL410450 calrl_human Human No 4.3 IC50 = 51000 nM Bind
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.
None None None None
CHEMBL3114454 calrl_human Human No 5.3 IC50 = 5150 nM Funct
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
490 5 1 4 4.2 O=C(CC1SC(c2ccccc2)N(C2CC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL3114464 calrl_human Human No 6.3 IC50 = 520 nM Funct
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
534 6 1 5 4.2 O=C(CC1SC(c2ccccc2)N(CC2CCCO2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL429803 calrl_human Human No 6.3 IC50 = 520 nM Funct
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
448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL314992 calrl_human Human No 5.3 IC50 = 5200 nM Bind
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
470 5 1 4 6.1 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(C(F)(F)F)cc2)nc2ccc(OC)cc12
CHEMBL2018514 calrl_human Human No 7.3 IC50 = 53 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
598 6 2 6 4.7 O=C1Nc2ccccc2C2(CCN(C(=O)CC(Cc3ccc4[nH]ncc4c3)C(=O)N3CCC(N4CCCCC4)CC3)CC2)O1
CHEMBL223156 calrl_human Human No 6.3 IC50 = 530 nM Funct
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
482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2
CHEMBL556703 calrl_human Human No 6.3 IC50 = 530 nM Funct
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
479 3 2 5 3.0 CN1C(=O)C[C@@H]2CN(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c32
CHEMBL223156 calrl_human Human No 6.3 IC50 = 530 nM Funct
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
482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2
CHEMBL223156 calrl_human Human No 6.3 IC50 = 530 nM Funct
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
482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2
CHEMBL385322 calrl_human Human No 6.3 IC50 = 530 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
405 3 3 6 0.7 Cn1c(=O)n(CC(=O)Nc2ccc3c(c2)CC2(C3)NC(=O)NC2=O)c2ccccc21
CHEMBL220715 calrl_human Human No 7.3 IC50 = 54 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
512 5 2 8 1.9 COc1cccc(-n2c(=O)n(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)NC(=O)N3C)c3ccccc32)n1
CHEMBL256813 calrl_human Human No 6.3 IC50 = 540 nM Funct
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
494 6 2 8 3.1 COCCn1cc(-c2ccsc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL572114 calrl_human Human No 7.3 IC50 = 55 nM Funct
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
516 3 2 4 2.4 O=C1CC2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)C(=O)N1
CHEMBL402887 calrl_human Human No 6.3 IC50 = 550 nM Funct
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
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
CHEMBL419684 calrl_human Human No 5.3 IC50 = 5500 nM Bind
Compound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligandCompound was tested in vitro for its binding affinity towards recombinant human Calcitonin gene-related peptide type receptor (membranes of HEK293 cells) using [125I]hCGRP as radioligand
436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12
CHEMBL382469 calrl_rat Rat No 7.3 IC50 = 56.7 nM Bind
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
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
CHEMBL445069 calrl_human Human No 6.3 IC50 = 567 nM Funct
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
480 3 2 6 3.2 Cn1cc(-c2cccc(F)c2F)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL480999 calrl_human Human No 7.2 IC50 = 57 nM Funct
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
474 3 2 5 1.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)CN3C(=O)C4(CCOCC4)c4ccccc43)cc1C2
CHEMBL4108361 calrl_human Human No 6.2 IC50 = 570 nM Funct
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).
555 3 2 5 5.2 O=C(N[C@H]1CC[C@H](c2cccc(F)c2F)[C@H](F)c2cccnc21)c1cnc2c(c1)C[C@@]1(C2)C(=O)Nc2ncccc21
CHEMBL435149 calrl_human Human No 5.2 IC50 = 5754.4 nM Funct
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
1196 28 12 14 -1.4 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL438426 calrl_human Human No 6.2 IC50 = 588.8 nM Funct
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
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)N(N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL471359 calrl_human Human No 7.2 IC50 = 59 nM Funct
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
419 3 3 5 1.3 Cc1cccc2c1[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C
CHEMBL2018498 calrl_human Human No 7.2 IC50 = 59 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
611 7 3 5 4.9 O=C(C[C@H](Nc1ccc2[nH]ccc2c1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL471705 calrl_human Human No 6.2 IC50 = 590 nM Funct
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
419 3 3 5 1.3 Cc1ccc2c(c1)[nH]c(=O)n2CC(=O)Nc1ccc2c(c1)C[C@]1(C2)C(=O)NC(=O)N1C
CHEMBL2018359 calrl_human Human No 6.2 IC50 = 590 nM Bind
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
596 6 2 6 3.8 CC(C)(C)OC(=O)N[C@@H](CC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1)C(=O)N1CCC(N2CCCCC2)CC1
CHEMBL419684 calrl_human Human No 5.2 IC50 = 5900 nM Bind
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
436 5 1 4 5.7 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc(Cl)cc2)nc2ccc(OC)cc12
CHEMBL2024588 calrl_human Human No 8.2 IC50 = 6 nM Funct
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
538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12
CHEMBL237848 calrl_human Human No 8.2 IC50 = 6 nM Funct
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
512 4 2 5 3.1 CCN1C[C@H](c2cccc(F)c2F)CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C1=O
CHEMBL238276 calrl_human Human No 8.2 IC50 = 6 nM Funct
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
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
CHEMBL3904139 calrl_human Human No 8.2 IC50 = 6.3 nM Funct
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).
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
CHEMBL197529 calrl_rat Rat No 8.2 IC50 = 6.4 nM Bind
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
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
CHEMBL564487 calrl_human Human No 8.2 IC50 = 6.5 nM Funct
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
479 3 3 5 3.1 CC12CC(=O)Nc3cccc(c31)N(CC(=O)Nc1ccc3c(c1)C[C@]1(C3)C(=O)Nc3ncccc31)C2
CHEMBL1092838 calrl_human Human No 8.2 IC50 = 6.5 nM Funct
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
467 2 2 5 2.9 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2
CHEMBL2023185 calrl_human Human No 8.2 IC50 = 6.6 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
607 7 2 6 6.2 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCCC3)n[nH]c12
CHEMBL1770558 calrl_human Human No 8.2 IC50 = 6.7 nM Funct
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
507 3 2 6 3.9 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2ccnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2018520 calrl_human Human No 8.2 IC50 = 6.7 nM Bind
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
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
CHEMBL2369458 calrl_rat Rat No 8.2 IC50 = 6.8 nM Bind
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
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL2023187 calrl_human Human No 8.2 IC50 = 6.8 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
593 7 2 6 5.8 Cc1cc(CC(OC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccccn2)cc2c(CN3CCCC3)n[nH]c12
CHEMBL2018513 calrl_human Human No 8.2 IC50 = 6.9 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
542 6 2 4 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCCCC2)cc2cn[nH]c12
CHEMBL2369458 calrl_human Human No 8.2 IC50 = 6.9 nM Bind
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
None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)[C@@H](C)O)C(C)C)C(C)C)C(C)C
CHEMBL471706 calrl_human Human No 7.2 IC50 = 60 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4cc(Cl)ccc43)cc1C2
CHEMBL3114474 calrl_human Human No 7.2 IC50 = 60 nM Funct
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
618 7 2 6 4.9 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1N1CCNCC1
CHEMBL571459 calrl_human Human No 7.2 IC50 = 60 nM Funct
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
566 3 2 4 4.9 O=C1Nc2ccccc2C2(CCN(C(=O)N[C@@H]3CC[C@@H](c4cccc(F)c4F)CN(CC(F)(F)F)C3=O)CC2)O1
CHEMBL220101 calrl_human Human No 7.2 IC50 = 61 nM Funct
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
475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2
CHEMBL220101 calrl_human Human No 7.2 IC50 = 61 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
475 4 2 7 1.4 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCOC4)c4ccccc43)cc1C2
CHEMBL212942 calrl_human Human No 6.2 IC50 = 616 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cccnc3NC2=O)CC1
CHEMBL3114479 calrl_human Human No 7.2 IC50 = 62 nM Funct
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
600 7 1 6 5.7 CC(C)(C)CCN1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1-n1cccn1
CHEMBL240904 calrl_human Human No 6.2 IC50 = 620 nM Funct
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
414 3 3 5 1.6 CC(C)C1CC[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)C(=O)NC1
CHEMBL265906 calrl_human Human No 6.2 IC50 = 620 nM Bind
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.
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O
CHEMBL377252 calrl_human Human No 6.2 IC50 = 627 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
591 4 2 5 4.4 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(N2Cc3cnccc3NC2=O)CC1
CHEMBL487244 calrl_human Human No 7.2 IC50 = 64 nM Funct
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
439 3 3 5 1.6 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4ccc(Cl)cc43)cc1C2
CHEMBL1770567 calrl_human Human No 7.2 IC50 = 64 nM Funct
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
590 4 2 8 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2c(-c3nccs3)cnc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL223756 calrl_human Human No 7.2 IC50 = 64 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4cnccn4)c4ccccc43)cc1C2
CHEMBL375224 calrl_human Human No 7.2 IC50 = 64 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
523 4 2 8 0.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(C4CCS(=O)(=O)C4)c4ccccc43)cc1C2
CHEMBL3114493 calrl_human Human No 7.2 IC50 = 65 nM Funct
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
664 7 1 6 5.4 CN1CCN(c2cccc(F)c2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL239630 calrl_human Human No 7.2 IC50 = 65 nM Funct
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
466 3 3 5 2.3 O=C1NC[C@H](c2ccccc2F)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL3910081 calrl_human Human No 7.2 IC50 = 65 nM Funct
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).
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
CHEMBL386824 calrl_human Human No 5.2 IC50 = 6500 nM Bind
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.
None None None None
CHEMBL255755 calrl_human Human No 6.2 IC50 = 651 nM Funct
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
513 4 2 7 3.4 O=C(Nc1cc(-c2cccnc2)cn(CC(F)(F)F)c1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL402844 calrl_human Human No 6.2 IC50 = 665 nM Funct
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
488 6 2 7 3.1 COCCn1cc(-c2ccccc2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL563727 calrl_human Human No 7.2 IC50 = 67 nM Funct
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
477 3 2 5 3.2 CN1C(=O)Cc2cn(CC(=O)Nc3ccc4c(c3)C[C@]3(C4)C(=O)Nc4ncccc43)c3cccc1c23
CHEMBL413872 calrl_human Human No 7.2 IC50 = 67.6 nM Funct
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
1196 28 13 14 -1.7 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NNC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL213670 calrl_human Human No 6.2 IC50 = 672 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
526 4 2 6 3.7 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2ccnc2O)CC1
CHEMBL223805 calrl_human Human No 6.2 IC50 = 690 nM Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
391 3 4 5 0.6 O=C(Cn1c(=O)[nH]c2ccccc21)Nc1ccc2c(c1)CC1(C2)NC(=O)NC1=O
CHEMBL415812 calrl_human Human No 5.2 IC50 = 6900 nM Bind
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.
None None None None
CHEMBL577320 calrl_human Human No 6.2 IC50 = 692 nM Funct
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
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
CHEMBL1770559 calrl_human Human No 8.1 IC50 = 7.2 nM Funct
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
589 4 2 6 5.0 O=C(N[C@@H]1CC[C@@H](c2cccc(F)c2F)Cn2cc(CC(F)(F)F)nc21)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL564466 calrl_human Human No 8.1 IC50 = 7.2 nM Funct
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
493 3 3 5 3.7 O=C(CN1CC2CCCC(=O)Nc3cccc1c32)Nc1ccc2c(c1)C[C@]1(C2)C(=O)Nc2ncccc21
CHEMBL1089772 calrl_human Human No 8.1 IC50 = 7.2 nM Funct
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
481 3 2 5 3.3 CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2
CHEMBL1090841 calrl_human Human No 8.1 IC50 = 7.3 nM Funct
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
453 2 2 5 2.7 CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2
CHEMBL1770565 calrl_human Human No 8.1 IC50 = 7.4 nM Funct
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
578 4 2 7 3.6 CN(C)C(=O)c1cnc2n1C[C@H](c1cccc(F)c1F)CC[C@H]2NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2430173 calrl_human Human No 8.1 IC50 = 7.4 nM Funct
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP productionAntagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
576 5 4 4 4.9 Cc1cc(CC(NC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ncc(Br)[nH]2)cc2cn[nH]c12
CHEMBL1770563 calrl_human Human No 8.1 IC50 = 7.9 nM Funct
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
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
CHEMBL2024588 calrl_human Human No 8.1 IC50 = 7.9 nM Bind
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
538 7 3 5 4.5 Cc1cc(CC(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)c2ccc(CO)cn2)cc2cn[nH]c12
CHEMBL429803 calrl_human Human No 6.2 IC50 = 700 nM Funct
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
448 3 3 5 2.1 O=C1NC[C@H](c2ccccc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL2018354 calrl_human Human No 6.2 IC50 = 700 nM Bind
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
587 8 2 6 3.4 O=C(C[C@H](NCc1ccccn1)C(=O)N1CCC(N2CCCCC2)CC1)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL428096 calrl_human Human No 5.2 IC50 = 7000 nM Bind
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.
None None None None
CHEMBL266666 calrl_human Human No 4.2 IC50 = 70000 nM Bind
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.
None None None None
CHEMBL198925 calrl_rat Rat No 4.2 IC50 = 70500 nM Bind
Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40Affinity against calcitonin gene related peptide receptor (1 uM) in rat spleen using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
787 15 5 8 3.7 COc1cccc(CCNC(=O)N[C@@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)c1
CHEMBL376719 calrl_human Human No 6.2 IC50 = 708.0 nM Funct
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
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL3114463 calrl_human Human No 6.2 IC50 = 710 nM Funct
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
532 5 1 4 5.4 O=C(CC1SC(c2ccccc2)N(C2CCCCC2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL405543 calrl_human Human No 6.2 IC50 = 715 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
620 5 3 7 4.6 O=C(O)c1ccc2c(c1)nc(O)n2C1CCN(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(F)(F)F)C2=O)CC1
CHEMBL270175 calrl_human Human No 6.2 IC50 = 715 nM Funct
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
460 3 3 7 2.7 Cn1cc(-c2cccc(O)c2)cc(NC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)c1=O
CHEMBL488255 calrl_human Human No 7.1 IC50 = 72 nM Funct
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
519 5 2 8 1.8 COC(=O)[C@H](C)n1c(=O)n(CC(=O)Nc2ccc3c(c2)C[C@]2(C3)C(=O)NC(=O)N2C)c2cc(C)cc(C)c21
CHEMBL3114492 calrl_human Human No 7.1 IC50 = 72 nM Funct
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
664 7 1 6 5.4 CN1CCN(c2ccc(F)cc2C2SC(CC(=O)N3CCC(N4CCc5ccccc5NC4=O)CC3)C(=O)N2CCC(C)(C)C)CC1
CHEMBL2018497 calrl_human Human No 7.1 IC50 = 73 nM Bind
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
629 7 3 9 2.7 Cc1nc(N[C@@H](CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCCCC3)CC2)nc2nn[nH]c12
CHEMBL408093 calrl_human Human No 6.1 IC50 = 730 nM Funct
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
577 4 2 6 3.8 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL386757 calrl_human Human No 7.1 IC50 = 74 nM Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
668 7 2 7 6.0 O=C(N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O)N1CCC(n2cc(-c3ccc(OC(F)F)cc3)nc2O)CC1
CHEMBL482178 calrl_human Human No 7.1 IC50 = 74 nM Funct
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
483 4 2 8 1.2 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccncn4)c4ccccc43)cc1C2
CHEMBL3114678 calrl_human Human No 6.1 IC50 = 740 nM Funct
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
662 9 2 4 6.1 CC(C)CCN(Cc1cc(Br)c(O)c(Br)c1)C(=O)CCC(=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL88111 calrl_human Human No 4.1 IC50 = 74000 nM Bind
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
446 5 1 6 4.8 CCC1CN2CCC1CC2[C@H](O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(OC)cc12
CHEMBL3114467 calrl_human Human No 6.1 IC50 = 750 nM Funct
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
558 6 1 4 5.4 O=C(CC1SC(c2ccccc2)N(Cc2ccc(F)cc2)C1=O)N1CCC(N2Cc3ccccc3NC2=O)CC1
CHEMBL240686 calrl_human Human No 6.1 IC50 = 750 nM Funct
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
454 3 3 6 2.2 O=C1NCC(c2ccsc2)CC[C@H]1NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1
CHEMBL470321 calrl_human Human No 7.1 IC50 = 76 nM Funct
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
423 3 3 5 1.1 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)[nH]c4c(F)cccc43)cc1C2
CHEMBL508016 calrl_human Human No 7.1 IC50 = 76 nM Funct
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
490 7 3 7 0.7 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(CCCC(N)=O)c4ccccc43)cc1C2
CHEMBL3114458 calrl_human Human No 5.1 IC50 = 7600 nM Funct
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
506 4 1 4 4.9 CC(C)(C)N1C(=O)C(CC(=O)N2CCC(N3Cc4ccccc4NC3=O)CC2)SC1c1ccccc1
CHEMBL223642 calrl_human Human No 6.1 IC50 = 776.3 nM Funct
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
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1)[C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL223156 calrl_human Human No 7.1 IC50 = 78 nM Funct
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
482 4 2 7 1.8 CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2
CHEMBL223156 calrl_human Human No 7.1 IC50 = 78 nM Funct
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
482 4