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 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
627 6 3 5 3.5 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL207197 calrl_human Human Yes 10.6 EC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL207197 calrl_human Human Yes 10.6 EC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL450668 calrl_human Human Yes 10.5 EC50 = 0.0 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
645 6 3 6 3.6 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)NC(=O)N5CCC(CC5)N6CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL450668 calrl_human Human Yes 10.5 EC50 = 0.0 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
645 6 3 6 3.6 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)NC(=O)N5CCC(CC5)N6CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL2178422 calrl_human Human Yes 9.9 EC50 = 0.1 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
535 4 2 8 2.3 C1CC(C2=C(C=CC=N2)C(C1C3=C(C(=CC=C3)F)F)N)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL3288288 calrl_human Human No 9.8 EC50 = 0.2 Funct
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
884 12 5 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL3288288 calrl_human Human No 9.8 EC50 = 0.2 Funct
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
884 12 5 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL412994 calrl_human Human No 9.7 EC50 = 0.2 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
3791 124 59 57 -15.7 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL412994 calrl_human Human No 9.7 EC50 = 0.2 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
3791 124 59 57 -15.7 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL3288290 calrl_human Human No 7.0 EC50 = 100 Funct
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
766 12 4 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL3288290 calrl_human Human No 7.0 EC50 = 100 Funct
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
766 12 4 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL2059896 calrl_human Human No 7.9 EC50 = 12 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 2 5 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CC(=O)NC7=CC=CC=C67
CHEMBL2059896 calrl_human Human No 7.9 EC50 = 12 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 2 5 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CC(=O)NC7=CC=CC=C67
CHEMBL2059900 calrl_human Human No 7.9 EC50 = 13 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
627 6 2 6 4.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=CC=C7
CHEMBL2059900 calrl_human Human No 7.9 EC50 = 13 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
627 6 2 6 4.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=CC=C7
CHEMBL2059898 calrl_human Human No 6.9 EC50 = 130 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 2 5 4.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CNC(=O)C7=CC=CC=C67
CHEMBL2059898 calrl_human Human No 6.9 EC50 = 130 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 2 5 4.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CNC(=O)C7=CC=CC=C67
CHEMBL2059897 calrl_human Human No 7.8 EC50 = 15 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 2 5 4.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7CC(=O)N6
CHEMBL2059897 calrl_human Human No 7.8 EC50 = 15 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 2 5 4.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7CC(=O)N6
CHEMBL2059906 calrl_human Human No 8.5 EC50 = 3 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 3 5 4.1 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)N6
CHEMBL2059906 calrl_human Human No 8.5 EC50 = 3 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 3 5 4.1 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)N6
CHEMBL2059905 calrl_human Human No 7.5 EC50 = 31 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
616 5 2 6 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL2059905 calrl_human Human No 7.5 EC50 = 31 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
616 5 2 6 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL3288289 calrl_human Human No 7.0 EC50 = 96 Funct
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
752 12 4 8 3.2 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL3288289 calrl_human Human No 7.0 EC50 = 96 Funct
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
752 12 4 8 3.2 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL452966 calrl_human Human No 11.0 IC50 = 0.0 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
628 7 2 6 4.1 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL452966 calrl_human Human No 11.0 IC50 = 0.0 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
628 7 2 6 4.1 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL508453 calrl_human Human No 11.0 IC50 = 0.0 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
646 7 2 7 4.2 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL508453 calrl_human Human No 11.0 IC50 = 0.0 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
646 7 2 7 4.2 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL508215 calrl_human Human No 10.8 IC50 = 0.0 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
625 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL508215 calrl_human Human No 10.8 IC50 = 0.0 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
625 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018517 calrl_human Human No 10.7 IC50 = 0.0 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018517 calrl_human Human No 10.7 IC50 = 0.0 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2022601 calrl_human Human No 10.7 IC50 = 0.0 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
608 8 2 6 4.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL447297 calrl_human Human No 10.7 IC50 = 0.0 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
625 7 2 6 4.9 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL207197 calrl_human Human Yes 10.7 IC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2022601 calrl_human Human No 10.7 IC50 = 0.0 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
608 8 2 6 4.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL447297 calrl_human Human No 10.7 IC50 = 0.0 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
625 7 2 6 4.9 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL207197 calrl_human Human Yes 10.7 IC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL451164 calrl_human Human No 10.7 IC50 = 0.0 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
646 7 2 7 4.2 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=C(C=C(C=C7)F)NC6=O)C=NN2
CHEMBL451164 calrl_human Human No 10.7 IC50 = 0.0 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
646 7 2 7 4.2 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=C(C=C(C=C7)F)NC6=O)C=NN2
CHEMBL450668 calrl_human Human Yes 10.6 IC50 = 0.0 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
645 6 3 6 3.6 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)NC(=O)N5CCC(CC5)N6CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL197529 calrl_human Human No 10.5 IC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL207197 calrl_human Human Yes 10.5 IC50 = 0.0 Funct
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL197529 calrl_human Human No 10.5 IC50 = 0.0 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL207197 calrl_human Human Yes 10.5 IC50 = 0.0 Funct
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2022606 calrl_human Human No 10.4 IC50 = 0.0 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
619 8 2 6 5.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022606 calrl_human Human No 10.4 IC50 = 0.0 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
619 8 2 6 5.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2369459 calrl_human Human No 10.4 IC50 = 0.0 Funct
Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor
3789 110 55 57 -15.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)O)CC(=O)O)NC(=O)C(C)N)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C(C)C)C(=O)N4CCCC4C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC5=CC=CC=C5)C(=O)N)C(C)O
CHEMBL2369459 calrl_human Human No 10.4 IC50 = 0.0 Funct
Displacement of radiolabeled CGRPalpha from human CGRP receptorDisplacement of radiolabeled CGRPalpha from human CGRP receptor
3789 110 55 57 -15.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)O)CC(=O)O)NC(=O)C(C)N)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C(C)C)C(=O)N4CCCC4C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC5=CC=CC=C5)C(=O)N)C(C)O
CHEMBL501603 calrl_human Human No 10.4 IC50 = 0.0 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
625 6 2 6 4.4 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC4(CCN(CC4)C)CC3)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL501603 calrl_human Human No 10.4 IC50 = 0.0 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
625 6 2 6 4.4 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC4(CCN(CC4)C)CC3)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018507 calrl_human Human No 10.3 IC50 = 0.0 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
638 8 2 5 3.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4C=C(NC4=O)C5=CC=CC=C5)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018507 calrl_human Human No 10.3 IC50 = 0.0 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
638 8 2 5 3.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4C=C(NC4=O)C5=CC=CC=C5)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL408415 calrl_human Human No 10.3 IC50 = 0.1 Funct
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
882 13 5 8 3.4 C1CN(CCC1N2C=C(NC2=O)C3=CC=CC=C3)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL408415 calrl_human Human No 10.3 IC50 = 0.1 Funct
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
882 13 5 8 3.4 C1CN(CCC1N2C=C(NC2=O)C3=CC=CC=C3)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL499488 calrl_human Human No 10.3 IC50 = 0.1 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
623 7 2 6 4.6 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCC=CC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL499488 calrl_human Human No 10.3 IC50 = 0.1 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
623 7 2 6 4.6 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCC=CC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL452686 calrl_human Human No 10.2 IC50 = 0.1 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
643 7 2 7 4.8 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL452686 calrl_human Human No 10.2 IC50 = 0.1 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
643 7 2 7 4.8 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=C(C(=CC=C7)F)NC6=O)C=NN2
CHEMBL197529 calrl_human Human No 10.2 IC50 = 0.1 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2018517 calrl_human Human No 10.2 IC50 = 0.1 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL197529 calrl_human Human No 10.2 IC50 = 0.1 Funct
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
870 12 5 8 3.1 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2018517 calrl_human Human No 10.2 IC50 = 0.1 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL508349 calrl_human Human No 10.2 IC50 = 0.1 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
620 7 2 7 3.8 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4=CC=NC=C4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL508349 calrl_human Human No 10.2 IC50 = 0.1 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
620 7 2 7 3.8 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4=CC=NC=C4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2023189 calrl_human Human No 10.2 IC50 = 0.1 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
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2023189 calrl_human Human No 10.2 IC50 = 0.1 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
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2018504 calrl_human Human No 10.2 IC50 = 0.1 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018504 calrl_human Human No 10.2 IC50 = 0.1 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL502243 calrl_human Human No 10.2 IC50 = 0.1 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
640 8 2 6 4.4 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6C=C(NC6=O)C7=CC=CC=C7)C=NN2
CHEMBL502243 calrl_human Human No 10.2 IC50 = 0.1 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
640 8 2 6 4.4 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)N6C=C(NC6=O)C7=CC=CC=C7)C=NN2
CHEMBL2023191 calrl_human Human No 10.2 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
603 7 2 7 3.3 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C=NN2
CHEMBL2023191 calrl_human Human No 10.2 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
603 7 2 7 3.3 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C=NN2
CHEMBL2018504 calrl_human Human No 10.1 IC50 = 0.1 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018504 calrl_human Human No 10.1 IC50 = 0.1 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL1092882 calrl_human Human No 10.1 IC50 = 0.1 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
489 2 2 5 1.7 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=C8C(=CC=C7)NC(=O)CN8C6=O
CHEMBL1092882 calrl_human Human No 10.1 IC50 = 0.1 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
489 2 2 5 1.7 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=C8C(=CC=C7)NC(=O)CN8C6=O
CHEMBL2023189 calrl_human Human No 10.1 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2023189 calrl_human Human No 10.1 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2430167 calrl_human Human No 10.1 IC50 = 0.1 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
638 7 3 5 4.1 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC(=NC(=C4)Cl)C)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018519 calrl_human Human No 10.1 IC50 = 0.1 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 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018519 calrl_human Human No 10.1 IC50 = 0.1 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 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018505 calrl_human Human No 10.1 IC50 = 0.1 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 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018505 calrl_human Human No 10.1 IC50 = 0.1 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 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2023190 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
630 7 2 6 4.5 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)N5CCC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2023190 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
630 7 2 6 4.5 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)N5CCC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022606 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
619 8 2 6 5.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022606 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
619 8 2 6 5.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2431248 calrl_human Human No 10.0 IC50 = 0.1 Funct
Antagonist activity at CGRP receptor (unknown origin) by cell based cAMP assayAntagonist activity at CGRP receptor (unknown origin) by cell based cAMP assay
586 4 2 7 3.4 CC1(CN(C2(CCCC2)C(=O)N1CC(=O)NC3=CC4=C(CC5(C4)C6=C(NC5=O)N=CC=C6)C=C3)C)C7=CC(=CC(=C7)F)F
CHEMBL2022600 calrl_human Human No 10.0 IC50 = 0.1 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
622 7 2 6 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022600 calrl_human Human No 10.0 IC50 = 0.1 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
622 7 2 6 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022603 calrl_human Human No 10.0 IC50 = 0.1 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 6 4.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022601 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
608 8 2 6 4.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022603 calrl_human Human No 10.0 IC50 = 0.1 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 6 4.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022601 calrl_human Human No 10.0 IC50 = 0.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
608 8 2 6 4.3 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018508 calrl_human Human No 9.9 IC50 = 0.1 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
623 7 2 5 4.2 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL585568 calrl_human Human No 9.9 IC50 = 0.1 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
531 4 2 6 3.7 CC1(CCC(N(C1=O)CC(=O)NC2=CC3=C(CC4(C3)C5=C(NC4=O)N=CC=C5)C=C2)C6=C(C=CC=C6F)F)C
CHEMBL2018508 calrl_human Human No 9.9 IC50 = 0.1 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
623 7 2 5 4.2 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL585568 calrl_human Human No 9.9 IC50 = 0.1 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
531 4 2 6 3.7 CC1(CCC(N(C1=O)CC(=O)NC2=CC3=C(CC4(C3)C5=C(NC4=O)N=CC=C5)C=C2)C6=C(C=CC=C6F)F)C
CHEMBL507893 calrl_human Human No 9.9 IC50 = 0.1 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
637 7 2 7 5.0 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4=CC=C(C=C4)F)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2430169 calrl_human Human No 9.9 IC50 = 0.1 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
604 7 3 5 3.1 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC(=NC=C4)C)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL507893 calrl_human Human No 9.9 IC50 = 0.1 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
637 7 2 7 5.0 CC1=C2C(=CC(=C1)CC(C(=O)N3CCN(CC3)C4=CC=C(C=C4)F)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018507 calrl_human Human No 9.8 IC50 = 0.2 Funct
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
638 8 2 5 3.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4C=C(NC4=O)C5=CC=CC=C5)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018507 calrl_human Human No 9.8 IC50 = 0.2 Funct
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
638 8 2 5 3.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4C=C(NC4=O)C5=CC=CC=C5)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2022603 calrl_human Human No 9.8 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 6 4.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022603 calrl_human Human No 9.8 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 6 4.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL499810 calrl_human Human No 9.7 IC50 = 0.2 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
609 7 1 6 5.5 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7C=N6)C=NN2
CHEMBL2018505 calrl_human Human No 9.7 IC50 = 0.2 Funct
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
644 7 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL499810 calrl_human Human No 9.8 IC50 = 0.2 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
609 7 1 6 5.5 CC1=C2C(=CC(=C1)CC(C(=O)N3CCC(CC3)N4CCCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7C=N6)C=NN2
CHEMBL2018505 calrl_human Human No 9.8 IC50 = 0.2 Funct
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
644 7 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2430177 calrl_human Human No 9.7 IC50 = 0.2 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
645 8 3 4 5.4 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=C(C=C4)C(C)(C)C)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL382469 calrl_human Human No 9.7 IC50 = 0.2 Funct
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
856 12 5 8 3.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2018519 calrl_human Human No 9.7 IC50 = 0.2 Funct
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
644 7 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL382469 calrl_human Human No 9.7 IC50 = 0.2 Funct
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
856 12 5 8 3.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL2018519 calrl_human Human No 9.7 IC50 = 0.2 Funct
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
644 7 2 6 3.6 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL1770729 calrl_human Human No 9.7 IC50 = 0.2 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
593 3 2 8 2.4 CC1(CCCO1)C2=CN=C3N2CC(CCC3NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL2024603 calrl_human Human No 9.7 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
539 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C=O)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL1770729 calrl_human Human No 9.7 IC50 = 0.2 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
593 3 2 8 2.4 CC1(CCCO1)C2=CN=C3N2CC(CCC3NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL2024603 calrl_human Human No 9.7 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
539 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C=O)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2063115 calrl_human Human No 9.7 IC50 = 0.2 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
520 4 1 7 3.7 C1CC(C2=C(CC1C3=C(C(=CC=C3)F)F)C=CC=N2)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL2063115 calrl_human Human No 9.7 IC50 = 0.2 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
520 4 1 7 3.7 C1CC(C2=C(CC1C3=C(C(=CC=C3)F)F)C=CC=N2)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL2430166 calrl_human Human No 9.7 IC50 = 0.2 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
634 7 2 6 4.8 CC1=C2C(=CC(=C1)CC(C3=NC=C4N3CCN(C4)C5CCCCC5)OC(=O)N6CCC(CC6)C7=CC8=CC=CC=C8NC7=O)C=NN2
CHEMBL2035983 calrl_human Human No 9.6 IC50 = 0.2 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
573 4 3 8 1.9 CC1(CNC2(CCCC2)C(=O)N1CC(=O)NC3=CN=C4CC5(CC4=C3)C6=C(NC5=O)N=CC=C6)C7=CC(=CC(=C7)F)F
CHEMBL2035983 calrl_human Human No 9.6 IC50 = 0.2 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
573 4 3 8 1.9 CC1(CNC2(CCCC2)C(=O)N1CC(=O)NC3=CN=C4CC5(CC4=C3)C6=C(NC5=O)N=CC=C6)C7=CC(=CC(=C7)F)F
CHEMBL1770724 calrl_human Human No 9.6 IC50 = 0.2 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
581 4 2 8 2.3 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2022604 calrl_human Human No 9.6 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
591 8 2 6 4.6 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022609 calrl_human Human No 9.6 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 7 2 5 5.2 CC1=CC(=CC2=C(NN=C12)C3=CC=CC=C3)CC(C4=CC=CC=N4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O
CHEMBL1770724 calrl_human Human No 9.6 IC50 = 0.2 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
581 4 2 8 2.3 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2022604 calrl_human Human No 9.6 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
591 8 2 6 4.6 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022609 calrl_human Human No 9.6 IC50 = 0.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 7 2 5 5.2 CC1=CC(=CC2=C(NN=C12)C3=CC=CC=C3)CC(C4=CC=CC=N4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O
CHEMBL1770728 calrl_human Human No 9.6 IC50 = 0.3 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
609 6 2 8 3.4 CCC(CC)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL1770728 calrl_human Human No 9.6 IC50 = 0.3 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
609 6 2 8 3.4 CCC(CC)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2430165 calrl_human Human No 9.6 IC50 = 0.3 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
642 8 2 6 4.5 CC1=C2C(=CC(=C1)CC(C3=NC=C4N3CCN(C4)CC5=CC=CC=C5)OC(=O)N6CCC(CC6)C7=CC8=CC=CC=C8NC7=O)C=NN2
CHEMBL2022599 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 7 2 6 4.1 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C4=CC=NC=C4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022599 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 7 2 6 4.1 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C4=CC=NC=C4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024603 calrl_human Human No 9.6 IC50 = 0.3 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
539 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C=O)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL2023188 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022600 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
622 7 2 6 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024603 calrl_human Human No 9.6 IC50 = 0.3 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
539 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C=O)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.6 IC50 = 0.3 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL2023188 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022600 calrl_human Human No 9.6 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
622 7 2 6 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N4CCCCC4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2018508 calrl_human Human No 9.5 IC50 = 0.3 Funct
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
623 7 2 5 4.2 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL3114495 calrl_human Human No 9.5 IC50 = 0.3 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
693 9 1 7 5.7 CC(C)N1CCN(CC1)C2=C(C=CC=C2F)C3N(C(=O)C(S3)CC(=O)N4CCC(CC4)N5CCC6=CC=CC=C6NC5=O)CCC(C)(C)C
CHEMBL2018508 calrl_human Human No 9.5 IC50 = 0.3 Funct
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
623 7 2 5 4.2 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL1770715 calrl_human Human No 9.5 IC50 = 0.3 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 5 2 7 2.2 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL1770715 calrl_human Human No 9.5 IC50 = 0.3 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 5 2 7 2.2 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL1770726 calrl_human Human No 9.5 IC50 = 0.3 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
595 5 2 8 2.7 CCOC(C)(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770726 calrl_human Human No 9.5 IC50 = 0.3 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
595 5 2 8 2.7 CCOC(C)(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL2018503 calrl_human Human No 9.5 IC50 = 0.3 Funct
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
613 6 2 6 3.7 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2022598 calrl_human Human No 9.5 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
582 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N(C)C)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022607 calrl_human Human No 9.5 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 6 2 5 4.6 CC1=CC(=CC2=C(NN=C12)Br)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL2018503 calrl_human Human No 9.5 IC50 = 0.3 Funct
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
613 6 2 6 3.7 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2022598 calrl_human Human No 9.5 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
582 7 2 6 3.0 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)C(=O)N(C)C)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022607 calrl_human Human No 9.5 IC50 = 0.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 6 2 5 4.6 CC1=CC(=CC2=C(NN=C12)Br)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL2023188 calrl_human Human No 9.5 IC50 = 0.3 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
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2035983 calrl_human Human No 9.5 IC50 = 0.3 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
573 4 3 8 1.9 CC1(CNC2(CCCC2)C(=O)N1CC(=O)NC3=CN=C4CC5(CC4=C3)C6=C(NC5=O)N=CC=C6)C7=CC(=CC(=C7)F)F
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.3 Funct
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 3 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)N4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2023188 calrl_human Human No 9.5 IC50 = 0.3 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
613 7 2 6 4.7 CC1=C2C(=CC(=C1)CC(C3=NC(=CC(=C3)C(=O)N(C)C)Cl)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2035983 calrl_human Human No 9.5 IC50 = 0.3 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
573 4 3 8 1.9 CC1(CNC2(CCCC2)C(=O)N1CC(=O)NC3=CN=C4CC5(CC4=C3)C6=C(NC5=O)N=CC=C6)C7=CC(=CC(=C7)F)F
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.3 Funct
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 3 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)N4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.4 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 3 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)N4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018506 calrl_human Human No 9.5 IC50 = 0.4 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 3 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)N4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL1770557 calrl_human Human No 9.4 IC50 = 0.4 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 9 3.3 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770557 calrl_human Human No 9.4 IC50 = 0.4 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 9 3.3 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL2430174 calrl_human Human No 9.4 IC50 = 0.4 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
621 7 3 5 4.3 CC1=C2C(=CC(=C1)CC(C3=NC=C(N3CC4=CC(=CC=C4)F)C)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024595 calrl_human Human No 9.4 IC50 = 0.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 6 2 5 4.6 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024595 calrl_human Human No 9.4 IC50 = 0.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 6 2 5 4.6 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2022608 calrl_human Human No 9.4 IC50 = 0.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
545 6 2 5 4.5 CC1=CC(=CC2=C(NN=C12)Cl)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL2431248 calrl_human Human No 9.4 IC50 = 0.4 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
586 4 2 7 3.4 CC1(CN(C2(CCCC2)C(=O)N1CC(=O)NC3=CC4=C(CC5(C4)C6=C(NC5=O)N=CC=C6)C=C3)C)C7=CC(=CC(=C7)F)F
CHEMBL2430178 calrl_human Human No 9.4 IC50 = 0.4 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 3 6 4.0 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC(=CC(=C4)F)F)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2430176 calrl_human Human No 9.4 IC50 = 0.4 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
704 7 3 6 5.0 CC1=C2C(=CC(=C1)CC(C3=NC(=CN3CC4=CC(=CC(=C4)F)F)Br)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2022608 calrl_human Human No 9.4 IC50 = 0.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
545 6 2 5 4.5 CC1=CC(=CC2=C(NN=C12)Cl)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1770720 calrl_human Human No 9.4 IC50 = 0.4 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 10 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL1770720 calrl_human Human No 9.4 IC50 = 0.4 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 10 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL1770728 calrl_human Human No 9.4 IC50 = 0.4 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
609 6 2 8 3.4 CCC(CC)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL1770728 calrl_human Human No 9.4 IC50 = 0.4 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
609 6 2 8 3.4 CCC(CC)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2430170 calrl_human Human No 9.4 IC50 = 0.4 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
590 7 3 5 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CN=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024595 calrl_human Human No 9.3 IC50 = 0.5 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
589 6 2 5 4.6 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024599 calrl_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
561 6 2 5 4.8 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024595 calrl_human Human No 9.3 IC50 = 0.5 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
589 6 2 5 4.6 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024599 calrl_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
561 6 2 5 4.8 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024594 calrl_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 5 3 4 4.0 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)NC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024594 calrl_human Human No 9.3 IC50 = 0.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
589 5 3 4 4.0 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)NC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL525571 calrl_human Human No 9.3 IC50 = 0.5 Funct
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.
3126 104 47 44 -9.3 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL2369463 calrl_human Human No 9.3 IC50 = 0.5 Funct
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.
3027 99 44 43 -10.8 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)N
CHEMBL1089433 calrl_human Human No 9.3 IC50 = 0.5 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 5 3.1 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL1089433 calrl_human Human No 9.3 IC50 = 0.5 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 5 3.1 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL3114496 calrl_human Human No 9.2 IC50 = 0.6 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
707 9 1 7 5.8 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CCC4=CC=CC=C4NC3=O)C5=C(C(=CC=C5)F)N6CCN(CC6)C(C)(C)C
CHEMBL525571 calrl_rat Rat No 9.2 IC50 = 0.6 Funct
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
3126 104 47 44 -9.3 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL1770723 calrl_human Human No 9.2 IC50 = 0.6 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
553 4 2 8 1.7 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770715 calrl_human Human No 9.2 IC50 = 0.6 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 5 2 7 2.2 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL562069 calrl_human Human No 9.2 IC50 = 0.6 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 4 1.8 C1C2=CN(C3=C2C(=CC=C3)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1770723 calrl_human Human No 9.2 IC50 = 0.6 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
553 4 2 8 1.7 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770715 calrl_human Human No 9.2 IC50 = 0.6 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 5 2 7 2.2 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL562069 calrl_human Human No 9.2 IC50 = 0.6 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 4 1.8 C1C2=CN(C3=C2C(=CC=C3)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1770568 calrl_human Human No 9.2 IC50 = 0.6 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
550 4 2 6 3.1 CC(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL570933 calrl_human Human No 9.2 IC50 = 0.6 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
517 3 3 6 1.1 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=CC=CC8=C7C(C6=O)(CC(=O)N8)CN
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL1770568 calrl_human Human No 9.2 IC50 = 0.6 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
550 4 2 6 3.1 CC(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL570933 calrl_human Human No 9.2 IC50 = 0.6 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
517 3 3 6 1.1 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=CC=CC8=C7C(C6=O)(CC(=O)N8)CN
CHEMBL512773 calrl_human Human No 9.2 IC50 = 0.6 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 5 0.8 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL1770714 calrl_human Human No 9.2 IC50 = 0.6 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 5 2 7 1.6 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770724 calrl_human Human No 9.2 IC50 = 0.6 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
581 4 2 8 2.3 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024599 calrl_human Human No 9.2 IC50 = 0.6 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
561 6 2 5 4.8 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770714 calrl_human Human No 9.2 IC50 = 0.6 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 5 2 7 1.6 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770724 calrl_human Human No 9.2 IC50 = 0.6 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
581 4 2 8 2.3 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024599 calrl_human Human No 9.2 IC50 = 0.6 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
561 6 2 5 4.8 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2430179 calrl_human Human No 9.2 IC50 = 0.6 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
607 7 3 5 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC(=CC=C4)F)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770727 calrl_human Human No 9.2 IC50 = 0.7 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
649 5 2 11 3.4 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OCC(F)(F)F
CHEMBL1770727 calrl_human Human No 9.2 IC50 = 0.7 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
649 5 2 11 3.4 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OCC(F)(F)F
CHEMBL1092208 calrl_human Human No 9.2 IC50 = 0.7 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 3 2 5 3.4 CCC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL1092208 calrl_human Human No 9.2 IC50 = 0.7 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 3 2 5 3.4 CCC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2018503 calrl_human Human No 9.2 IC50 = 0.7 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
613 6 2 6 3.7 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2018503 calrl_human Human No 9.2 IC50 = 0.7 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
613 6 2 6 3.7 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL1770729 calrl_human Human No 9.1 IC50 = 0.8 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
593 3 2 8 2.4 CC1(CCCO1)C2=CN=C3N2CC(CCC3NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL1770729 calrl_human Human No 9.1 IC50 = 0.8 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
593 3 2 8 2.4 CC1(CCCO1)C2=CN=C3N2CC(CCC3NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL2430185 calrl_human Human No 9.1 IC50 = 0.8 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 4 3.8 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770719 calrl_human Human No 9.1 IC50 = 0.8 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
565 4 2 7 2.0 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024594 calrl_human Human No 9.1 IC50 = 0.8 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
589 5 3 4 4.0 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)NC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024598 calrl_human Human No 9.1 IC50 = 0.8 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770719 calrl_human Human No 9.1 IC50 = 0.8 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
565 4 2 7 2.0 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024594 calrl_human Human No 9.1 IC50 = 0.8 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
589 5 3 4 4.0 CC1=C2C(=CC(=C1)CC(C3=NC(=CC=C3)Br)NC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024598 calrl_human Human No 9.1 IC50 = 0.8 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770722 calrl_human Human No 9.1 IC50 = 0.8 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 11 2.9 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL1770722 calrl_human Human No 9.1 IC50 = 0.8 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 11 2.9 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL2430168 calrl_human Human No 9.1 IC50 = 0.8 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
590 7 3 5 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=NC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770725 calrl_human Human No 9.1 IC50 = 0.9 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
567 3 3 8 1.8 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)O
CHEMBL1092837 calrl_human Human No 9.1 IC50 = 0.9 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
474 2 2 5 2.5 C1C2CN(C3=CC=CC(=C23)NC1=O)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL1770725 calrl_human Human No 9.1 IC50 = 0.9 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
567 3 3 8 1.8 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)O
CHEMBL1092837 calrl_human Human No 9.1 IC50 = 0.9 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
474 2 2 5 2.5 C1C2CN(C3=CC=CC(=C23)NC1=O)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL517467 calrl_human Human No 9.1 IC50 = 0.9 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
539 5 2 5 2.0 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C6=C(NC5=O)N=CC=C6)C=C3)C
CHEMBL517467 calrl_human Human No 9.1 IC50 = 0.9 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
539 5 2 5 2.0 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C6=C(NC5=O)N=CC=C6)C=C3)C
CHEMBL1162991 calrl_human Human No 9.1 IC50 = 0.9 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL466192 calrl_human Human No 9.1 IC50 = 0.9 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 5 0.2 CC1=CC2=C3C(=C1)NC(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL2430182 calrl_human Human No 9.1 IC50 = 0.9 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 8 3 4 4.1 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CCC4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1162991 calrl_human Human No 9.1 IC50 = 0.9 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL466192 calrl_human Human No 9.1 IC50 = 0.9 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 5 0.2 CC1=CC2=C3C(=C1)NC(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL2369463 calrl_rat Rat No 9.1 IC50 = 0.9 Funct
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
3027 99 44 43 -10.8 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)N
CHEMBL1770716 calrl_human Human No 9.0 IC50 = 0.9 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 9 3.1 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 0.9 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
537 7 2 5 2.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)C=O)C=NN2
CHEMBL1770716 calrl_human Human No 9.0 IC50 = 0.9 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 9 3.1 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 0.9 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
537 7 2 5 2.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)C=O)C=NN2
CHEMBL2430180 calrl_human Human No 9.0 IC50 = 1.0 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
607 7 3 5 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=C(C=C4)F)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024598 calrl_human Human No 9.0 IC50 = 1 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL238276 calrl_human Human No 9.0 IC50 = 1 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 10 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCOC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2024598 calrl_human Human No 9.0 IC50 = 1 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=CC4=CC=CC=C4C=N3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL3114676 calrl_human Human No 9.0 IC50 = 1 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
707 9 1 7 5.8 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CCC4=CC=CC=C4NC3=O)C5=C(C(=CC=C5)F)N6CCN(CC6)C(C)(C)C
CHEMBL238276 calrl_human Human No 9.0 IC50 = 1 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 10 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCOC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 1.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
537 7 2 5 2.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)C=O)C=NN2
CHEMBL2024589 calrl_human Human No 9.0 IC50 = 1.1 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
537 7 2 5 2.8 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)C=O)C=NN2
CHEMBL1090515 calrl_human Human No 8.9 IC50 = 1.2 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
503 2 1 5 1.9 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2022605 calrl_human Human No 8.9 IC50 = 1.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 8 2 7 3.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCOCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1090515 calrl_human Human No 8.9 IC50 = 1.2 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
503 2 1 5 1.9 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2022605 calrl_human Human No 8.9 IC50 = 1.2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 8 2 7 3.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CN4CCOCC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770722 calrl_human Human No 8.9 IC50 = 1.3 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 11 2.9 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL2024590 calrl_human Human No 8.9 IC50 = 1.3 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
606 8 2 5 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)CN7CCCCC7)C=NN2
CHEMBL564487 calrl_human Human Yes 8.9 IC50 = 1.3 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 5 2.2 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1089433 calrl_human Human No 8.9 IC50 = 1.3 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 5 3.1 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2022610 calrl_human Human No 8.9 IC50 = 1.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
539 7 2 6 3.4 CC1=CC(=CC2=C(NN=C12)C=O)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1770722 calrl_human Human No 8.9 IC50 = 1.3 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 11 2.9 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL2024590 calrl_human Human No 8.9 IC50 = 1.3 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
606 8 2 5 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)CN7CCCCC7)C=NN2
CHEMBL564487 calrl_human Human Yes 8.9 IC50 = 1.3 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 5 2.2 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1089433 calrl_human Human No 8.9 IC50 = 1.3 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 5 3.1 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2022610 calrl_human Human No 8.9 IC50 = 1.3 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
539 7 2 6 3.4 CC1=CC(=CC2=C(NN=C12)C=O)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1770717 calrl_human Human No 8.9 IC50 = 1.4 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
601 3 2 9 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)C4(CC4)C(F)(F)F)NC(=O)N5CCC6(CC5)C7=C(NC6=O)N=CC=C7
CHEMBL1770719 calrl_human Human No 8.9 IC50 = 1.4 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
565 4 2 7 2.0 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024596 calrl_human Human No 8.9 IC50 = 1.4 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024597 calrl_human Human No 8.9 IC50 = 1.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
561 6 2 5 4.9 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770717 calrl_human Human No 8.9 IC50 = 1.4 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
601 3 2 9 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)C4(CC4)C(F)(F)F)NC(=O)N5CCC6(CC5)C7=C(NC6=O)N=CC=C7
CHEMBL1770719 calrl_human Human No 8.9 IC50 = 1.4 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
565 4 2 7 2.0 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F)OC
CHEMBL2024596 calrl_human Human No 8.9 IC50 = 1.4 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024597 calrl_human Human No 8.9 IC50 = 1.4 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
561 6 2 5 4.9 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL1770725 calrl_human Human No 8.8 IC50 = 1.5 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
567 3 3 8 1.8 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)O
CHEMBL1092208 calrl_human Human No 8.8 IC50 = 1.5 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
502 3 2 5 3.4 CCC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2024593 calrl_human Human No 8.8 IC50 = 1.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
511 6 2 5 3.6 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL1770725 calrl_human Human No 8.8 IC50 = 1.5 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
567 3 3 8 1.8 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)O
CHEMBL1092208 calrl_human Human No 8.8 IC50 = 1.5 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
502 3 2 5 3.4 CCC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C8=C(NC7=O)N=CC=C8)C=C5C=C4
CHEMBL2024593 calrl_human Human No 8.8 IC50 = 1.5 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
511 6 2 5 3.6 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL1770556 calrl_human Human No 8.8 IC50 = 1.6 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 7 1.9 C1CC1C2=NN=C3N2CC(CCC3NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL518422 calrl_human Human No 8.8 IC50 = 1.6 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
504 4 2 6 2.0 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=CC=CC=C6N(C5=O)C7=NC=NC=C7
CHEMBL1770556 calrl_human Human No 8.8 IC50 = 1.6 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 7 1.9 C1CC1C2=NN=C3N2CC(CCC3NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL2430171 calrl_human Human No 8.8 IC50 = 1.6 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
590 7 3 5 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=CC=N4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL518422 calrl_human Human No 8.8 IC50 = 1.6 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
504 4 2 6 2.0 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C(C=C2)NC(=O)CN5C6=CC=CC=C6N(C5=O)C7=NC=NC=C7
CHEMBL1770718 calrl_human Human No 8.8 IC50 = 1.7 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 2 7 1.4 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770723 calrl_human Human No 8.8 IC50 = 1.7 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
553 4 2 8 1.7 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1090848 calrl_human Human No 8.8 IC50 = 1.7 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 5 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C4C(=C3)C=CC(=N4)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL1770718 calrl_human Human No 8.8 IC50 = 1.7 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 2 7 1.4 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770723 calrl_human Human No 8.8 IC50 = 1.7 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
553 4 2 8 1.7 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL2430164 calrl_human Human No 8.8 IC50 = 1.7 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
580 7 2 6 3.3 CCN1CCN2C(=CN=C2C(CC3=CC(=C4C(=C3)C=NN4)C)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C1
CHEMBL1090848 calrl_human Human No 8.8 IC50 = 1.7 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 5 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C4C(=C3)C=CC(=N4)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL2369459 calrl_human Human No 8.8 IC50 = 1.7 Funct
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
3789 110 55 57 -15.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)O)CC(=O)O)NC(=O)C(C)N)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C(C)C)C(=O)N4CCCC4C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC5=CC=CC=C5)C(=O)N)C(C)O
CHEMBL500384 calrl_human Human No 8.7 IC50 = 1.8 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
542 6 2 5 4.1 CC1=C2C(=CC(=C1)CC(C(=O)N3CCCCC3)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024590 calrl_human Human No 8.7 IC50 = 1.8 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 8 2 5 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)CN7CCCCC7)C=NN2
CHEMBL500384 calrl_human Human No 8.8 IC50 = 1.8 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
542 6 2 5 4.1 CC1=C2C(=CC(=C1)CC(C(=O)N3CCCCC3)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024590 calrl_human Human No 8.8 IC50 = 1.8 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 8 2 5 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C6=NC=C(C=C6)CN7CCCCC7)C=NN2
CHEMBL1770714 calrl_human Human No 8.7 IC50 = 1.9 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 5 2 7 1.6 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL2024593 calrl_human Human No 8.7 IC50 = 1.9 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
511 6 2 5 3.6 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2023186 calrl_human Human No 8.7 IC50 = 1.9 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
610 8 2 7 3.1 CC1=CC(=CC2=C(NN=C12)CN3CCOCC3)CC(C4=CC=CC=N4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O
CHEMBL1770714 calrl_human Human No 8.7 IC50 = 1.9 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 5 2 7 1.6 COCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL2024593 calrl_human Human No 8.7 IC50 = 1.9 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
511 6 2 5 3.6 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2430181 calrl_human Human No 8.7 IC50 = 1.9 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
607 7 3 5 3.9 CC1=C2C(=CC(=C1)CC(C3=NC=CN3CC4=CC=CC=C4F)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2023186 calrl_human Human No 8.7 IC50 = 1.9 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
610 8 2 7 3.1 CC1=CC(=CC2=C(NN=C12)CN3CCOCC3)CC(C4=CC=CC=N4)OC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O
CHEMBL530116 calrl_human Human No 8.0 IC50 = 10 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 4 1.6 CC1=CC(=C2C(=C1)N(C(=O)N2C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL392635 calrl_human Human No 8.0 IC50 = 10 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
576 5 2 7 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC3=CC=CC=N3)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL392937 calrl_human Human No 8.0 IC50 = 10 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
531 5 2 7 2.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCF)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL482178 calrl_human Human No 8.0 IC50 = 10 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 6 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=NC=NC=C6
CHEMBL2024172 calrl_human Human No 8.0 IC50 = 10 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
537 7 2 4 4.1 CCC1=CC(=NC=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL530116 calrl_human Human No 8.0 IC50 = 10 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 4 1.6 CC1=CC(=C2C(=C1)N(C(=O)N2C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL3114486 calrl_human Human No 8.0 IC50 = 10 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 8 1 6 4.3 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5N6CCN(CC6)C
CHEMBL392635 calrl_human Human No 8.0 IC50 = 10 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
576 5 2 7 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC3=CC=CC=N3)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL392937 calrl_human Human No 8.0 IC50 = 10 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
531 5 2 7 2.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCF)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL482178 calrl_human Human No 8.0 IC50 = 10 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 6 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=NC=NC=C6
CHEMBL2369452 calrl_rat Rat No 8.0 IC50 = 10 Funct
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
2925 96 42 41 -9.9 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)N
CHEMBL2024172 calrl_human Human No 8.0 IC50 = 10 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
537 7 2 4 4.1 CCC1=CC(=NC=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL213976 calrl_human Human No 7.0 IC50 = 100 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
543 4 2 8 2.6 C1CN(CCC1N2CC(=O)NC2=O)C(=O)NC3C(=O)N(C4=CC=CC=C4C(=N3)C5=CC=CC=C5)CC(F)(F)F
CHEMBL384799 calrl_human Human No 7.0 IC50 = 100 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
604 5 2 7 4.5 C1CN(CCC1N2C(=O)N=C(N2)C3=CC=CC=C3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL2018491 calrl_human Human No 7.0 IC50 = 100 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
650 7 3 5 3.0 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC(=O)NC6=CC=CC=C6Cl
CHEMBL213976 calrl_human Human No 7.0 IC50 = 100 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
543 4 2 8 2.6 C1CN(CCC1N2CC(=O)NC2=O)C(=O)NC3C(=O)N(C4=CC=CC=C4C(=N3)C5=CC=CC=C5)CC(F)(F)F
CHEMBL384799 calrl_human Human No 7.0 IC50 = 100 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
604 5 2 7 4.5 C1CN(CCC1N2C(=O)N=C(N2)C3=CC=CC=C3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL2018491 calrl_human Human No 7.0 IC50 = 100 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
650 7 3 5 3.0 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC(=O)NC6=CC=CC=C6Cl
CHEMBL198105 calrl_human Human No 6.0 IC50 = 1000 Funct
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
790 15 5 8 3.9 COC1=CC=CC=C1CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)N3CCN(CC3)C4=CC=NC=C4
CHEMBL238275 calrl_human Human No 6.0 IC50 = 1000 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
465 3 4 5 1.2 C1CC(C(=O)NCC1C2=CC=C(C=C2)O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL198105 calrl_human Human No 6.0 IC50 = 1000 Funct
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
790 15 5 8 3.9 COC1=CC=CC=C1CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)N3CCN(CC3)C4=CC=NC=C4
CHEMBL238275 calrl_human Human No 6.0 IC50 = 1000 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
465 3 4 5 1.2 C1CC(C(=O)NCC1C2=CC=C(C=C2)O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL269027 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1224 39 19 21 -6.8 CCC(C)C(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CO)C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)O)N
CHEMBL405694 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1206 35 18 20 -9.0 CC(C)C(C(=O)NC(C)C(=O)N1CCCC1C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)N)C(=O)NCC(=O)NC(CC2=CC=C(C=C2)O)C(=O)O)NC(=O)C(CC(=O)N)N
CHEMBL216229 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1312 37 19 21 -8.0 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CC(=O)N)C(=O)NC(C(C)O)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC(=O)N)N
CHEMBL267137 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1493 45 20 22 -6.9 CCC(C)C(C(=O)NC(CO)C(=O)N1CCCC1C(=O)NC(CCC(=O)N)C(=O)NCC(=O)NC(CC2=CC=C(C=C2)O)C(=O)O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CCCN=C(N)N)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC(=O)N)N
CHEMBL267182 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1416 43 19 22 -9.4 CCC(C)C(C(=O)NC(CO)C(=O)N1CCCC1C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CCCN=C(N)N)NC(=O)C3CCCN3C(=O)C(C)NC(=O)C(C(C)C)NC(=O)C(CC(=O)N)N
CHEMBL409205 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1282 37 18 20 -7.4 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)N)C(=O)NCC(=O)NC(CC1=CC=C(C=C1)O)C(=O)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC(=O)N)N
CHEMBL438008 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1205 35 17 20 -7.6 CC(C)C(C(=O)NC(C)C(=O)N1CCCC1C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CC(=O)N)N
CHEMBL438224 calrl_human Human No 5.0 IC50 = 10000 Funct
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.
1492 45 19 22 -7.8 CCC(C)C(C(=O)NC(CO)C(=O)N1CCCC1C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CCCN=C(N)N)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC(=O)N)N
CHEMBL257094 calrl_human Human No 6.0 IC50 = 1004 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
525 6 2 7 1.4 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL257094 calrl_human Human No 6.0 IC50 = 1004 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
525 6 2 7 1.4 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL198311 calrl_human Human No 5.0 IC50 = 10300 Funct
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
758 15 4 7 4.0 C1CN(CCN1C2=CC=NC=C2)C(=O)C(CCCCN)NC(=O)C(CC3=CC(=C(C(=C3)Br)N)Br)NC(=O)CCCC4=CC=CC=C4
CHEMBL198311 calrl_human Human No 5.0 IC50 = 10300 Funct
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
758 15 4 7 4.0 C1CN(CCN1C2=CC=NC=C2)C(=O)C(CCCCN)NC(=O)C(CC3=CC(=C(C(=C3)Br)N)Br)NC(=O)CCCC4=CC=CC=C4
CHEMBL403373 calrl_human Human No 6.0 IC50 = 1066 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 5 0.2 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CN=CC=C5
CHEMBL403373 calrl_human Human No 6.0 IC50 = 1066 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 5 0.2 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CN=CC=C5
CHEMBL215274 calrl_human Human No 7.0 IC50 = 107 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
621 5 2 8 4.6 C1CN(CCC1N2C=C(NC2=O)C3=CC=C(C=C3)F)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL215274 calrl_human Human No 7.0 IC50 = 107 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
621 5 2 8 4.6 C1CN(CCC1N2C=C(NC2=O)C3=CC=C(C=C3)F)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL268420 calrl_human Human No 7.0 IC50 = 107.2 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 15 -0.2 CC(C)C(C(=O)NC1CCC2CCC(N2C1=O)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C)C(=O)NC(CC4=CC=CC=C4)C(=O)N)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C5CCCN5C(=O)C(C(C)C)NC(=O)C(CC6=CC=CC=C6)N
CHEMBL268420 calrl_human Human No 7.0 IC50 = 107.2 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 15 -0.2 CC(C)C(C(=O)NC1CCC2CCC(N2C1=O)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C)C(=O)NC(CC4=CC=CC=C4)C(=O)N)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C5CCCN5C(=O)C(C(C)C)NC(=O)C(CC6=CC=CC=C6)N
CHEMBL258070 calrl_human Human No 5.0 IC50 = 10900 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 4 1.3 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=CC=C5
CHEMBL258070 calrl_human Human No 5.0 IC50 = 10900 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 4 1.3 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 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 9 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(=O)NC5=C4C=CC=N5
CHEMBL571203 calrl_human Human No 8.0 IC50 = 11 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
552 3 2 9 2.8 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 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 3 2 9 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(=O)NC5=C4C=CC=N5
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 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 9 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(=O)NC5=C4C=CC=N5
CHEMBL571203 calrl_human Human No 8.0 IC50 = 11 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
552 3 2 9 2.8 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.0 IC50 = 11 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 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL570531 calrl_human Human No 8.0 IC50 = 11 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 3 2 9 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(=O)NC5=C4C=CC=N5
CHEMBL2369454 calrl_rat Rat No 8.0 IC50 = 11 Funct
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
3060 100 44 43 -9.9 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL2018518 calrl_human Human No 8.0 IC50 = 11 Funct
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 7 2 5 3.5 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7)C=NN2
CHEMBL2369457 calrl_human Human No 8.0 IC50 = 11.2 Funct
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
3084 100 45 44 -11.4 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL221009 calrl_human Human No 7.0 IC50 = 110 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 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL376292 calrl_human Human No 7.0 IC50 = 110 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
483 4 2 6 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=NC=CC=N6
CHEMBL221009 calrl_human Human No 7.0 IC50 = 110 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 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL376292 calrl_human Human No 7.0 IC50 = 110 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
483 4 2 6 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=NC=CC=N6
CHEMBL570793 calrl_human Human No 7.0 IC50 = 112 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 9 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)C4=CC=NNC4=O
CHEMBL570793 calrl_human Human No 7.0 IC50 = 112 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 9 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)C4=CC=NNC4=O
CHEMBL386113 calrl_human Human No 6.0 IC50 = 1135 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 3.5 C1CN(CCC1N2C3=C(C=CC=N3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL386113 calrl_human Human No 6.0 IC50 = 1135 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 3.5 C1CN(CCC1N2C3=C(C=CC=N3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL256901 calrl_human Human No 6.9 IC50 = 119 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 8 2.5 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC(=CC=C5)F
CHEMBL256901 calrl_human Human No 6.9 IC50 = 119 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 8 2.5 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC(=CC=C5)F
CHEMBL255999 calrl_human Human No 5.9 IC50 = 1190 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
490 6 2 6 0.1 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CN=CC=C5
CHEMBL255999 calrl_human Human No 5.9 IC50 = 1190 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
490 6 2 6 0.1 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CN=CC=C5
CHEMBL455458 calrl_human Human No 7.9 IC50 = 12 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
503 3 2 5 0.3 CN1C(=O)CCCN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 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 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL1770560 calrl_human Human No 7.9 IC50 = 12 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
538 4 3 7 1.1 C1CC(C2=NC(=CN2CC1C3=C(C(=CC=C3)F)F)CO)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770564 calrl_human Human No 7.9 IC50 = 12 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
565 6 3 7 1.8 CNCCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770563 calrl_human Human No 7.9 IC50 = 12 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
538 4 3 7 1.1 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CO)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770562 calrl_human Human No 7.9 IC50 = 12 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
522 3 2 6 2.3 CC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2022602 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
508 6 2 5 4.2 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024587 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 6 2 4 3.7 CC1=CN=C(C=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.7 CC1=C2C(=CC(=C1)CC(C3=CC=CC(=N3)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL455458 calrl_human Human No 7.9 IC50 = 12 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
503 3 2 5 0.3 CN1C(=O)CCCN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 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 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL1770560 calrl_human Human No 7.9 IC50 = 12 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
538 4 3 7 1.1 C1CC(C2=NC(=CN2CC1C3=C(C(=CC=C3)F)F)CO)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770564 calrl_human Human No 7.9 IC50 = 12 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
565 6 3 7 1.8 CNCCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770563 calrl_human Human No 7.9 IC50 = 12 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
538 4 3 7 1.1 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CO)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770562 calrl_human Human No 7.9 IC50 = 12 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
522 3 2 6 2.3 CC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL519421 calrl_human Human No 7.9 IC50 = 12 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2369454 calrl_human Human No 7.9 IC50 = 12 Funct
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.
3060 100 44 43 -9.9 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL2022602 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
508 6 2 5 4.2 CC1=C2C(=CC(=C1)CC(C3=CC=CC=N3)OC(=O)N4CCC(CC4)C5=CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024587 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 6 2 4 3.7 CC1=CN=C(C=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 12 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.7 CC1=C2C(=CC(=C1)CC(C3=CC=CC(=N3)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL453865 calrl_human Human No 6.9 IC50 = 120 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 6 2 5 0.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CCC(=O)N(C)C
CHEMBL2018497 calrl_human Human No 6.9 IC50 = 120 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
630 7 3 9 2.3 CC1=NC(=NC2=NNN=C12)NC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7
CHEMBL239630 calrl_human Human No 6.9 IC50 = 120 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC=CC=C2F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL577320 calrl_human Human No 6.9 IC50 = 120 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
579 4 2 8 3.9 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(NC4=O)C5=CC=CC=C5
CHEMBL2018501 calrl_human Human No 6.9 IC50 = 120 Funct
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
702 7 2 5 5.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC=C(C7=CC=CC=C76)Br
CHEMBL221009 calrl_human Human No 6.9 IC50 = 120 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
405 3 3 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL453865 calrl_human Human No 6.9 IC50 = 120 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 6 2 5 0.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CCC(=O)N(C)C
CHEMBL2430175 calrl_human Human No 6.9 IC50 = 120 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
513 5 4 4 2.6 CC1=C2C(=CC(=C1)CC(C3=NC=C(N3)C)NC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2018497 calrl_human Human No 6.9 IC50 = 120 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
630 7 3 9 2.3 CC1=NC(=NC2=NNN=C12)NC(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)C(=O)N6CCC(CC6)N7CCCCC7
CHEMBL239630 calrl_human Human No 6.9 IC50 = 120 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC=CC=C2F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL577320 calrl_human Human No 6.9 IC50 = 120 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
579 4 2 8 3.9 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)CC(NC4=O)C5=CC=CC=C5
CHEMBL2018501 calrl_human Human No 6.9 IC50 = 120 Funct
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
702 7 2 5 5.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC=C(C7=CC=CC=C76)Br
CHEMBL221009 calrl_human Human No 6.9 IC50 = 120 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
405 3 3 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL221009 calrl_human Human No 5.9 IC50 = 1200 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 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL470321 calrl_human Human No 5.9 IC50 = 1200 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C(=CC=C5)F)NC4=O
CHEMBL520905 calrl_human Human No 5.9 IC50 = 1200 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=CC(=C5)F)NC4=O
CHEMBL530116 calrl_human Human No 5.9 IC50 = 1200 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 4 1.6 CC1=CC(=C2C(=C1)N(C(=O)N2C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL1092883 calrl_human Human No 5.9 IC50 = 1200 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
483 2 1 5 1.0 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC4=NC5=CC6=C(CC7(C6)C(=O)NC(=O)N7C)C=C5C=C4
CHEMBL221009 calrl_human Human No 5.9 IC50 = 1200 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 4 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5NC4=O
CHEMBL470321 calrl_human Human No 5.9 IC50 = 1200 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C(=CC=C5)F)NC4=O
CHEMBL520905 calrl_human Human No 5.9 IC50 = 1200 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=CC(=C5)F)NC4=O
CHEMBL530116 calrl_human Human No 5.9 IC50 = 1200 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 4 1.6 CC1=CC(=C2C(=C1)N(C(=O)N2C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL1092883 calrl_human Human No 5.9 IC50 = 1200 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
483 2 1 5 1.0 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC4=NC5=CC6=C(CC7(C6)C(=O)NC(=O)N7C)C=C5C=C4
CHEMBL216710 calrl_human Human No 5.9 IC50 = 1200 Funct
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.
1167 33 15 18 -4.2 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)N)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C(CC3=CC=CC=C3)N
CHEMBL88441 calrl_human Human No 4.9 IC50 = 12000 Funct
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
495 7 1 5 6.3 CCC1CN2CCC1CC2C(C3=CC(=NC4=C3C=C(C=C4)OC)C5=CC=C(C=C5)OC6=CC=CC=C6)O
CHEMBL577957 calrl_human Human No 6.9 IC50 = 122 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 9 1.7 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C(=O)NC(=O)N4
CHEMBL577957 calrl_human Human No 6.9 IC50 = 122 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 9 1.7 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C(=O)NC(=O)N4
CHEMBL3114460 calrl_human Human No 5.9 IC50 = 1220 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
509 7 1 5 2.1 COCCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5
CHEMBL487068 calrl_human Human No 7.9 IC50 = 13 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 5 0.6 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL455458 calrl_human Human No 7.9 IC50 = 13 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
503 3 2 5 0.3 CN1C(=O)CCCN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL1770727 calrl_human Human No 7.9 IC50 = 13 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
649 5 2 11 3.4 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OCC(F)(F)F
CHEMBL2024172 calrl_human Human No 7.9 IC50 = 13 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
537 7 2 4 4.1 CCC1=CC(=NC=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1162991 calrl_human Human No 7.9 IC50 = 13 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL570748 calrl_human Human No 7.9 IC50 = 13 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
542 4 2 9 2.6 CC1=NNC(=O)C(=C1)C2CCN(CC2)C(=O)NC3CCC(CN(C3=O)CC(F)(F)F)C4=C(C(=CC=C4)F)F
CHEMBL570746 calrl_human Human No 7.9 IC50 = 13 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
568 3 2 10 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5
CHEMBL466192 calrl_human Human No 7.9 IC50 = 13 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 5 0.2 CC1=CC2=C3C(=C1)NC(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL487068 calrl_human Human No 7.9 IC50 = 13 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 5 0.6 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL455458 calrl_human Human No 7.9 IC50 = 13 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
503 3 2 5 0.3 CN1C(=O)CCCN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL1770727 calrl_human Human No 7.9 IC50 = 13 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
649 5 2 11 3.4 CC(C)(C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F)OCC(F)(F)F
CHEMBL2024172 calrl_human Human No 7.9 IC50 = 13 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
537 7 2 4 4.1 CCC1=CC(=NC=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1162991 calrl_human Human No 7.9 IC50 = 13 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL570748 calrl_human Human No 7.9 IC50 = 13 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
542 4 2 9 2.6 CC1=NNC(=O)C(=C1)C2CCN(CC2)C(=O)NC3CCC(CN(C3=O)CC(F)(F)F)C4=C(C(=CC=C4)F)F
CHEMBL570746 calrl_human Human No 7.9 IC50 = 13 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
568 3 2 10 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5
CHEMBL466192 calrl_human Human No 7.9 IC50 = 13 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 5 0.2 CC1=CC2=C3C(=C1)NC(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL487077 calrl_human Human No 6.9 IC50 = 130 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 4 1.1 CC1=CC2=C(C=C1)NC(=O)N2CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3
CHEMBL521076 calrl_human Human No 6.9 IC50 = 130 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 5 -0.2 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CC(=O)N
CHEMBL2018356 calrl_human Human No 6.9 IC50 = 130 Funct
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
627 8 3 6 2.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NCC6=CC7=C(C=C6)NN=C7
CHEMBL487077 calrl_human Human No 6.9 IC50 = 130 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 4 1.1 CC1=CC2=C(C=C1)NC(=O)N2CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3
CHEMBL521076 calrl_human Human No 6.9 IC50 = 130 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 5 -0.2 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CC(=O)N
CHEMBL2018356 calrl_human Human No 6.9 IC50 = 130 Funct
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
627 8 3 6 2.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NCC6=CC7=C(C=C6)NN=C7
CHEMBL198762 calrl_human Human No 4.9 IC50 = 13000 Funct
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
748 17 6 6 5.1 COC1=CC=CC=C1CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL198762 calrl_human Human No 4.9 IC50 = 13000 Funct
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
748 17 6 6 5.1 COC1=CC=CC=C1CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL3114469 calrl_human Human No 5.9 IC50 = 1370 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
556 7 1 5 3.2 C1CN(CCC1N2CC3=CC=CC=C3NC2=O)C(=O)CC4C(=O)N(C(S4)C5=CC=CC=C5)CCC6=CC=CC=N6
CHEMBL415453 calrl_human Human No 5.9 IC50 = 1381 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 3.2 C1CN(CCC1N2C3=C(C=NC=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL415453 calrl_human Human No 5.9 IC50 = 1381 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 3.2 C1CN(CCC1N2C3=C(C=NC=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL3114487 calrl_human Human No 4.9 IC50 = 13900 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 8 1 6 4.3 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5N6CCN(CC6)C
CHEMBL426142 calrl_human Human No 5.9 IC50 = 1396 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
595 4 2 8 4.3 C1CN(CCC1N2C3=C(C=CC(=C3)F)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL426142 calrl_human Human No 5.9 IC50 = 1396 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
595 4 2 8 4.3 C1CN(CCC1N2C3=C(C=CC(=C3)F)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL384723 calrl_human Human No 5.9 IC50 = 1398 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 3.2 C1CN(CCC1N2C3=C(C=CN=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL384723 calrl_human Human No 5.9 IC50 = 1398 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 3.2 C1CN(CCC1N2C3=C(C=CN=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL215499 calrl_human Human No 7.9 IC50 = 14 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 4.5 C1CN(CCC1N2C=C(NC2=O)C3=CC=CC=C3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL455674 calrl_human Human No 7.9 IC50 = 14 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
489 3 3 5 0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CCCN6C4=O
CHEMBL519421 calrl_human Human No 7.9 IC50 = 14 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 14 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
586 6 3 4 4.7 CC1=C2C(=CC(=C1)CC(C3=CC=CC(=N3)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL237661 calrl_human Human No 7.9 IC50 = 14 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
485 3 3 6 1.7 C1CC(C(=O)NCC1C2=C(C(=CC=C2)F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1090848 calrl_human Human No 7.9 IC50 = 14 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 5 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C4C(=C3)C=CC(=N4)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL215499 calrl_human Human No 7.9 IC50 = 14 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 4.5 C1CN(CCC1N2C=C(NC2=O)C3=CC=CC=C3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL455674 calrl_human Human No 7.9 IC50 = 14 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
489 3 3 5 0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CCCN6C4=O
CHEMBL519421 calrl_human Human No 7.9 IC50 = 14 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2024600 calrl_human Human No 7.9 IC50 = 14 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
586 6 3 4 4.7 CC1=C2C(=CC(=C1)CC(C3=CC=CC(=N3)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL237661 calrl_human Human No 7.9 IC50 = 14 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
485 3 3 6 1.7 C1CC(C(=O)NCC1C2=C(C(=CC=C2)F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1090848 calrl_human Human No 7.9 IC50 = 14 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 5 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C4C(=C3)C=CC(=N4)CN5C6=C7C(=CC=C6)NC(=O)CN7C5=O
CHEMBL2369742 calrl_human Human No 7.9 IC50 = 14 Funct
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
3334 106 50 50 -15.1 CC(C)C(C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)CNC(=O)C(CO)NC(=O)C(CCCN=C(N)N)NC(=O)C(C(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(C(C)C)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL2369457 calrl_human Human No 7.8 IC50 = 14.5 Funct
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.
3084 100 45 44 -11.4 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL487068 calrl_human Human No 6.9 IC50 = 140 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 5 0.6 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL487068 calrl_human Human No 6.9 IC50 = 140 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 5 0.6 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2059903 calrl_human Human No 5.9 IC50 = 1400 Funct
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 7 3.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=NC=C7
CHEMBL2018493 calrl_human Human No 5.9 IC50 = 1400 Funct
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
575 7 2 7 2.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=NC=NC=C6
CHEMBL221160 calrl_human Human No 5.9 IC50 = 1400 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
406 3 2 5 1.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5OC4=O
CHEMBL2059903 calrl_human Human No 5.9 IC50 = 1400 Funct
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 7 3.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=NC=C7
CHEMBL2018493 calrl_human Human No 5.9 IC50 = 1400 Funct
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
575 7 2 7 2.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=NC=NC=C6
CHEMBL221160 calrl_human Human No 5.9 IC50 = 1400 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
406 3 2 5 1.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5OC4=O
CHEMBL376040 calrl_human Human No 4.9 IC50 = 14000 Funct
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.
1231 34 16 19 -4.0 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=C(C=C4)O)N
CHEMBL270175 calrl_human Human No 6.9 IC50 = 142 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 5 0.9 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC(=CC=C5)O
CHEMBL270175 calrl_human Human No 6.9 IC50 = 142 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 5 0.9 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC(=CC=C5)O
CHEMBL402887 calrl_human Human No 5.9 IC50 = 1421 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 8 0.7 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=NN5
CHEMBL402887 calrl_human Human No 5.9 IC50 = 1421 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 8 0.7 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=NN5
CHEMBL2371143 calrl_human Human No 6.8 IC50 = 146 Funct
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.
1376 42 15 17 -1.7 CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)CNC(=O)C(C(C)C1=CC=CC=C1)NC(=O)C(C(C)C2=CC=CC=C2)NC(=O)C(CCC(=O)N)NC(=O)C(CCC(=O)N)NC(=O)C3CCCN3C(=O)C(CCCCN)NC(=O)C4CCCN4C(=O)C(CCCN=C(N)N)N
CHEMBL1770564 calrl_human Human No 7.8 IC50 = 15 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
565 6 3 7 1.8 CNCCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL236590 calrl_human Human No 7.8 IC50 = 15 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
529 5 3 7 1.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCO)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL237849 calrl_human Human No 7.8 IC50 = 15 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
549 5 2 8 2.7 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2018514 calrl_human Human No 7.8 IC50 = 15 Funct
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
599 6 2 6 3.3 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CC4=C(C=C3)NN=C4)CC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL1770564 calrl_human Human No 7.8 IC50 = 15 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
565 6 3 7 1.8 CNCCC1=CN=C2N1CC(CCC2NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL236590 calrl_human Human No 7.8 IC50 = 15 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
529 5 3 7 1.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCO)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL237849 calrl_human Human No 7.8 IC50 = 15 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
549 5 2 8 2.7 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2018514 calrl_human Human No 7.8 IC50 = 15 Funct
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
599 6 2 6 3.3 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CC4=C(C=C3)NN=C4)CC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL487076 calrl_human Human No 6.8 IC50 = 150 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=C(C=C5)F)NC4=O
CHEMBL521076 calrl_human Human No 6.8 IC50 = 150 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 5 -0.2 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CC(=O)N
CHEMBL488082 calrl_human Human No 6.8 IC50 = 150 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
506 6 2 6 1.5 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)OC)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL241118 calrl_human Human No 6.8 IC50 = 150 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC=CC=C2F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2059898 calrl_human Human No 6.8 IC50 = 150 Funct
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 2 5 4.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CNC(=O)C7=CC=CC=C67
CHEMBL487076 calrl_human Human No 6.8 IC50 = 150 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 0.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=C(C=C5)F)NC4=O
CHEMBL521076 calrl_human Human No 6.8 IC50 = 150 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 5 -0.2 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CC(=O)N
CHEMBL488082 calrl_human Human No 6.8 IC50 = 150 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
506 6 2 6 1.5 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)OC)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL241118 calrl_human Human No 6.8 IC50 = 150 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC=CC=C2F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2059898 calrl_human Human No 6.8 IC50 = 150 Funct
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 2 5 4.8 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CNC(=O)C7=CC=CC=C67
CHEMBL488065 calrl_human Human No 5.8 IC50 = 1500 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 5 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=CC(=C5)OC)NC4=O
CHEMBL488065 calrl_human Human No 5.8 IC50 = 1500 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 5 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C=CC(=C5)OC)NC4=O
CHEMBL3114681 calrl_human Human No 5.8 IC50 = 1500 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
493 5 1 4 3.1 CC(C)N1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5
CHEMBL256802 calrl_human Human No 5.8 IC50 = 1528 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
475 4 2 5 1.3 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=C(C=C5)OC
CHEMBL256802 calrl_human Human No 5.8 IC50 = 1528 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
475 4 2 5 1.3 CN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=C(C=C5)OC
CHEMBL384408 calrl_human Human No 6.8 IC50 = 156 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
585 6 2 9 2.9 COC(=O)C1=CN(C(=O)N1)C2CCN(CC2)C(=O)NC3C(=O)N(C4=CC=CC=C4C(=N3)C5=CC=CC=C5)CC(F)(F)F
CHEMBL384408 calrl_human Human No 6.8 IC50 = 156 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
585 6 2 9 2.9 COC(=O)C1=CN(C(=O)N1)C2CCN(CC2)C(=O)NC3C(=O)N(C4=CC=CC=C4C(=N3)C5=CC=CC=C5)CC(F)(F)F
CHEMBL381798 calrl_human Human No 5.8 IC50 = 1583 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 4.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL381798 calrl_human Human No 5.8 IC50 = 1583 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 4.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL406459 calrl_human Human Yes 6.8 IC50 = 159 Funct
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.
1170 31 13 16 -0.4 CC(C)C(C(=O)NCC(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)N
CHEMBL438120 calrl_human Human No 7.8 IC50 = 16 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
556 6 2 7 1.9 CN(C)CCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL438120 calrl_human Human No 7.8 IC50 = 16 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
556 6 2 7 1.9 CN(C)CCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL2369464 calrl_human Human No 7.8 IC50 = 16 Funct
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.
2788 92 40 39 -9.5 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)N
CHEMBL480999 calrl_human Human No 6.8 IC50 = 160 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 3 2 5 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5C6(C4=O)CCOCC6
CHEMBL3114475 calrl_human Human No 6.8 IC50 = 160 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
620 8 1 6 4.1 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5N6CCOCC6
CHEMBL480999 calrl_human Human No 6.8 IC50 = 160 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 3 2 5 1.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5C6(C4=O)CCOCC6
CHEMBL257094 calrl_human Human No 6.8 IC50 = 164 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
525 6 2 7 1.4 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL257094 calrl_human Human No 6.8 IC50 = 164 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
525 6 2 7 1.4 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL2369464 calrl_rat Rat No 7.8 IC50 = 17.9 Funct
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
2788 92 40 39 -9.5 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)N
CHEMBL270796 calrl_human Human No 6.8 IC50 = 170 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
505 6 3 6 0.8 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=C(C=C5)O
CHEMBL220101 calrl_human Human No 6.8 IC50 = 170 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
476 4 2 5 0.9 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6CCOC6
CHEMBL2059895 calrl_human Human No 6.8 IC50 = 170 Funct
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
600 5 2 5 4.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC6=O
CHEMBL2018499 calrl_human Human No 6.8 IC50 = 170 Funct
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
613 7 3 6 3.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NN=C7
CHEMBL3114473 calrl_human Human No 6.8 IC50 = 170 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
571 7 1 6 4.6 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=C(C=CC=C5F)F
CHEMBL270796 calrl_human Human No 6.8 IC50 = 170 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
505 6 3 6 0.8 COCCN1C=C(C=C(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=CC=C(C=C5)O
CHEMBL220101 calrl_human Human No 6.8 IC50 = 170 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
476 4 2 5 0.9 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6CCOC6
CHEMBL411804 calrl_human Human No 6.8 IC50 = 170 Funct
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.
1184 31 13 16 -0.2 CC(C)C(C(=O)NCC(=O)NC(C)(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)N
CHEMBL2059895 calrl_human Human No 6.8 IC50 = 170 Funct
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
600 5 2 5 4.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC6=O
CHEMBL2018499 calrl_human Human No 6.8 IC50 = 170 Funct
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
613 7 3 6 3.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NN=C7
CHEMBL198232 calrl_human Human No 4.8 IC50 = 17000 Funct
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
717 17 5 5 5.6 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL196582 calrl_human Human No 4.8 IC50 = 17000 Funct
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
717 17 5 5 5.6 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL198232 calrl_human Human No 4.8 IC50 = 17000 Funct
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
717 17 5 5 5.6 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL196582 calrl_human Human No 4.8 IC50 = 17000 Funct
Antagonist activity against human CGRP receptorAntagonist activity against human CGRP receptor
717 17 5 5 5.6 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)NCCC3=CC=CC=C3
CHEMBL313797 calrl_human Human No 4.8 IC50 = 17000 Funct
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
455 5 1 5 5.5 CCC1CN2CCC1CC2C(C3=CC(=NC4=C3C=C(C=C4)OC)C5=CC(=C(C=C5)F)Cl)O
CHEMBL2024587 calrl_human Human No 7.8 IC50 = 18 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 6 2 4 3.7 CC1=CN=C(C=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL257252 calrl_human Human No 7.8 IC50 = 18 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 9 2.6 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=C(C(=CC=C5)F)F
CHEMBL2024587 calrl_human Human No 7.8 IC50 = 18 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 6 2 4 3.7 CC1=CN=C(C=C1)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL257252 calrl_human Human No 7.8 IC50 = 18 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 9 2.6 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=C(C(=CC=C5)F)F
CHEMBL2018498 calrl_human Human No 6.8 IC50 = 180 Funct
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 5 4.0 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NC=C7
CHEMBL374666 calrl_human Human No 6.8 IC50 = 180 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)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=CC(=CC(=C6)F)F
CHEMBL3114470 calrl_human Human No 6.8 IC50 = 180 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
553 7 1 5 4.5 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=CC=CC=C5F
CHEMBL2018498 calrl_human Human No 6.8 IC50 = 180 Funct
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 5 4.0 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NC=C7
CHEMBL374666 calrl_human Human No 6.8 IC50 = 180 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)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=CC(=CC(=C6)F)F
CHEMBL240686 calrl_human Human No 5.8 IC50 = 1800 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
455 3 3 5 1.2 C1CC(C(=O)NCC1C2=CSC=C2)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL240686 calrl_human Human No 5.8 IC50 = 1800 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
455 3 3 5 1.2 C1CC(C(=O)NCC1C2=CSC=C2)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL267406 calrl_human Human No 4.8 IC50 = 18000 Funct
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.
987 29 15 17 -5.3 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C(CC2=CC=C(C=C2)O)N
CHEMBL215424 calrl_human Human No 5.7 IC50 = 1837 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
592 4 2 8 3.1 C1CN(CCC1N2CC3=C(C=CC=N3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL215424 calrl_human Human No 5.7 IC50 = 1837 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
592 4 2 8 3.1 C1CN(CCC1N2CC3=C(C=CC=N3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL1794015 calrl_human Human No 6.7 IC50 = 185 Funct
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
3189 105 47 51 -17.4 CC(C)CC(C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)O)NC(=O)COCCOCCNC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL428247 calrl_human Human No 6.7 IC50 = 186 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 8 2.5 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=CC=C5F
CHEMBL428247 calrl_human Human No 6.7 IC50 = 186 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 8 2.5 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=CC=C5F
CHEMBL1770558 calrl_human Human No 7.7 IC50 = 19 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
508 3 2 6 1.9 C1CC(C2=NC=CN2CC1C3=C(C(=CC=C3)F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL2018512 calrl_human Human No 7.7 IC50 = 19 Funct
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
530 5 2 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCCCC6)C=NN2
CHEMBL1770558 calrl_human Human No 7.7 IC50 = 19 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
508 3 2 6 1.9 C1CC(C2=NC=CN2CC1C3=C(C(=CC=C3)F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL3114488 calrl_human Human No 7.7 IC50 = 19 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
647 8 1 6 4.8 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CCC4=CC=CC=C4NC3=O)C5=CC=CC=C5N6CCN(CC6)C
CHEMBL2018512 calrl_human Human No 7.7 IC50 = 19 Funct
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
530 5 2 5 3.1 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC4(CC3)C5=CC=CC=C5NC(=O)O4)C(=O)N6CCCCC6)C=NN2
CHEMBL3114472 calrl_human Human No 6.7 IC50 = 190 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
571 7 1 6 4.6 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=C(C=C(C=C5)F)F
CHEMBL3350392 calrl_human Human No 4.7 IC50 = 19000 Funct
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.
1183 33 16 19 -4.6 CC(C)C(C(=O)NCC(=O)NC(CO)C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C(CC3=CC=C(C=C3)O)N
CHEMBL214800 calrl_human Human No 6.7 IC50 = 193 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
633 6 2 8 4.4 COC1=CC=C(C=C1)C2=CN(C(=O)N2)C3CCN(CC3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL214800 calrl_human Human No 6.7 IC50 = 193 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
633 6 2 8 4.4 COC1=CC=C(C=C1)C2=CN(C(=O)N2)C3CCN(CC3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1770720 calrl_human Human No 8.7 IC50 = 2 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 10 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL2018511 calrl_human Human No 8.7 IC50 = 2 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
557 6 2 4 3.4 CC1CCN(CC1)C(=O)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL237662 calrl_human Human No 8.7 IC50 = 2 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
543 6 2 7 1.7 COCCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL237663 calrl_human Human No 8.7 IC50 = 2 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
539 5 2 6 2.6 C1CC1CN2CC(CCC(C2=O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL392635 calrl_human Human No 8.7 IC50 = 2 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
576 5 2 7 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC3=CC=CC=N3)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL415263 calrl_human Human No 8.7 IC50 = 2 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
559 6 2 7 2.5 CSCCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL392636 calrl_human Human No 8.7 IC50 = 2 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
591 6 2 8 1.3 CS(=O)(=O)CCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL562069 calrl_human Human No 8.7 IC50 = 2 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 4 1.8 C1C2=CN(C3=C2C(=CC=C3)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 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 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2024596 calrl_human Human No 8.7 IC50 = 2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
541 7 3 6 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CO)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1770720 calrl_human Human No 8.7 IC50 = 2 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 10 3.4 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC(=O)O5)N=CC=C6
CHEMBL3114494 calrl_human Human No 8.7 IC50 = 2 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
679 9 1 7 5.2 CCN1CCN(CC1)C2=C(C=CC=C2F)C3N(C(=O)C(S3)CC(=O)N4CCC(CC4)N5CCC6=CC=CC=C6NC5=O)CCC(C)(C)C
CHEMBL2018511 calrl_human Human No 8.7 IC50 = 2 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
557 6 2 4 3.4 CC1CCN(CC1)C(=O)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL237662 calrl_human Human No 8.7 IC50 = 2 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
543 6 2 7 1.7 COCCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL237663 calrl_human Human No 8.7 IC50 = 2 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
539 5 2 6 2.6 C1CC1CN2CC(CCC(C2=O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL392635 calrl_human Human No 8.7 IC50 = 2 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
576 5 2 7 2.3 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC3=CC=CC=N3)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL415263 calrl_human Human No 8.7 IC50 = 2 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
559 6 2 7 2.5 CSCCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL392636 calrl_human Human No 8.7 IC50 = 2 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
591 6 2 8 1.3 CS(=O)(=O)CCN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL562069 calrl_human Human No 8.7 IC50 = 2 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 4 1.8 C1C2=CN(C3=C2C(=CC=C3)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2 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 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2369459 calrl_human Human No 8.7 IC50 = 2 Funct
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
3789 110 55 57 -15.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)O)CC(=O)O)NC(=O)C(C)N)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C(C)C)C(=O)N4CCCC4C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC5=CC=CC=C5)C(=O)N)C(C)O
CHEMBL2024596 calrl_human Human No 8.7 IC50 = 2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma 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 3 4 4.3 CC1=C2C(=CC(=C1)CC(C3=NC4=CC=CC=C4C=C3)NC(=O)N5CCC(CC5)N6CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
541 7 3 6 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CO)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL3037882 calrl_human Human No 8.7 IC50 = 2 Funct
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)
3793 122 58 59 -20.9 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)O)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL3037882 calrl_human Human No 8.7 IC50 = 2 Funct
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
3793 122 58 59 -20.9 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)O)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2.1 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
541 7 3 6 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CO)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL2024602 calrl_human Human No 8.7 IC50 = 2.1 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
541 7 3 6 2.7 CC1=C2C(=CC(=C1)CC(C3=NC=CC(=C3)CO)OC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O)C=NN2
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 Funct
Antagonist activity against human CGRP receptor by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor by cell based cAMP accumulation assay
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1092838 calrl_human Human No 8.7 IC50 = 2.2 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 5 2.2 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C(=O)NC(=O)N7C)C=C5C=C4
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 Funct
Antagonist activity against human CGRP receptor by cell based cAMP accumulation assayAntagonist activity against human CGRP receptor by cell based cAMP accumulation assay
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL236593 calrl_human Human Yes 8.7 IC50 = 2.2 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1092838 calrl_human Human No 8.7 IC50 = 2.2 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 5 2.2 CC12CC(=O)NC3=C1C(=CC=C3)N(C2)CC4=NC5=CC6=C(CC7(C6)C(=O)NC(=O)N7C)C=C5C=C4
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.3 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
576 3 2 10 2.6 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.3 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
576 3 2 10 2.6 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL525571 calrl_human Human No 8.6 IC50 = 2.3 Funct
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
3126 104 47 44 -9.3 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL2369463 calrl_human Human No 8.6 IC50 = 2.3 Funct
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
3027 99 44 43 -10.8 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)N
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 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 5 -0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CN6C4=O
CHEMBL1770556 calrl_human Human No 8.6 IC50 = 2.4 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 7 1.9 C1CC1C2=NN=C3N2CC(CCC3NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL564088 calrl_human Human Yes 8.6 IC50 = 2.4 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
466 3 3 5 1.6 C1C2CN(C3=CC=CC(=C23)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL236593 calrl_human Human Yes 8.6 IC50 = 2.4 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 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 5 -0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CN6C4=O
CHEMBL466192 calrl_human Human No 8.6 IC50 = 2.4 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 5 0.2 CC1=CC2=C3C(=C1)NC(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 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 5 -0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CN6C4=O
CHEMBL1770556 calrl_human Human No 8.6 IC50 = 2.4 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 7 1.9 C1CC1C2=NN=C3N2CC(CCC3NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6)C7=C(C(=CC=C7)F)F
CHEMBL236593 calrl_human Human Yes 8.6 IC50 = 2.4 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
567 4 2 9 3.0 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL453643 calrl_human Human No 8.6 IC50 = 2.4 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 5 -0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CN6C4=O
CHEMBL2369459 calrl_rat Rat No 8.6 IC50 = 2.4 Funct
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
3789 110 55 57 -15.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N1)C(C)O)CC(=O)O)NC(=O)C(C)N)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(C(C)C)C(=O)N4CCCC4C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC5=CC=CC=C5)C(=O)N)C(C)O
CHEMBL1092882 calrl_human Human No 8.6 IC50 = 2.5 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
489 2 2 5 1.7 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=C8C(=CC=C7)NC(=O)CN8C6=O
CHEMBL464078 calrl_human Human No 8.6 IC50 = 2.5 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
526 4 2 5 3.0 C1CSCCC1N2C3=CC=CC=C3N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1092882 calrl_human Human No 8.6 IC50 = 2.5 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
489 2 2 5 1.7 C1C2=C(CC13C4=C(NC3=O)N=CC=C4)C=C5C(=C2)C=CC(=N5)CN6C7=C8C(=CC=C7)NC(=O)CN8C6=O
CHEMBL464078 calrl_human Human No 8.6 IC50 = 2.5 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
526 4 2 5 3.0 C1CSCCC1N2C3=CC=CC=C3N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL1770566 calrl_human Human No 8.6 IC50 = 2.6 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
584 4 2 6 3.6 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6C7=C(NC6=O)N=CC=C7
CHEMBL1770557 calrl_human Human No 8.6 IC50 = 2.6 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 9 3.3 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL1770566 calrl_human Human No 8.6 IC50 = 2.6 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
584 4 2 6 3.6 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)C4=CC=CC=C4)NC(=O)N5CCC(CC5)N6C7=C(NC6=O)N=CC=C7
CHEMBL1770557 calrl_human Human No 8.6 IC50 = 2.6 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 9 3.3 C1CC(C2=NC=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
CHEMBL382469 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
856 12 5 8 3.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.7 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
576 3 2 10 2.6 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL570746 calrl_human Human No 8.6 IC50 = 2.7 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
568 3 2 10 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5
CHEMBL3288290 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
766 12 4 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL2018511 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
557 6 2 4 3.4 CC1CCN(CC1)C(=O)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL382469 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
856 12 5 8 3.2 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC(=C(C(=C4)Br)O)Br)C(=O)NC(CCCCN)C(=O)N5CCN(CC5)C6=CC=NC=C6
CHEMBL1770721 calrl_human Human No 8.6 IC50 = 2.7 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
576 3 2 10 2.6 C1CC(C2=NN=C(N2CC1C3=C(C(=CC=C3)F)F)CC(F)(F)F)NC(=O)N4CCC5(CC4)C6=C(NC5=O)N=CC=C6
CHEMBL570746 calrl_human Human No 8.6 IC50 = 2.7 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
568 3 2 10 3.1 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5
CHEMBL3288290 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
766 12 4 9 3.1 C1CN(CCC1N2C(=O)C3=CC=CC=C3NC2=O)C(=O)NC(CC4=CC5=CC=CC=C5S4)C(=O)NC(CCCCN)C(=O)N6CCN(CC6)C7=CC=NC=C7
CHEMBL2018511 calrl_human Human No 8.6 IC50 = 2.7 Funct
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
557 6 2 4 3.4 CC1CCN(CC1)C(=O)C(CC2=CC(=C3C(=C2)C=NN3)C)CC(=O)N4CCC(CC4)N5CC6=CC=CC=C6NC5=O
CHEMBL1770726 calrl_human Human No 8.5 IC50 = 2.9 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
595 5 2 8 2.7 CCOC(C)(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL1770726 calrl_human Human No 8.5 IC50 = 2.9 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
595 5 2 8 2.7 CCOC(C)(C)C1=CN=C2N1CC(CCC2NC(=O)N3CCC4(CC3)C5=C(NC(=O)O4)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL2430163 calrl_human Human No 8.5 IC50 = 2.9 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
552 6 3 6 2.5 CC1=C2C(=CC(=C1)CC(C3=NC=C4N3CCNC4)OC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O)C=NN2
CHEMBL2024171 calrl_human Human No 7.7 IC50 = 20 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
527 6 2 5 3.4 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C6=CC=CC=N6)C=NN2
CHEMBL2059905 calrl_human Human No 7.7 IC50 = 20 Funct
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
616 5 2 6 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL2059900 calrl_human Human No 7.7 IC50 = 20 Funct
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 6 4.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=CC=C7
CHEMBL2024171 calrl_human Human No 7.7 IC50 = 20 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
527 6 2 5 3.4 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)N4CC5=C(C(=CC=C5)F)NC4=O)C6=CC=CC=N6)C=NN2
CHEMBL2059905 calrl_human Human No 7.7 IC50 = 20 Funct
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
616 5 2 6 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C7=CC=CC=C7NC(=O)O6
CHEMBL2059900 calrl_human Human No 7.7 IC50 = 20 Funct
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 6 4.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CC=CC=C7
CHEMBL2369464 calrl_human Human No 7.7 IC50 = 20.2 Funct
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
2788 92 40 39 -9.5 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCN=C(N)N)N
CHEMBL198925 calrl_human Human No 6.7 IC50 = 200 Funct
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
790 15 5 8 3.9 COC1=CC=CC(=C1)CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)N3CCN(CC3)C4=CC=NC=C4
CHEMBL198925 calrl_human Human No 6.7 IC50 = 200 Funct
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
790 15 5 8 3.9 COC1=CC=CC(=C1)CCNC(=O)NC(CC2=CC(=C(C(=C2)Br)O)Br)C(=O)NC(CCCCN)C(=O)N3CCN(CC3)C4=CC=NC=C4
CHEMBL429765 calrl_human Human No 6.7 IC50 = 200 Funct
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.
1023 27 12 15 -1.8 CC(C)C(C(=O)N1CCCC1C(=O)NC(C(C)O)C(=O)NC(CC(=O)O)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)O)N
CHEMBL471530 calrl_human Human No 5.7 IC50 = 2000 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
440 3 3 4 1.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C(=CC=C5)Cl)NC4=O
CHEMBL471530 calrl_human Human No 5.7 IC50 = 2000 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
440 3 3 4 1.3 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C(C(=CC=C5)Cl)NC4=O
CHEMBL268539 calrl_human Human No 6.7 IC50 = 205 Funct
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.
1212 32 13 16 2.1 CC(C)C(C(=O)NCC(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)NC(=O)C
CHEMBL255966 calrl_human Human No 6.7 IC50 = 209 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 7 2.4 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=CC=C5
CHEMBL255966 calrl_human Human No 6.7 IC50 = 209 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 7 2.4 C1CN(CCC1N2C3=C(NC2=O)N=CC=C3)C(=O)NC4=CC(=CN(C4=O)CC(F)(F)F)C5=CC=CC=C5
CHEMBL455674 calrl_human Human No 7.7 IC50 = 21 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
489 3 3 5 0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CCCN6C4=O
CHEMBL237663 calrl_human Human No 7.7 IC50 = 21 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
539 5 2 6 2.6 C1CC1CN2CC(CCC(C2=O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL570748 calrl_human Human No 7.7 IC50 = 21 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
542 4 2 9 2.6 CC1=NNC(=O)C(=C1)C2CCN(CC2)C(=O)NC3CCC(CN(C3=O)CC(F)(F)F)C4=C(C(=CC=C4)F)F
CHEMBL455674 calrl_human Human No 7.7 IC50 = 21 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
489 3 3 5 0.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=C6C(=CC=C5)NC(=O)CCCN6C4=O
CHEMBL237663 calrl_human Human No 7.7 IC50 = 21 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
539 5 2 6 2.6 C1CC1CN2CC(CCC(C2=O)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5)C6=C(C(=CC=C6)F)F
CHEMBL570748 calrl_human Human No 7.7 IC50 = 21 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
542 4 2 9 2.6 CC1=NNC(=O)C(=C1)C2CCN(CC2)C(=O)NC3CCC(CN(C3=O)CC(F)(F)F)C4=C(C(=CC=C4)F)F
CHEMBL2369465 calrl_human Human No 7.7 IC50 = 21.9 Funct
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.
3041 98 43 43 -8.9 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL2059904 calrl_human Human No 6.7 IC50 = 210 Funct
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 7 3.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CN=CC=C7
CHEMBL3114471 calrl_human Human No 6.7 IC50 = 210 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
571 7 1 6 4.6 CC(C)(C)CCN1C(SC(C1=O)CC(=O)N2CCC(CC2)N3CC4=CC=CC=C4NC3=O)C5=C(C(=CC=C5)F)F
CHEMBL2059904 calrl_human Human No 6.7 IC50 = 210 Funct
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 7 3.4 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)C(=O)NC(=N6)C7=CN=CC=C7
CHEMBL237664 calrl_human Human No 7.7 IC50 = 22 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
499 3 2 6 1.9 CN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL237661 calrl_human Human No 7.7 IC50 = 22 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
485 3 3 6 1.7 C1CC(C(=O)NCC1C2=C(C(=CC=C2)F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL237664 calrl_human Human No 7.7 IC50 = 22 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
499 3 2 6 1.9 CN1CC(CCC(C1=O)NC(=O)N2CCC(CC2)N3C4=C(NC3=O)N=CC=C4)C5=C(C(=CC=C5)F)F
CHEMBL237661 calrl_human Human No 7.7 IC50 = 22 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
485 3 3 6 1.7 C1CC(C(=O)NCC1C2=C(C(=CC=C2)F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL2369457 calrl_rat Rat No 7.7 IC50 = 22 Funct
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
3084 100 45 44 -11.4 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CNC=N4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)N
CHEMBL405544 calrl_human Human No 6.7 IC50 = 220 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
655 5 2 9 3.5 CS(=O)(=O)C1=CC2=C(C=C1)N(C(=O)N2)C3CCN(CC3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL453644 calrl_human Human No 6.7 IC50 = 220 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 5 0.1 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL391660 calrl_human Human No 6.7 IC50 = 220 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC(=CC=C2)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1162991 calrl_human Human No 6.7 IC50 = 220 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL520778 calrl_human Human No 6.7 IC50 = 220 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
506 4 2 5 2.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6CCSCC6
CHEMBL2018502 calrl_human Human No 6.7 IC50 = 220 Funct
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
623 7 2 5 5.1 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC=CC7=CC=CC=C76
CHEMBL405544 calrl_human Human No 6.7 IC50 = 220 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
655 5 2 9 3.5 CS(=O)(=O)C1=CC2=C(C=C1)N(C(=O)N2)C3CCN(CC3)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL453644 calrl_human Human No 6.7 IC50 = 220 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 5 0.1 CN1C(=O)CN2C3=C(C=CC=C31)N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4
CHEMBL391660 calrl_human Human No 6.7 IC50 = 220 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
467 3 3 5 1.6 C1CC(C(=O)NCC1C2=CC(=CC=C2)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL1162991 calrl_human Human No 6.7 IC50 = 220 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
489 3 2 5 0.4 CC1=CC2=C3C(=C1)N(C(=O)CN3C(=O)N2CC(=O)NC4=CC5=C(CC6(C5)C(=O)NC(=O)N6C)C=C4)C
CHEMBL520778 calrl_human Human No 6.7 IC50 = 220 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
506 4 2 5 2.1 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6CCSCC6
CHEMBL20034 calrl_human Human No 6.7 IC50 = 220 Funct
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.
924 25 12 14 -2.1 CC(C)C(C(=O)NCC(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(C(C)O)NC(=O)C3CCCN3
CHEMBL2018502 calrl_human Human No 6.7 IC50 = 220 Funct
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
623 7 2 5 5.1 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC=CC7=CC=CC=C76
CHEMBL427743 calrl_human Human No 6.7 IC50 = 224 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
592 4 2 8 3.1 C1CN(CCC1N2CC3=C(C=NC=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL427743 calrl_human Human No 6.7 IC50 = 224 Funct
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP productionActivity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
592 4 2 8 3.1 C1CN(CCC1N2CC3=C(C=NC=C3)NC2=O)C(=O)NC4C(=O)N(C5=CC=CC=C5C(=N4)C6=CC=CC=C6)CC(F)(F)F
CHEMBL194631 calrl_human Human No 6.7 IC50 = 226 Funct
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
831 13 4 9 3.7 COC1=CC=CC=C1N2CCN(CC2)C(=O)NC(CC3=CC(=C(C(=C3)Br)O)Br)C(=O)NC(CCCCN)C(=O)N4CCN(CC4)C5=CC=NC=C5
CHEMBL194631 calrl_human Human No 6.7 IC50 = 226 Funct
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
831 13 4 9 3.7 COC1=CC=CC=C1N2CCN(CC2)C(=O)NC(CC3=CC(=C(C(=C3)Br)O)Br)C(=O)NC(CCCCN)C(=O)N4CCN(CC4)C5=CC=NC=C5
CHEMBL471358 calrl_human Human No 7.6 IC50 = 23 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 4 1.4 CC1=CC(=C2C(=C1)N(C(=O)N2)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL236590 calrl_human Human No 7.6 IC50 = 23 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
529 5 3 7 1.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCO)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL549503 calrl_human Human Yes 7.6 IC50 = 23 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 5 2.0 C1CC(=O)NC2=C3C1CN(C3=CC=C2)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL577110 calrl_human Human No 7.6 IC50 = 23 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 9 3.6 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C(=O)NC(=N4)C5=CC=CC=C5
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2059896 calrl_human Human No 7.6 IC50 = 23 Funct
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 2 5 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CC(=O)NC7=CC=CC=C67
CHEMBL471358 calrl_human Human No 7.6 IC50 = 23 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 4 1.4 CC1=CC(=C2C(=C1)N(C(=O)N2)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL236590 calrl_human Human No 7.6 IC50 = 23 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
529 5 3 7 1.2 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CCO)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
CHEMBL549503 calrl_human Human Yes 7.6 IC50 = 23 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 5 2.0 C1CC(=O)NC2=C3C1CN(C3=CC=C2)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL577110 calrl_human Human No 7.6 IC50 = 23 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 9 3.6 C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC4(CC3)C(=O)NC(=N4)C5=CC=CC=C5
CHEMBL519421 calrl_human Human No 7.6 IC50 = 23 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
519 5 2 5 1.2 CC1=CC(=C2C(=C1)N(C(=O)N2CC(=O)N(C)C)CC(=O)NC3=CC4=C(CC5(C4)C(=O)NC(=O)N5C)C=C3)C
CHEMBL2059896 calrl_human Human No 7.6 IC50 = 23 Funct
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 2 5 4.7 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC3=CSC4=CC=CC=C43)NC(=O)N5CCC6(CC5)CC(=O)NC7=CC=CC=C67
CHEMBL2018499 calrl_human Human No 6.6 IC50 = 230 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
613 7 3 6 3.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NN=C7
CHEMBL2018499 calrl_human Human No 6.6 IC50 = 230 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
613 7 3 6 3.5 C1CCN(CC1)C2CCN(CC2)C(=O)C(CC(=O)N3CCC(CC3)N4CC5=CC=CC=C5NC4=O)NC6=CC7=C(C=C6)NN=C7
CHEMBL455670 calrl_human Human No 7.6 IC50 = 24 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
519 7 2 5 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CCCC(=O)N(C)C
CHEMBL564088 calrl_human Human Yes 7.6 IC50 = 24 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
466 3 3 5 1.6 C1C2CN(C3=CC=CC(=C23)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL464078 calrl_human Human No 7.6 IC50 = 24 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
526 4 2 5 3.0 C1CSCCC1N2C3=CC=CC=C3N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL2024591 calrl_human Human No 7.6 IC50 = 24 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
506 6 2 4 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C6=CC=CC=N6)C=NN2
CHEMBL375533 calrl_human Human No 7.6 IC50 = 24 Funct
Inhibition of CGRP-induced cAMP production in E10 cellsInhibition of CGRP-induced cAMP production in E10 cells
489 4 2 6 1.8 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)C6=NC=CS6
CHEMBL455670 calrl_human Human No 7.6 IC50 = 24 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
519 7 2 5 0.7 CN1C(=O)NC(=O)C12CC3=C(C2)C=C(C=C3)NC(=O)CN4C5=CC=CC=C5N(C4=O)CCCC(=O)N(C)C
CHEMBL564088 calrl_human Human Yes 7.6 IC50 = 24 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
466 3 3 5 1.6 C1C2CN(C3=CC=CC(=C23)NC1=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL464078 calrl_human Human No 7.6 IC50 = 24 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
526 4 2 5 3.0 C1CSCCC1N2C3=CC=CC=C3N(C2=O)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4
CHEMBL2024591 calrl_human Human No 7.6 IC50 = 24 Funct
Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation countingDisplacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting
506 6 2 4 4.0 CC1=C2C(=CC(=C1)CC(CC(=O)N3CCC(CC3)C4=CC5=CC=CC=C5NC4=O)C6=CC=CC=N6)C=NN2
CHEMBL375533 calrl_human Human No 7.6 IC50 = 24 Funct