ChEMBL ligand: CHEMBL236593 (Mk-0974, MK-0974, MK0974, Telcagepant)
Calcitonin gene-related peptide 1 in Human [ChEMBL: CHEMBL5293] [UniProtKB: P06881] Calcitonin gene-related peptide 1 in Rat [ChEMBL: CHEMBL5735] [UniProtKB: P01256] There should be some charts here, you may need to enable JavaScript!
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602] There should be some charts here, you may need to enable JavaScript!
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602] There should be some charts here, you may need to enable JavaScript!
CGRP receptor in Human [GtoPdb: 48] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Calcitonin gene-related peptide 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5293] [UniProtKB: P06881]
ChEMBL	Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	B	4	pKi	>100000	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
ChEMBL	Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay	B	9.11	pKi	0.78	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
ChEMBL	Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	B	8.66	pIC50	2.2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
Calcitonin gene-related peptide 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5735] [UniProtKB: P01256]
ChEMBL	Inhibition of rat CGRP	B	5.92	pKi	1200	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602]
ChEMBL	Inhibition of human CLR/RAMP1	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2020) 63: 6600-6623 [PMID:32058712]
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602]
ChEMBL	Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries	B	8.43	pKd	3.71	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound	B	8.72	pKd	1.9	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Displacement of [125I]-CGRP from human recombinant CGRP receptor	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
ChEMBL	Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cells	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	Antagonist activity at human CGRP receptor	B	9.11	pKi	0.77	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3157-3161 [PMID:23632269]
ChEMBL	Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells	B	9.11	pKi	0.77	nM	Ki	ACS Med Chem Lett (2013) 4: 863-868 [PMID:24900761]
ChEMBL	Binding affinity to human CGRP receptor	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assay	F	7.96	pIC50	11	nM	IC50	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum	F	7.96	pIC50	11	nM	IC50	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	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 serum	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	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 assay	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
ChEMBL	Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	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	F	8.62	pIC50	2.4	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	Antagonist activity against human CGRP receptor by cell based cAMP accumulation assay	F	8.66	pIC50	2.2	nM	IC50	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production	F	8.66	pIC50	2.2	nM	IC50	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	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 assay	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
CGRP receptor in Human [GtoPdb: 48]
GtoPdb	-	-	9.1	pKi	-	-	-	J Pharmacol Exp Ther (2008) 324: 416-21 [PMID:18039958]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]