ChEMBL ligand: CHEMBL207197 (Bibn 4096 bs, Bibn-4096bs, BIBN 4096 BS, BIBN-4096 BS, BIBN-4096BS, Olcegepant)
Calcitonin gene-related peptide 1 in Human [ChEMBL: CHEMBL5293] [UniProtKB: P06881] 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] calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Rat [ChEMBL: CHEMBL4755] [GtoPdb: 47] [UniProtKB: Q63118] There should be some charts here, you may need to enable JavaScript!
AMY1 receptor in Human [GtoPdb: 44] 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	Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay	B	10.85	pKi	0.01	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	Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method	B	10.5	pKi	0.03	nM	Ki	J Med Chem (2020) 63: 7906-7920 [PMID:32558564]
ChEMBL	Antagonist activity at human cloned CLR/RAMP1 receptor expressed in E10 cells measured as inhibition of CGRP-mediated cAMP production	F	10	pIC50	0.1	nM	IC50	Bioorg Med Chem Lett (2006) 16: 2595-2598 [PMID:16527483]
ChEMBL	Inhibition of human CLR/RAMP1	B	10.52	pIC50	0.03	nM	IC50	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 cerebral arteries	B	10.1	pKd	0.08	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries	B	10.4	pKd	0.04	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 180 mins by gamma counting	B	10.85	pKi	0.01	nM	Ki	Bioorg Med Chem Lett (2012) 22: 3941-3945 [PMID:22607672]
ChEMBL	Binding affinity to human CGRP receptor	B	10.85	pKi	0.01	nM	Ki	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells	B	11	pKi	0.01	nM	Ki	ACS Med Chem Lett (2012) 3: 337-341 [PMID:24900474]
ChEMBL	Antagonist activity at human CGRP receptor	B	11	pKi	0.01	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3157-3161 [PMID:23632269]
ChEMBL	Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting	B	11	pKi	0.01	nM	Ki	Bioorg Med Chem Lett (2014) 24: 845-849 [PMID:24405707]
ChEMBL	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 assay	F	8.4	pIC50	4	nM	IC50	Bioorg Med Chem Lett (2014) 24: 845-849 [PMID:24405707]
ChEMBL	Antagonist activity against human CGRP receptor	B	10.52	pIC50	0.03	nM	IC50	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells	B	10.7	pIC50	0.02	nM	IC50	Bioorg Med Chem Lett (2012) 22: 4719-4722 [PMID:22732695]
ChEMBL	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 radioimmunoassay	B	10.59	pEC50	0.03	nM	EC50	Bioorg Med Chem Lett (2014) 24: 2744-2748 [PMID:24794104]
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4755] [GtoPdb: 47] [UniProtKB: Q63118]
ChEMBL	Displacement of [125I]CGRP from CGRP receptor in rat spleen homogenate after 180 mins by gamma counting	B	8.47	pKi	3.4	nM	Ki	Bioorg Med Chem Lett (2012) 22: 3941-3945 [PMID:22607672]
ChEMBL	Binding affinity to rat CGRP receptor	B	8.47	pKi	3.4	nM	Ki	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
AMY1 receptor in Human [GtoPdb: 44]
CGRP receptor in Human [GtoPdb: 48]
GtoPdb	-	-	11	pKi	0.01	nM	Ki	J Biol Chem (2002) 277: 14294-8 [PMID:11847213]; Br J Pharmacol (2000) 129: 420-3 [PMID:10711339]; Br J Pharmacol (2003) 140: 477-86 [PMID:12970090]; Mol Pharmacol (2006) 70: 1984-1991 [PMID:16959943]; Bioorg Med Chem Lett (2014) 24: 845-9 [PMID:24405707]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]