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ChEMBL ligand: CHEMBL207197 (Bibn 4096 bs, Bibn-4096bs, BIBN 4096 BS, BIBN-4096 BS, BIBN-4096BS, Olcegepant) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]