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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 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]