ubrogepant [Ligand Id: 10176] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2364638 (MK-1602, Ubrelvy, Ubrogepant, Ubrogepant anhydrous)
  • RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human [ChEMBL: CHEMBL2107838] [GtoPdb: 5147] [UniProtKB: O60894Q16602]
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  • CGRP receptor in Human [GtoPdb: 48]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2107838] [GtoPdb: 5147] [UniProtKB: O60894Q16602]
ChEMBL Displacement of [125I]hCGRP from human recombinant CGRP receptor expressed in HEK293 cell membranes incubated for 3 hrs by scintillation counting method B 10.17 pKi 0.07 nM Ki US-8481556-B2. Piperidinone carboxamide azaindane CGRP receptor antagonists (2013)
ChEMBL Antagonist activity at human CLR/RAMP1 B 10.17 pKi 0.07 nM Ki J Med Chem (2020) 63: 6600-6623 [PMID:32058712]
CGRP receptor in Human [GtoPdb: 48]

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]