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 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]