tapinarof [Ligand Id: 9686] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL259571 (Benvitimod, GSK-2894512, GSK2894512, Tapinarof, Vtama, Wbi-1001, WBI-1001)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aryl hydrocarbon receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3201] [GtoPdb: 2951] [UniProtKB: P35869]
GtoPdb Direct binding of tapinarof to the AhR-ARNT heterodimer by fluorescence assay. - 7 pKd 100 nM Kd J Invest Dermatol (2017) 137: 2110-2119 [PMID:28595996]
ChEMBL Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay B 7.56 pEC50 27.34 nM EC50 Eur J Med Chem (2022) 231: 114122-114122 [PMID:35123295]

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]