rifaximin [Ligand Id: 12012] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1617 (L-105, Normix, NSC-758957, Rifacol, Rifamycin l 105, Rifaxidin, Rifaximin, Rifaximina, Rifaximine, Targaxan, Xifaxan, Xifaxanta, Xifaxsan)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Transactivation of full length human PXR transfected in human HepG2 cells after 18 hrs by luciferase reporter assay relative to rifaximin B 4.95 pEC50 11200 nM EC50 Eur J Med Chem (2015) 103: 551-562 [PMID:26408814]
ChEMBL Agonist activity at human full-length PXR transfected in human HepG2 cells co-transfected with pSG5-RXR assessed as induction of transactivation by dual-luciferase reporter gene assay B 5.4 pEC50 4000 nM EC50 Eur J Med Chem (2014) 73: 126-134 [PMID:24388834]
ChEMBL Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay B 5.66 pEC50 2200 nM EC50 J Med Chem (2011) 54: 4590-4599 [PMID:21599020]

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]