SR12813 [Ligand Id: 2763] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL458767 (SR-12813)
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
ChEMBL Induction of degradation of Flag-tagged human HMGCR-dCat-ELuc membrane domain (1 to 499 residues) expressed in HEK293 cells assessed as reduction in HMGCR-dCat-Eluc protein level after 4 hrs by luciferase reporter assay B 5.96 pEC50 1100 nM EC50 Bioorg Med Chem (2020) 28: 115576-115576 [PMID:32616181]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Activation of PXR in human LS180 cells assessed as P-gp induction by measuring intracellular accumulation of rhodamine 123 preincubated for 48 hrs followed by rhodamine 123 addition after 40 mins and measured after 90 mins by fluorescence assay B 5.9 pEC50 1250 nM EC50 Medchemcomm (2016) 7: 1910-1915
GtoPdb - - 6.7 pEC50 - - - Mol Endocrinol (2000) 14: 27-39 [PMID:10628745]
ChEMBL Agonist activity at human pregnane X receptor expressed in HEK293 cells by luciferase reporter gene assay B 7.1 pEC50 80 nM EC50 Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688]
ChEMBL Agonist activity at human PXR B 7.22 pEC50 60 nM EC50 J Med Chem (2016) 59: 9201-9214 [PMID:27652492]

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]