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ChEMBL ligand: CHEMBL458767 (SR-12813) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]