fluvastatin [Ligand Id: 2951] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1078 (Fluvastatin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] | ||||||||
| ChEMBL | Inhibition of human recombinant NTCP expressed in CHO cells assessed as reduction in [3H]taurocholate uptake incubated for 2 mins by scintillation counting method | B | 4.4 | pIC50 | 40000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126623-126623 [PMID:31439379] |
| sirtuin 6/NAD-dependent protein deacetylase sirtuin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163182] [GtoPdb: 2712] [UniProtKB: Q8N6T7] | ||||||||
| ChEMBL | Activation of recombinant SIRT6 (unknown origin) using fluoro substrate peptide incubated for 1 hr in presence of NAD by Fluor de Lys assay based fluorometric analysis | B | 5.15 | pEC50 | 7100 | nM | EC50 | ACS Med Chem Lett (2020) 11: 2285-2289 [PMID:33214841] |
| hydroxymethylglutaryl-CoA reductase in Human [GtoPdb: 639] [UniProtKB: P04035] | ||||||||
| GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 6.56 | pKi | 256 | nM | Ki | Biochemistry (2005) 44: 11741-8 [PMID:16128575] |
| GtoPdb | - | - | 7.55 | pKi | 28 | nM | Ki | Biochem Soc Trans (2003) 31: 528-31 [PMID:12773150] |
| GtoPdb | Inhibition of HMG-CoA reductase | - | 7.55 | pIC50 | 28 | nM | IC50 | Science (2001) 292: 1160-4 [PMID:11349148] |
| hydroxymethylglutaryl-CoA reductase in Rat [GtoPdb: 639] [UniProtKB: P51639] | ||||||||
| GtoPdb | in vitro inhibition of cholesterol synthesis | - | 8.42 | pIC50 | 3.78 | nM | IC50 | Am J Cardiol (2001) 87: 28B-32B [PMID:11256847] |
| GtoPdb | in vitro inhibition of HMG-CoA reductase | - | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4228-31 [PMID:19502059] |
| GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (1993) 36: 3674-85 [PMID:8246237] |
| GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (1991) 34: 2962-83 [PMID:1656041] |
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]
