fluvastatin [Ligand Id: 2951] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1078 (Fluvastatin)
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • hydroxymethylglutaryl-CoA reductase in Human [GtoPdb: 639] [UniProtKB: P04035]
  • hydroxymethylglutaryl-CoA reductase in Rat [GtoPdb: 639] [UniProtKB: P51639]
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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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]