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

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ChEMBL ligand: CHEMBL1078 (Fluvastatin)
  • 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
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 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]