mevastatin [Ligand Id: 3031] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL54440 (Mevastatin, Mevastatina, Mevastatine, NSC-759322)
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat [ChEMBL: CHEMBL3247] [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/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
ChEMBL DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) B 6.92 pIC50 119 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL The compound was tested in vitro for inhibitory activity against HMG-CoA reductase B 7.55 pIC50 28.4 nM IC50 J Med Chem (1992) 35: 3813-3821 [PMID:1433193]
ChEMBL Inhibitory concentration against 3-hydroxy-3-methylglutaryl-CoA reductase B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2005) 15: 1027-1032 [PMID:15686906]
ChEMBL Inhibition of HMG-CoA Reductase (unknown origin) B 7.64 pIC50 23 nM IC50 J Med Chem (2019) 62: 10005-10025 [PMID:31188592]
GtoPdb - - 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2005) 15: 1027-32 [PMID:15686906]
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639]
GtoPdb - - 8.85 pKi 1.4 nM Ki J Med Chem (1987) 30: 1858-73 [PMID:3656359]
ChEMBL Binding affinity against HMG-CoA reductase in rat liver microsomes B 8.85 pKi 1.4 nM Ki J Med Chem (1987) 30: 1858-1873 [PMID:3656359]
GtoPdb in vitro inhibition of HMG-CoA reductase - 9 pKi 1 nM Ki J Med Chem (1985) 28: 401-5 [PMID:3981532]
ChEMBL Binding affinity was determined against purified rat liver HMG-coA reductase enzyme B 9 pKi ~1 nM Ki J Med Chem (1985) 28: 401-405 [PMID:3981532]
ChEMBL Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparation B 5.94 pIC50 1150 nM IC50 Bioorg Med Chem Lett (1997) 7: 549-554
GtoPdb in vitro inhibition of HMG-CoA reductase - 5.94 pIC50 1150 nM IC50 Bioorg Med Chem Lett (1997) 7: 549-554
GtoPdb in vitro inhibition of HMG-CoA reductase - 6 pIC50 1000 nM IC50 J Med Chem (1985) 28: 597-601 [PMID:3989819]
GtoPdb - - 6 pIC50 1000 nM IC50 J Med Chem (1985) 28: 597-601 [PMID:3989819]
ChEMBL Inhibition of HMG-CoA reductase from rat liver B 6 pIC50 1000 nM IC50 J Med Chem (1985) 28: 597-601 [PMID:3989819]
GtoPdb in vitro inhibition of HMG-CoA reductase - 7 pIC50 110 nM IC50 Bioorg Med Chem Lett (1997) 7: 549-554
ChEMBL Inhibition of rat HMG-CoA reductase using 0.37 MBq DL-[3-14C]HMG-CoA B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2009) 19: 4228-4231 [PMID:19502059]
GtoPdb in vitro inhibition of HMG-CoA reductase - 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2009) 19: 4228-31 [PMID:19502059]
GtoPdb in vitro inhibition of HMG-CoA reductase - 7.52 pIC50 30 nM IC50 J Med Chem (1991) 34: 357-66 [PMID:1992137]
ChEMBL Inhibition of HMG-CoA reductase activity in partially purified rat liver B 7.52 pIC50 30 nM IC50 J Med Chem (1991) 34: 357-366 [PMID:1992137]
ChEMBL Ability to inhibit HMG-CoA reductase (HMGR) by cholesterol synthesis inhibition screen (CSI) in rats B 7.59 pIC50 26 nM IC50 J Med Chem (1990) 33: 21-31 [PMID:2296019]
ChEMBL Ability to inhibit HMG-CoA reductase (HMGR) by cholesterol synthesis inhibition screen (CSI) in rats B 7.6 pIC50 25.12 nM IC50 J Med Chem (1990) 33: 21-31 [PMID:2296019]
ChEMBL Ability to inhibit HMG-CoA reductase (HMGR) by CoA reductase inhibition screen (COR) in rats B 7.6 pIC50 25.12 nM IC50 J Med Chem (1990) 33: 21-31 [PMID:2296019]
GtoPdb in vitro inhibition of HMG-CoA reductase - 7.6 pIC50 25 nM IC50 J Med Chem (1991) 34: 367-73 [PMID:1992138]
ChEMBL Compound was evaluated for the inhibition of HMG-CoA reductase (COR) in rats. B 7.6 pIC50 25 nM IC50 J Med Chem (1991) 34: 367-373 [PMID:1992138]
ChEMBL Ability to inhibit HMG-CoA reductase (HMGR) by CoA reductase inhibition screen (COR) in rats B 7.6 pIC50 25 nM IC50 J Med Chem (1990) 33: 21-31 [PMID:2296019]
ChEMBL Inhibition of HMG-CoA reductase in rat liver microsomes B 7.89 pIC50 13 nM IC50 J Med Chem (1987) 30: 1858-1873 [PMID:3656359]
GtoPdb in vitro inhibition of HMG-CoA reductase - 8 pIC50 10 nM IC50 J Med Chem (1985) 28: 347-58 [PMID:3973903]
ChEMBL In vitro inhibitory activity against HMG CoA reductase B 8 pIC50 10 nM IC50 J Med Chem (1985) 28: 347-358 [PMID:3973903]

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]