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

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ChEMBL ligand: CHEMBL54440 (Mevastatin, 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 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]