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ChEMBL ligand: CHEMBL54440 (Mevastatin, Mevastatina, Mevastatine, NSC-759322) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]