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ChEMBL ligand: CHEMBL54440 (Mevastatin, 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 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]