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ChEMBL ligand: CHEMBL1144 (C10AA03, Pravachol, Pravastatin, Pravator) |
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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] | ||||||||
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 6.99 | pKi | 103 | nM | Ki | Biochemistry (2005) 44: 11741-8 [PMID:16128575] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 5.86 | pIC50 | 1370 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1285-8 [PMID:11392538] |
ChEMBL | Inhibition of human HMGR catalytic domain using 800 uM HMG-CoA as substrate measured every 20 secs for 10 mins | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2016) 79: 1500-1507 [PMID:27228159] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1992) 35: 2095-103 [PMID:1597859] |
ChEMBL | Tested in vitro for the inhibition of HMG-CoA reductase from partially purified microsomal preparations. | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1992) 35: 2095-2103 [PMID:1597859] |
ChEMBL | DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) | B | 8.25 | pIC50 | 5.59 | nM | IC50 | DrugMatrix in vitro pharmacology data |
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639] | ||||||||
ChEMBL | Inhibition of HMGR in rat hepatic microsomes assessed as conversion of [14C]HMG-CoA to [14C]mevalonic acid | B | 7.5 | pIC50 | 31.6 | nM | IC50 | J Med Chem (2008) 51: 2722-2733 [PMID:18412317] |
ChEMBL | Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 31-45 [PMID:18072721] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 31-45 [PMID:18072721] |
GtoPdb | in vitro inhibition of cholesterol synthesis | - | 8.16 | pIC50 | 6.93 | nM | IC50 | Am J Cardiol (2001) 87: 28B-32B [PMID:11256847] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1993) 36: 3658-62 [PMID:8246234] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.38 | pEC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1285-8 [PMID:11392538] |
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] | ||||||||
ChEMBL | Inhibition of rat Oat1 expressed in pig LLC-PK11 cells | B | 4.28 | pKi | 52000 | nM | Ki | Bioorg Med Chem (2011) 19: 3320-3340 [PMID:21571536] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells | F | 4.86 | pIC50 | 13700 | nM | IC50 | J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells | F | 4.81 | pIC50 | 15600 | nM | IC50 | J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359] |
squalene monooxygenase/Squalene monooxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3592] [GtoPdb: 2433] [UniProtKB: Q14534] | ||||||||
ChEMBL | In vitro inhibitory activity against pig liver microsomal squalene epoxidase | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 3207-3216 [PMID:7650673] |
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]