Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T53585 | ||||
Target Name | 3-hydroxy-3-methylglutaryl-coenzyme A reductase | ||||
Target Type | Successful |
||||
Drug Potency against Target | Fluvastatin | Drug Info | IC50 = 27.6 nM | [552514] | |
6-hydroxy-7,9-octadecadiynoic acid | Drug Info | IC50 = 7000 nM | |||
Simvistatin | Drug Info | IC50 = 11 nM | [552347] | ||
PITAVASTATIN CALCIUM | Drug Info | IC50 = 10550 nM | [529042] | ||
PF-3052334 | Drug Info | IC50 = 1.9 nM | [529210] | ||
Simvastatin | Drug Info | IC50 = 11.2 nM | [552514] | ||
(Z)-5-octadecen-7,9-diynoic acid | Drug Info | IC50 = 1500 nM | |||
GLPTGG | Drug Info | IC50 = 19400 nM | [529130] | ||
GFPTGG | Drug Info | IC50 = 16900 nM | [529130] | ||
9-octadecynoic acid | Drug Info | IC50 = 5000 nM | |||
GFPEGG | Drug Info | IC50 = 1700 nM | [529130] | ||
(Z)-7-octedecan-9-ynoic acid | Drug Info | IC50 = 3000 nM | |||
Rosuvastatin | Drug Info | IC50 = 5.4 nM | [552514] | ||
Pravastatin | Drug Info | IC50 = 44.1 nM | [552514] | ||
Atorvastatin | Drug Info | IC50 = 8.2 nM | [552514] | ||
GFPDGG | Drug Info | IC50 = 1500 nM | [529130] | ||
3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid | Drug Info | IC50 = 5000 nM | |||
Statins | Drug Info | IC50 = 10 nM | [552514] | ||
7,9-octadecadiynoic acid | Drug Info | IC50 = 5000 nM | |||
Lovastatin | Drug Info | IC50 = 24 nM | [553225] | ||
Meglutol | Drug Info | IC50 = 4000 nM | [527409] | ||
(E)-5-octadecen-7,9-diynoic acid | Drug Info | IC50 = 500 nM | |||
F(4-Fluoro)VAE | Drug Info | IC50 = 3800 nM | [529130] | ||
7,9-tetradecadiynoic acid | Drug Info | IC50 = 3000 nM | |||
(E)-octadecan-9-ynoic acid | Drug Info | IC50 = 2000 nM | |||
Action against Disease Model | Pravastatin | IC50 on sterol synthesis in h uMan myoblasts in culture: 110nM | [553240] | Drug Info | |
Simvastatin | IC50 on sterol synthesis in h uMan myoblasts in culture: 4.0nM | [553240] | Drug Info | ||
Lovastatin | IC50 on sterol synthesis in h uMan myoblasts in culture: 19nM | [553240] | Drug Info | ||
References | |||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 553240 | Action of lovastatin, simvastatin, and pravastatin on sterol synthesis and their antiproliferative effect in cultured myoblasts from human striated muscle. Biochem Pharmacol. 1996 Nov 8;52(9):1387-92. | ||||
Ref 552347 | Comparative pharmacology of rosuvastatin. Atheroscler Suppl. 2003 Mar;4(1):9-14. | ||||
Ref 529042 | Bioorg Med Chem. 2007 Dec 15;15(24):7809-29. Epub 2007 Aug 28.Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents. | ||||
Ref 529210 | J Med Chem. 2008 Jan 10;51(1):31-45. Epub 2007 Dec 12.Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia. | ||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 529130 | Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. | ||||
Ref 529130 | Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. | ||||
Ref 553240 | Action of lovastatin, simvastatin, and pravastatin on sterol synthesis and their antiproliferative effect in cultured myoblasts from human striated muscle. Biochem Pharmacol. 1996 Nov 8;52(9):1387-92. | ||||
Ref 529130 | Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. | ||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 529130 | Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. | ||||
Ref 552514 | New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42. | ||||
Ref 553225 | Pravastatin inhibited the cholesterol synthesis in human hepatoma cell line Hep G2 less than simvastatin and lovastatin, which is reflected in the upregulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase and squalene synthase. Biochem Pharmacol. 1993 Jun 9;45(11):2203-8. | ||||
Ref 527409 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):989-94.Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase. | ||||
Ref 529130 | Bioorg Med Chem. 2008 Feb 1;16(3):1309-18. Epub 2007 Oct 23.Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. | ||||
Ref 553240 | Action of lovastatin, simvastatin, and pravastatin on sterol synthesis and their antiproliferative effect in cultured myoblasts from human striated muscle. Biochem Pharmacol. 1996 Nov 8;52(9):1387-92. |
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