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 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 553240Action 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 552347Comparative pharmacology of rosuvastatin. Atheroscler Suppl. 2003 Mar;4(1):9-14.
Ref 529042Bioorg 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 529210J 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 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 529130Bioorg 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 529130Bioorg 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 553240Action 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 529130Bioorg 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 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 529130Bioorg 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 552514New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
Ref 553225Pravastatin 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 527409Bioorg 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 529130Bioorg 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 553240Action 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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