Target Validation Information
Target ID T26623
Target Name Aldose reductase
Target Type
Successful
Drug Potency against Target EPALRESTATE Drug Info IC50 = 70 nM [529340]
2-Benzyl-7-hydroxy-chromen-4-one Drug Info IC50 = 6610 nM [525506]
TINGENIN B Drug Info IC50 = 7000 nM [526834]
Apigenin-7-O-beta-D-glucuronide Drug Info IC50 = 1280 nM [529340]
QUERCITRIN Drug Info IC50 = 160 nM [529340]
Apigenin-7-O-beta-D-glucuronide methyl ester Drug Info IC50 = 9020 nM [529340]
7-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one Drug Info IC50 = 2500 nM [525506]
6-(Naphthalene-2-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 360 nM [527771]
6,7-Dihydroxy-2-phenyl-chromen-4-one Drug Info IC50 = 3980 nM [525506]
7-Hydroxy-2-(4-methoxy-benzyl)-chromen-4-one Drug Info IC50 = 7010 nM [525506]
DIADZEIN Drug Info IC50 = 13630 nM [525506]
6-(3-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 240 nM [527771]
6-(4-Bromo-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 350 nM [527771]
6-(Biphenyl-2-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 2200 nM [527771]
2-(3,4-Dihydroxy-benzyl)-7-hydroxy-chromen-4-one Drug Info IC50 = 3140 nM [525506]
6-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one Drug Info IC50 = 13120 nM [525506]
6-(Naphthalene-1-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 150 nM [527771]
6-(Benzofuran-2-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 150 nM [527771]
6-Benzenesulfonyl-2H-pyridazin-3-one Drug Info IC50 = 600 nM [527771]
6-(2-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 540 nM [527771]
(6-Methoxy-2-oxo-2H-quinolin-1-yl)-acetic acid Drug Info IC50 = 910 nM [533420]
6-(2-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 170 nM [527771]
6-(4-Methoxy-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 2000 nM [527771]
6-Phenylmethanesulfonyl-2H-pyridazin-3-one Drug Info IC50 = 600 nM [527771]
6-(Toluene-4-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 1900 nM [527771]
6-(1H-Indole-2-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 590 nM [527771]
2-Benzhydryl-7-hydroxy-chromen-4-one Drug Info IC50 = 10890 nM [525506]
6-(4-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 380 nM [527771]
NSC-94258 Drug Info IC50 = 14650 nM [525506]
PALBINONE Drug Info IC50 = 11400 nM [530306]
LIDORESTAT Drug Info IC50 = 5 nM [527533]
6-(2-Bromo-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 210 nM [527771]
7-Hydroxy-6-nitro-2-phenyl-chromen-4-one Drug Info IC50 = 3870 nM [525506]
6-(4-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 474 nM [527771]
6-(Benzothiazole-2-sulfonyl)-2H-pyridazin-3-one Drug Info IC50 = 450 nM [527771]
7-Hydroxy-4-phenylcoumarin Drug Info IC50 = 2400 nM [531138]
4-(3-Benzoyl-1H-pyrrol-1-yl)butanoic acid Drug Info IC50 = 6040 nM [530758]
3-(3-Benzoyl-1H-pyrrol-1-yl)propanoic acid Drug Info IC50 = 9700 nM [530758]
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid Drug Info IC50 = 1970 nM [530758]
Quercetin 3-O-neohesperidoside Drug Info IC50 = 18000 nM [526409]
Epalrestat Drug Info IC50 = 280 nM [552858]
Isorhamnetin 3-O-rhamnoside Drug Info IC50 = 19000 nM [526409]
2-(4-aminophenylsulfonamido)acetic acid Drug Info IC50 = 16000 nM [529308]
O5-Acetyl-O7-nitrooxyethyl chrysin Drug Info IC50 = 860 nM [530856]
CHRYSIN Drug Info IC50 = 7790 nM [530856]
O7-Nitrooxyethyl chrysin Drug Info IC50 = 490 nM [530856]
TRIPTOCALLINE A Drug Info IC50 = 14000 nM [526834]
MANGIFERIN Drug Info IC50 = 3200 nM [526834]
TINGENONE Drug Info IC50 = 13000 nM [526834]
3,5-dichlorosalicylic acid Drug Info IC50 = 11300 nM [529899]
ZOPOLRESTAT Drug Info IC50 = 60 nM [530801]
(8-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid Drug Info IC50 = 3300 nM [533420]
(4-Methyl-2-oxo-2H-quinolin-1-yl)-acetic acid Drug Info IC50 = 6000 nM [533420]
(6-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid Drug Info IC50 = 2400 nM [533420]
MINALRESTAT Drug Info IC50 = 40 nM [529899]
ASTRAGALIN Drug Info IC50 = 5090 nM [529340]
KAEMPFEROL Drug Info IC50 = 1330 nM [529340]
Sulindac Drug Info IC50 = 100 nM [553168]
APIGENIN Drug Info IC50 = 6670 nM [529340]
IMIRESTAT Drug Info IC50 = 5 nM [530231]
Isorhamnetin 3,7-disulfate Drug Info IC50 = 1800 nM [534149]
CONTIGOSIDE B Drug Info IC50 = 16000 nM [534149]
Tamarixetin 3-glucoside-7-sulfate Drug Info IC50 = 5000 nM [534149]
2,3-dihydroxypropanal Drug Info IC50 = 10 nM [529225]
2-(3,4-Dihydroxy-phenyl)-7-hydroxy-chromen-4-one Drug Info IC50 = 6520 nM [525506]
References
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 526834J Nat Prod. 2003 Sep;66(9):1191-6.Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 533420J Med Chem. 1986 Oct;29(10):2024-8.Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 530306J Nat Prod. 2009 Aug;72(8):1465-70.Inhibitors of aldose reductase and formation of advanced glycation end-products in moutan cortex (Paeonia suffruticosa).
Ref 527533J Med Chem. 2005 May 5;48(9):3141-52.Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 527771J Med Chem. 2005 Oct 6;48(20):6326-39.A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Ref 531138Bioorg Med Chem Lett. 2010 Oct 1;20(19):5630-3. Epub 2010 Aug 12.6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2.
Ref 530758Bioorg Med Chem. 2010 Mar 15;18(6):2107-14. Epub 2010 Feb 11.Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case ofbioisosterism between a carboxylic acid moiety and that of a tetrazole.
Ref 530758Bioorg Med Chem. 2010 Mar 15;18(6):2107-14. Epub 2010 Feb 11.Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case ofbioisosterism between a carboxylic acid moiety and that of a tetrazole.
Ref 530758Bioorg Med Chem. 2010 Mar 15;18(6):2107-14. Epub 2010 Feb 11.Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case ofbioisosterism between a carboxylic acid moiety and that of a tetrazole.
Ref 526409J Nat Prod. 2002 Aug;65(8):1151-5.New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Prunus mume.
Ref 552858Inhibitory activities of prenylated flavonoids from Sophora flavescens against aldose reductase and generation of advanced glycation endproducts. J Pharm Pharmacol. 2008 Sep;60(9):1227-36. doi: 10.1211/jpp.60.9.0016.
Ref 526409J Nat Prod. 2002 Aug;65(8):1151-5.New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Prunus mume.
Ref 529308Bioorg Med Chem. 2008 Apr 1;16(7):3926-32. Epub 2008 Jan 30.Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
Ref 530856Bioorg Med Chem. 2010 May 1;18(9):3020-5. Epub 2010 Mar 27.Synthesis, characterization and vasculoprotective effects of nitric oxide-donating derivatives of chrysin.
Ref 530856Bioorg Med Chem. 2010 May 1;18(9):3020-5. Epub 2010 Mar 27.Synthesis, characterization and vasculoprotective effects of nitric oxide-donating derivatives of chrysin.
Ref 530856Bioorg Med Chem. 2010 May 1;18(9):3020-5. Epub 2010 Mar 27.Synthesis, characterization and vasculoprotective effects of nitric oxide-donating derivatives of chrysin.
Ref 526834J Nat Prod. 2003 Sep;66(9):1191-6.Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
Ref 526834J Nat Prod. 2003 Sep;66(9):1191-6.Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
Ref 526834J Nat Prod. 2003 Sep;66(9):1191-6.Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
Ref 529899Bioorg Med Chem. 2009 Feb 1;17(3):1244-50. Epub 2008 Dec 24.Correlation of binding constants and molecular modelling of inhibitors in the active sites of aldose reductase and aldehyde reductase.
Ref 530801Bioorg Med Chem. 2010 Apr 1;18(7):2485-90. Epub 2010 Mar 1.Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
Ref 533420J Med Chem. 1986 Oct;29(10):2024-8.Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
Ref 533420J Med Chem. 1986 Oct;29(10):2024-8.Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
Ref 533420J Med Chem. 1986 Oct;29(10):2024-8.Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
Ref 529899Bioorg Med Chem. 2009 Feb 1;17(3):1244-50. Epub 2008 Dec 24.Correlation of binding constants and molecular modelling of inhibitors in the active sites of aldose reductase and aldehyde reductase.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 553168Inhibition of lens and cataract aldose reductase by protein-bound anti-rheumatic drugs: salicylate, indomethacin, oxyphenbutazone, sulindac. Exp Eye Res. 1982 Jul;35(1):21-7.
Ref 529340J Nat Prod. 2008 Apr;71(4):713-5. Epub 2008 Feb 26.Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
Ref 530231J Med Chem. 1991 Nov;34(11):3229-34.Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
Ref 534149J Nat Prod. 1996 Apr;59(4):443-5.Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.
Ref 534149J Nat Prod. 1996 Apr;59(4):443-5.Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.
Ref 534149J Nat Prod. 1996 Apr;59(4):443-5.Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.
Ref 529225Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20764-9. Epub 2007 Dec 17.Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10.
Ref 525506J Med Chem. 1999 Jun 3;42(11):1881-93.1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.

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