Target Validation Information
Target ID T60857
Target Name Aldo-keto reductase family 1 member C3
Target Type
Successful
Drug Potency against Target M-Phenoxybenzoic Acid For Cis-Isomer Drug Info IC50 = 680 nM [527759]
3-Bromo-5-phenylsalicylc acid Drug Info Ki = 4200 nM [530095]
2-(4-chlorobenzylidene)cyclopentylmethyl ether Drug Info Ki = 16200 nM [529980]
2-[(2,2-diphenylacetyl)amino]benzoic acid Drug Info IC50 = 11000 nM [527759]
EM1396 Drug Info IC50 = 13 nM [528576]
EM-1424 Drug Info IC50 = 9.5 nM [528576]
References
Ref 527759Bioorg Med Chem Lett. 2005 Dec 1;15(23):5170-5. Epub 2005 Sep 23.Nonsteroidal anti-inflammatory drugs and their analogues as inhibitors of aldo-keto reductase AKR1C3: new lead compounds for the development of anticancer agents.
Ref 530095J Med Chem. 2009 May 28;52(10):3259-64.Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).
Ref 529980Eur J Med Chem. 2009 Jun;44(6):2563-71. Epub 2009 Feb 5.New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.
Ref 527759Bioorg Med Chem Lett. 2005 Dec 1;15(23):5170-5. Epub 2005 Sep 23.Nonsteroidal anti-inflammatory drugs and their analogues as inhibitors of aldo-keto reductase AKR1C3: new lead compounds for the development of anticancer agents.
Ref 528576J Biol Chem. 2007 Mar 16;282(11):8368-79. Epub 2006 Dec 13.Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase.
Ref 528576J Biol Chem. 2007 Mar 16;282(11):8368-79. Epub 2006 Dec 13.Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase.

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