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

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