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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