| 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 | [1] | |
| 3-Bromo-5-phenylsalicylc acid | Drug Info | Ki = 4200 nM | [2] | ||
| 2-(4-chlorobenzylidene)cyclopentylmethyl ether | Drug Info | Ki = 16200 nM | [3] | ||
| 2-[(2,2-diphenylacetyl)amino]benzoic acid | Drug Info | IC50 = 11000 nM | [1] | ||
| EM1396 | Drug Info | IC50 = 13 nM | [4] | ||
| EM-1424 | Drug Info | IC50 = 9.5 nM | [4] | ||
| References | |||||
| REF 1 | Bioorg 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 2 | J 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 3 | Eur 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 4 | J 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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