Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T07217 | ||||
Target Name | Fatty acid-binding protein 4 (FABP4) | ||||
Type of Target |
Patented-recorded |
||||
Drug Potency against Target | 1-benzyl-2,3-dimethyl-1H-indole-7-carboxylic acid | Drug Info | IC50 = 3600 nM | [3] | |
2-(2,3-bis(2-chlorobenzyloxy)phenyl)acetic acid | Drug Info | Ki = 16 nM | [2] | ||
2-(3-Methyl-indole-1-sulfonyl)-benzoic acid | Drug Info | IC50 = 8500 nM | [1] | ||
2-(4-Fluoro-indole-1-sulfonyl)-benzoic acid | Drug Info | IC50 = 10000 nM | [1] | ||
2-(4-Methyl-indole-1-sulfonyl)-benzoic acid | Drug Info | IC50 = 12000 nM | [1] | ||
2-(5-Bromo-indole-1-sulfonyl)-benzoic acid | Drug Info | IC50 = 12000 nM | [1] | ||
2-(6-Methoxy-indole-1-sulfonyl)-benzoic acid | Drug Info | IC50 = 6100 nM | [1] | ||
2-(Carbazole-9-sulfonyl)-benzoic acid | Drug Info | IC50 = 4300 nM | [1] | ||
3-Carbazol-9-yl-propionic acid | Drug Info | IC50 = 9400 nM | [1] | ||
4-Carbazol-9-yl-butyric acid | Drug Info | IC50 = 570 nM | [1] | ||
5-Carbazol-9-yl-pentanoic acid | Drug Info | IC50 = 800 nM | [1] | ||
BMS-480404 | Drug Info | Ki = 2.5 nM | [2] | ||
Hexadecanoic acid | Drug Info | IC50 = 930 nM | [1] | ||
LINOLEIC ACID | Drug Info | IC50 = 1000 nM | [4] | ||
References | |||||
REF 1 | Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8. | ||||
REF 2 | NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein. J Med Chem. 2006 Aug 10;49(16):5013-7. | ||||
REF 3 | N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1745-8. | ||||
REF 4 | Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3675-9. | ||||
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