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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