Target Validation Information
TTD ID T72444
Target Name Bacterial Beta-ketoacyl-ACP synthase III (Bact fabH)
Type of Target
Literature-reported
Drug Potency against Target 2-(3-Phenoxy-benzoylamino)-benzoic acid Drug Info IC50 = 2700 nM [1]
2-(4-Bromo-3-phenoxy-benzoylamino)-benzoic acid Drug Info IC50 = 1100 nM [1]
2-(4-chlorophenylsulfonyl)naphthalene-1,4-diol Drug Info IC50 = 3.61 nM [2]
2-(4-Fluoro-3-phenoxy-benzoylamino)-benzoic acid Drug Info IC50 = 3800 nM [1]
2-(4-propylphenylsulfonyl)naphthalene-1,4-diol Drug Info IC50 = 3.09 nM [2]
2-(methylsulfonyl)naphthalene-1,4-diol Drug Info IC50 = 3.53 nM [2]
2-(naphthalen-2-ylsulfonyl)naphthalene-1,4-diol Drug Info IC50 = 1.49 nM [2]
2-(p-tolylthio)naphthalene-1,4-dione Drug Info IC50 = 112 nM [2]
2-(phenylsulfonyl)naphthalene-1,4-diol Drug Info IC50 = 2.84 nM [2]
2-Fluoro-6-(3-phenoxy-benzoylamino)-benzoic acid Drug Info IC50 = 6000 nM [1]
2-Hydroxy-6-(3-phenoxy-benzoylamino)-benzoic acid Drug Info IC50 = 410 nM [1]
2-tosylanthracene-1,4-diol Drug Info IC50 = 8.47 nM [2]
2-tosylbenzene-1,4-diol Drug Info IC50 = 34.4 nM [2]
2-tosylnaphthalene Drug Info IC50 = 138.1 nM [2]
2-Tosylnaphthalene-1,4-diol Drug Info IC50 = 0.61 nM [2]
2-tosylnaphthalene-1,4-dione Drug Info IC50 = 1.99 nM [2]
2-[3-(Pyridin-4-yloxy)-benzoylamino]-benzoic acid Drug Info IC50 = 10000 nM [1]
References
REF 1 Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial age... J Med Chem. 2005 Mar 10;48(5):1596-609.
REF 2 Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6402-5.

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