Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T53748 | ||||
Target Name | Plasmodium Enoyl-ACP reductase (Malaria fabI) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Triclosan | Drug Info | IC50 = 100 nM | [7] | |
(-)-CATECHINGALLATE | Drug Info | Ki = 40 nM | [2] | ||
2-(2,4-dichlorophenoxy)-5-(2-methylbutyl)phenol | Drug Info | IC50 = 290 nM | [6] | ||
2-(2,4-dichlorophenoxy)-5-(3-phenylpropyl)phenol | Drug Info | IC50 = 440 nM | [4] | ||
2-(2,4-dichlorophenoxy)-5-ethylphenol | Drug Info | IC50 = 110 nM | [4] | ||
2-(2,4-dichlorophenoxy)-5-isobutylphenol | Drug Info | IC50 = 180 nM | [6] | ||
2-(2,4-dichlorophenoxy)-5-isopentylphenol | Drug Info | IC50 = 120 nM | [6] | ||
2-(2,4-dichlorophenoxy)-5-methylphenol | Drug Info | IC50 = 200 nM | [4] | ||
2-(2,4-dichlorophenoxy)-5-phenethylphenol | Drug Info | IC50 = 76 nM | [6] | ||
2-(2,4-dichlorophenoxy)-5-propylphenol | Drug Info | IC50 = 210 nM | [4] | ||
2-(4-amino-2-chlorophenoxy)-5-chlorophenol | Drug Info | IC50 = 360 nM | [1] | ||
2-(4-chloro-2-hydroxyphenoxy)benzenaminium | Drug Info | IC50 = 7000 nM | [6] | ||
3,7,3',4'-TETRAHYDROXYFLAVONE | Drug Info | IC50 = 1000 nM | [2] | ||
3,7-dihydroxy-flavone | Drug Info | IC50 = 10000 nM | [2] | ||
3-chloro-4-(4-chloro-2-hydroxyphenoxy)benzamide | Drug Info | IC50 = 120 nM | [1] | ||
4-(2,4-dichloro-phenoxy)-2'-methyl-biphenyl-3-ol | Drug Info | IC50 = 440 nM | [4] | ||
4-(2,4-dichloro-phenoxy)-4'-fluoro-biphenyl-3-ol | Drug Info | IC50 = 38 nM | [4] | ||
4-(2,4-dichloro-phenoxy)-biphenyl-3-ol | Drug Info | IC50 = 140 nM | [4] | ||
4-(2,4-dichlorophenoxy)-3'-methylbiphenyl-3-ol | Drug Info | IC50 = 230 nM | [6] | ||
4-(2,4-dichlorophenoxy)-3-hydroxybenzonitrile | Drug Info | IC50 = 49 nM | [4] | ||
4-(2,4-dichlorophenoxy)-4'-methylbiphenyl-3-ol | Drug Info | IC50 = 190 nM | [6] | ||
5-benzyl-2-(2,4-dichlorophenoxy)phenol | Drug Info | IC50 = 71 nM | [6] | ||
5-butyl-2-(2,4-dichlorophenoxy)phenol | Drug Info | IC50 = 480 nM | [6] | ||
5-chloro-2-(2-chloro-4-hydroxyphenoxy)phenol | Drug Info | IC50 = 220 nM | [1] | ||
5-chloro-2-(2-chloro-4-nitrophenoxy)phenol | Drug Info | IC50 = 180 nM | [1] | ||
BUTEIN | Drug Info | Ki = 14 nM | [3] | ||
Epigallocatechin gallate | Drug Info | Ki = 8 nM | [3] | ||
GALLOCATECHIN GALLATE | Drug Info | IC50 = 500 nM | [2] | ||
ISORHAMNETIN | Drug Info | IC50 = 5000 nM | [2] | ||
MORIN | Drug Info | IC50 = 5000 nM | [2] | ||
OROIDIN | Drug Info | Ki = 800 nM | [5] | ||
References | |||||
REF 1 | Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. ... Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. | ||||
REF 2 | Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem. 2006 Jun 1;49(11):3345-53. | ||||
REF 3 | Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR). J Med Chem. 2007 Feb 22;50(4):765-75. | ||||
REF 4 | X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalar... J Biol Chem. 2007 Aug 31;282(35):25436-44. | ||||
REF 5 | Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tubercul... Bioorg Med Chem. 2007 Nov 1;15(21):6834-45. | ||||
REF 6 | Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier pr... Eur J Med Chem. 2009 Jul;44(7):3009-19. | ||||
REF 7 | Development of modern InhA inhibitors to combat drug resistant strains of Mycobacterium tuberculosis. Curr Top Med Chem. 2007;7(5):489-98. | ||||
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