Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T53748 | ||||
Target Name | Enoyl-ACP reductase | ||||
Target Type | Successful |
||||
Drug Potency against Target | 2-(2,4-dichlorophenoxy)-5-(3-phenylpropyl)phenol | Drug Info | IC50 = 440 nM | [528892] | |
4-(2,4-dichloro-phenoxy)-biphenyl-3-ol | Drug Info | IC50 = 140 nM | [528892] | ||
BUTEIN | Drug Info | Ki = 14 nM | [528645] | ||
4-(2,4-dichlorophenoxy)-4'-methylbiphenyl-3-ol | Drug Info | IC50 = 190 nM | [529962] | ||
2-(2,4-dichlorophenoxy)-5-methylphenol | Drug Info | IC50 = 200 nM | [528892] | ||
2-(2,4-dichlorophenoxy)-5-(2-methylbutyl)phenol | Drug Info | IC50 = 290 nM | [529962] | ||
5-butyl-2-(2,4-dichlorophenoxy)phenol | Drug Info | IC50 = 480 nM | [529962] | ||
MORIN | Drug Info | IC50 = 5000 nM | [528213] | ||
FISETIN | Drug Info | IC50 = 1000 nM | [528213] | ||
OROIDIN | Drug Info | Ki = 800 nM | [529012] | ||
5-chloro-2-(2-chloro-4-hydroxyphenoxy)phenol | Drug Info | IC50 = 220 nM | [527778] | ||
3,7-dihydroxy-flavone | Drug Info | IC50 = 10000 nM | [528213] | ||
GALLOCATECHIN GALLATE | Drug Info | IC50 = 500 nM | [528213] | ||
ISORHAMNETIN | Drug Info | IC50 = 5000 nM | [528213] | ||
5-chloro-2-(2-chloro-4-nitrophenoxy)phenol | Drug Info | IC50 = 180 nM | [527778] | ||
(-)-CATECHINGALLATE | Drug Info | Ki = 40 nM | [528213] | ||
EPIGALOCATECHIN GALLATE | Drug Info | Ki = 8 nM | [528645] | ||
2-(2,4-dichlorophenoxy)-5-isobutylphenol | Drug Info | IC50 = 180 nM | [529962] | ||
2-(2,4-dichlorophenoxy)-5-ethylphenol | Drug Info | IC50 = 110 nM | [528892] | ||
4-(2,4-dichloro-phenoxy)-4'-fluoro-biphenyl-3-ol | Drug Info | IC50 = 38 nM | [528892] | ||
2-(2,4-dichlorophenoxy)-5-propylphenol | Drug Info | IC50 = 210 nM | [528892] | ||
2-(2,4-dichlorophenoxy)-5-isopentylphenol | Drug Info | IC50 = 120 nM | [529962] | ||
4-(2,4-dichlorophenoxy)-3'-methylbiphenyl-3-ol | Drug Info | IC50 = 230 nM | [529962] | ||
2-(4-amino-2-chlorophenoxy)-5-chlorophenol | Drug Info | IC50 = 360 nM | [527778] | ||
4-(2,4-dichloro-phenoxy)-2'-methyl-biphenyl-3-ol | Drug Info | IC50 = 440 nM | [528892] | ||
5-benzyl-2-(2,4-dichlorophenoxy)phenol | Drug Info | IC50 = 71 nM | [529962] | ||
2-(2,4-dichlorophenoxy)-5-phenethylphenol | Drug Info | IC50 = 76 nM | [529962] | ||
4-(2,4-dichlorophenoxy)-3-hydroxybenzonitrile | Drug Info | IC50 = 49 nM | [528892] | ||
2-(4-chloro-2-hydroxyphenoxy)benzenaminium | Drug Info | IC50 = 7000 nM | [529962] | ||
3-chloro-4-(4-chloro-2-hydroxyphenoxy)benzamide | Drug Info | IC50 = 120 nM | [527778] | ||
Triclosan | Drug Info | IC50 = 100 nM | [552683] | ||
References | |||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 528645 | J Med Chem. 2007 Feb 22;50(4):765-75. Epub 2007 Jan 31.Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR). | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 529012 | Bioorg Med Chem. 2007 Nov 1;15(21):6834-45. Epub 2007 Aug 22.Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli. | ||||
Ref 527778 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. Epub 2005 Sep 29.Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 527778 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. Epub 2005 Sep 29.Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives. | ||||
Ref 528213 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
Ref 528645 | J Med Chem. 2007 Feb 22;50(4):765-75. Epub 2007 Jan 31.Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR). | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 527778 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. Epub 2005 Sep 29.Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 528892 | J Biol Chem. 2007 Aug 31;282(35):25436-44. Epub 2007 Jun 13.X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy. | ||||
Ref 529962 | Eur J Med Chem. 2009 Jul;44(7):3009-19. Epub 2009 Jan 19.Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase. | ||||
Ref 527778 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. Epub 2005 Sep 29.Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives. | ||||
Ref 552683 | 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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