Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00235
Target NameEnoyl-ACP reductase    
Type of TargetSuccessful target    
Drug Potency against TargetTriclosanIC50 = 100 nM[1]
TriclosanIC50 = 300 nM[2]
FISETINIC50 = 1000 nM[3]
2-(2-((benzylamino)methyl)phenoxy)-5-chlorophenolIC50 = 10000 nM[4]
3,7-dihydroxy-flavoneIC50 = 10000 nM[3]
2-(2,4-dichlorophenoxy)-5-ethylphenolIC50 = 110 nM[5]
2-(2,4-dichlorophenoxy)-5-isopentylphenolIC50 = 120 nM[6]
3-chloro-4-(4-chloro-2-hydroxyphenoxy)benzamideIC50 = 120 nM[7]
4-(2,4-dichloro-phenoxy)-biphenyl-3-olIC50 = 140 nM[5]
2-(2,4-dichlorophenoxy)-5-isobutylphenolIC50 = 180 nM[6]
5-chloro-2-(2-chloro-4-nitrophenoxy)phenolIC50 = 180 nM[7]
4-(2,4-dichlorophenoxy)-4'-methylbiphenyl-3-olIC50 = 190 nM[6]
2-(2,4-dichlorophenoxy)-5-methylphenolIC50 = 200 nM[5]
2-(2,4-dichlorophenoxy)-5-propylphenolIC50 = 210 nM[5]
5-chloro-2-(2-chloro-4-hydroxyphenoxy)phenolIC50 = 220 nM[7]
4-(2,4-dichlorophenoxy)-3'-methylbiphenyl-3-olIC50 = 230 nM[6]
2-(2-((benzylamino)methyl)phenoxy)-5-chlorophenolIC50 = 2500 nM[6]
2-(2,4-dichlorophenoxy)-5-(2-methylbutyl)phenolIC50 = 290 nM[6]
2-(4-amino-2-chlorophenoxy)-5-chlorophenolIC50 = 360 nM[7]
4-(2,4-dichloro-phenoxy)-4'-fluoro-biphenyl-3-olIC50 = 38 nM[5]
2-(2,4-dichlorophenoxy)-5-(3-phenylpropyl)phenolIC50 = 440 nM[5]
4-(2,4-dichloro-phenoxy)-2'-methyl-biphenyl-3-olIC50 = 440 nM[5]
5-butyl-2-(2,4-dichlorophenoxy)phenolIC50 = 480 nM[6]
4-(2,4-dichlorophenoxy)-3-hydroxybenzonitrileIC50 = 49 nM[5]
GALLOCATECHIN GALLATEIC50 = 500 nM[3]
ISORHAMNETINIC50 = 5000 nM[3]
MORINIC50 = 5000 nM[3]
2-(4-chloro-2-hydroxyphenoxy)benzenaminiumIC50 = 7000 nM[6]
5-benzyl-2-(2,4-dichlorophenoxy)phenolIC50 = 71 nM[6]
2-(2,4-dichlorophenoxy)-5-phenethylphenolIC50 = 76 nM[6]
BUTEINKi = 14 nM[8]
EPICATECHIN GALLATEKi = 16 nM[8]
EPIGALLOCATECHINKi = 17.56 nM[8]
(-)-CATECHINGALLATEKi = 40 nM[3]
EPIGALOCATECHIN GALLATEKi = 8 nM[8]
OROIDINKi = 800 nM[9]
Ref 1Curr Top Med Chem. 2007;7(5):489-98.Development of modern InhA inhibitors to combat drug resistant strains of Mycobacterium tuberculosis. To Reference
Ref 2J Biol Chem. 2002 Apr 12;277(15):13106-14. Epub 2002 Jan 15.Structural elucidation of the specificity of the antibacterial agent triclosan for malarial enoyl acyl carrier protein reductase. To Reference
Ref 3J 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. To Reference
Ref 4Bioorg Med Chem Lett. 2006 Apr 15;16(8):2163-9. Epub 2006 Feb 8.Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 2'-substituted triclosan derivatives. To Reference
Ref 5J 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. To Reference
Ref 6Eur 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. To Reference
Ref 7Bioorg 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. To Reference
Ref 8J 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). To Reference
Ref 9Bioorg 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. To Reference



 

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