Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00112
Target NameArachidonate 5-lipoxygenase    
Type of TargetSuccessful target    
Drug Potency against TargetZileutonIC50 = 500~1000 nM[1]
LicofeloneIC50 = 160 nM[2]
3-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acrylamideIC50 = 100 nM[3]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-acrylamideIC50 = 100 nM[4]
N-Hydroxy-N-methyl-3-phenanthren-3-yl-acrylamideIC50 = 100 nM[3]
1,5-Dihydroxy-10H-anthracen-9-oneIC50 = 10000 nM[5]
BAICALEINIC50 = 10000 nM[6]
1,8,9-Trimethoxy-9,10-dihydro-anthraceneIC50 = 10000 nM[5]
TZI-41127IC50 = 110 nM[7]
2-(1H-Indol-3-ylmethyl)-1,2-dihydro-indazol-3-oneIC50 = 1100 nM[6]
N-(4-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amineIC50 = 120 nM[8]
N-Hydroxy-N-methyl-3-phenanthren-9-yl-acrylamideIC50 = 120 nM[3]
5-Methyl-2-p-tolyl-thiazol-4-olIC50 = 1200 nM[9]
Phenanthrene-3-carboxylic acid hydroxyamideIC50 = 1200 nM[3]
1-Hydroxy-8-methoxy-10H-anthracen-9-oneIC50 = 12000 nM[5]
N-Hydroxy-3-phenyl-acrylamideIC50 = 12000 nM[3]
N-(4-Ethylphenyl)benzo[d]oxazol-2-amineIC50 = 1210 nM[8]
3-Biphenyl-4-yl-N-hydroxy-N-methyl-acrylamideIC50 = 130 nM[3]
N-Hydroxy-N-methyl-3-phenanthren-2-yl-acrylamideIC50 = 130 nM[3]
2-Methyl-1,2-dihydro-indazol-3-oneIC50 = 1300 nM[6]
1-Hydroxy-10H-anthracen-9-oneIC50 = 13000 nM[5]
1,3,8-Trihydroxy-6-methyl-10H-anthracen-9-oneIC50 = 14000 nM[5]
4-Bromo-N-hydroxy-benzamideIC50 = 14000 nM[3]
Naphthalene-2-carboxylic acid hydroxyamideIC50 = 14000 nM[3]
N-Hydroxy-N-methyl-benzamideIC50 = 14000 nM[3]
2-Pyridin-3-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 1500 nM[6]
N-Hydroxy-4-iodo-benzamideIC50 = 15000 nM[3]
JUGLONEIC50 = 17000 nM[5]
N-Hydroxy-4-naphthalen-1-yl-benzamideIC50 = 180 nM[3]
2-Thiazol-5-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 1800 nM[6]
N-Hydroxy-2-methyl-3-naphthalen-2-yl-acrylamideIC50 = 1800 nM[3]
10-Acetyl-1,8-dihydroxy-10H-anthracen-9-oneIC50 = 18000 nM[5]
Phenanthrene-2-carboxylic acid hydroxyamideIC50 = 1900 nM[3]
N-Hydroxy-2-naphthalen-2-yl-acetamideIC50 = 19000 nM[3]
1,2-Dihydro-indazol-3-oneIC50 = 2000 nM[6]
BW-755CIC50 = 2000 nM[10]
ANTHRONEIC50 = 2000 nM[5]
4-Hydroxy-5-methoxy-10H-anthracen-9-oneIC50 = 2000 nM[5]
N-(3-Bromophenyl)-5-methoxybenzo[d]oxazol-2-amineIC50 = 2030 nM[8]
4-(1H-indol-3-yl)-1-morpholinobutan-1-oneIC50 = 2060 nM[11]
N-Hydroxy-N-methyl-3-naphthalen-1-yl-acrylamideIC50 = 210 nM[3]
2-Pyridin-4-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 2400 nM[6]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 270 nM[6]
N-Hydroxy-N-methyl-2,3,3-triphenyl-acrylamideIC50 = 2700 nM[3]
N-Hydroxy-3-naphthalen-2-yl-N-p-tolyl-acrylamideIC50 = 280 nM[3]
N-hydroxy-N'-[1-(4-isobutylphenyl)ethyl]ureaIC50 = 2900 nM[12]
A-78773IC50 = 298 nM[13]
NAPHTHAZALINIC50 = 3000 nM[5]
1-Methyl-1,2-dihydro-indazol-3-oneIC50 = 3000 nM[6]
REV-5901IC50 = 3000 nM[6]
TEBUFELONEIC50 = 3000 nM[14]
2-Phenyl-1,2-dihydro-indazol-3-oneIC50 = 310 nM[6]
2-Pyridin-2-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 3100 nM[6]
N-Hydroxy-4-naphthalen-2-yl-benzamideIC50 = 330 nM[3]
1-Benzyl-1,2-dihydro-indazol-3-oneIC50 = 3400 nM[6]
2-Benzyl-1,2-dihydro-indazol-3-oneIC50 = 360 nM[6]
2-Biphenyl-4-yl-N-hydroxy-N-methyl-acetamideIC50 = 360 nM[3]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-propionamideIC50 = 380 nM[3]
2-Thiophen-2-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 400 nM[6]
1,2-Dihydroxy-10H-anthracen-9-oneIC50 = 4000 nM[5]
4,5-Dihydroxy-10H-anthracen-9-oneIC50 = 4000 nM[5]
PYROGALLOLIC50 = 4000 nM[5]
3,4-Dihydroxy-10H-anthracen-9-oneIC50 = 4000 nM[5]
1,8-Dichloro-10H-anthracen-9-oneIC50 = 4000 nM[5]
10-Benzoyl-1,8-dihydroxy-10H-anthracen-9-oneIC50 = 4000 nM[5]
Biphenyl-4-carboxylic acid hydroxyamideIC50 = 4100 nM[3]
2-(4-Methoxy-phenyl)-5-phenyl-thiazol-4-olIC50 = 450 nM[9]
5-Chloro-N-phenylbenzo[d]oxazol-2-amineIC50 = 4500 nM[8]
5-Methyl-N-phenylbenzo[d]oxazol-2-amineIC50 = 4600 nM[8]
IbuproxamIC50 = 4840 nM[4]
4-Butoxy-N-hydroxy-N-methyl-benzamideIC50 = 490 nM[3]
Acetic acid 5-butyl-2-phenyl-thiazol-4-yl esterIC50 = 500 nM[9]
Hexanoic acid 2,5-diphenyl-thiazol-4-yl esterIC50 = 500 nM[9]
N-Hydroxy-3-naphthalen-2-yl-N-phenyl-acrylamideIC50 = 52 nM[3]
2-(4-Butoxy-phenoxy)-N-hydroxy-acetamideIC50 = 5300 nM[3]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-oneIC50 = 540 nM[6]
2-Phenethyl-1,2-dihydro-indazol-3-oneIC50 = 550 nM[6]
N-(2-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amineIC50 = 5660 nM[8]
N-Hydroxy-N-methyl-2-naphthalen-2-yl-propionamideIC50 = 590 nM[3]
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]ureaIC50 = 600 nM[12]
1,8-Dihydroxy-2-propionyl-10H-anthracen-9-oneIC50 = 6000 nM[5]
Biphenyl-3-carboxylic acid hydroxyamideIC50 = 6000 nM[3]
N-Hydroxy-4-isobutyl-benzamideIC50 = 6000 nM[3]
NAFAZATROMIC50 = 6000 nM[10]
2-Naphthalen-1-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 610 nM[6]
Acetic acid 2-phenyl-5-propyl-thiazol-4-yl esterIC50 = 660 nM[9]
3-Biphenyl-3-yl-N-hydroxy-N-methyl-acrylamideIC50 = 70 nM[3]
2-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acetamideIC50 = 720 nM[3]
4-Pentadeca-1,3,6-trienylsulfanyl-butyric acidIC50 = 7200 nM[10]
2-(4-Phenyl-butyl)-1,2-dihydro-indazol-3-oneIC50 = 780 nM[6]
5-Methoxy-N-phenylbenzo[d]oxazol-2-amineIC50 = 7880 nM[8]
3-Benzoyl-N-hydroxy-benzamideIC50 = 7900 nM[3]
4,5-Dimethoxy-10H-anthracen-9-oneIC50 = 8000 nM[5]
2-(4-Butoxy-phenoxy)-N-hydroxy-propionamideIC50 = 8060 nM[3]
2'-Nitro-biphenyl-4-carboxylic acid hydroxyamideIC50 = 8300 nM[3]
2-(4-Butoxy-phenoxy)-N-hydroxy-N-methyl-acetamideIC50 = 890 nM[3]
N-Phenylbenzo[d]oxazol-2-amineIC50 = 8910 nM[8]
5-Chloro-N-(4-ethylphenyl)benzo[d]oxazol-2-amineIC50 = 950 nM[8]
N-Hydroxy-3-naphthalen-2-yl-acrylamideIC50 = 950 nM[3]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-oneIC50 = 970 nM[6]
N-Hydroxy-3-naphthalen-2-yl-propionamideIC50 = 9700 nM[3]
Anthracene-2-carboxylic acid hydroxyamideIC50 = 980 nM[3]
Ref 1Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. To Reference
Ref 2J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference
Ref 3J Med Chem. 1990 Mar;33(3):992-8.Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships. To Reference
Ref 4J Med Chem. 1987 Nov;30(11):2121-6.In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase. To Reference
Ref 5J Med Chem. 1997 Nov 7;40(23):3773-80.Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity. To Reference
Ref 6J Med Chem. 1991 Mar;34(3):1028-36.Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity. To Reference
Ref 7Bioorg. Med. Chem. Lett. 4(20):2383-2388 (1994) To Reference
Ref 8Bioorg Med Chem. 2010 Nov 1;18(21):7580-5. Epub 2010 Oct 1.Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors. To Reference
Ref 9J Med Chem. 1991 Jul;34(7):2158-65.4-hydroxythiazole inhibitors of 5-lipoxygenase. To Reference
Ref 10J Med Chem. 1990 Apr;33(4):1163-70.Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes. To Reference
Ref 11Bioorg Med Chem Lett. 2007 May 1;17(9):2414-20. Epub 2007 Feb 17.Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling. To Reference
Ref 12J Med Chem. 1997 Feb 28;40(5):819-24.Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. To Reference
Ref 13J Med Chem. 1998 May 21;41(11):1970-9.(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist. To Reference
Ref 14J Med Chem. 1998 Mar 26;41(7):1124-37.New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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