Target Validation Information
TTD ID T00140
Target Name Arachidonate 5-lipoxygenase (5-LOX)
Type of Target
Successful
Drug Potency against Target Zileuton Drug Info IC50 = 500~1000 nM [13]
Licofelone Drug Info IC50 = 160 nM [1]
1,2-Dihydro-indazol-3-one Drug Info IC50 = 2000 nM [3]
1,2-Dihydroxy-10H-anthracen-9-one Drug Info IC50 = 4000 nM [10]
1,3,8-Trihydroxy-6-methyl-10H-anthracen-9-one Drug Info IC50 = 14000 nM [10]
1,5-Dihydroxy-10H-anthracen-9-one Drug Info IC50 = 10000 nM [10]
1,8,9-Trimethoxy-9,10-dihydro-anthracene Drug Info IC50 = 10000 nM [10]
1,8-Dichloro-10H-anthracen-9-one Drug Info IC50 = 4000 nM [10]
1,8-Dihydroxy-2-propionyl-10H-anthracen-9-one Drug Info IC50 = 6000 nM [10]
1-Benzyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 3400 nM [3]
1-Hydroxy-10H-anthracen-9-one Drug Info IC50 = 13000 nM [10]
1-Hydroxy-8-methoxy-10H-anthracen-9-one Drug Info IC50 = 12000 nM [10]
1-Methyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 3000 nM [3]
10-Acetyl-1,8-dihydroxy-10H-anthracen-9-one Drug Info IC50 = 18000 nM [10]
10-Benzoyl-1,8-dihydroxy-10H-anthracen-9-one Drug Info IC50 = 4000 nM [10]
2'-Nitro-biphenyl-4-carboxylic acid hydroxyamide Drug Info IC50 = 8300 nM [6]
2-(1H-Indol-3-ylmethyl)-1,2-dihydro-indazol-3-one Drug Info IC50 = 1100 nM [3]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Drug Info IC50 = 540 nM [3]
2-(4-Butoxy-phenoxy)-N-hydroxy-acetamide Drug Info IC50 = 5300 nM [6]
2-(4-Butoxy-phenoxy)-N-hydroxy-N-methyl-acetamide Drug Info IC50 = 890 nM [6]
2-(4-Butoxy-phenoxy)-N-hydroxy-propionamide Drug Info IC50 = 8060 nM [6]
2-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acetamide Drug Info IC50 = 720 nM [6]
2-(4-Methoxy-phenyl)-5-phenyl-thiazol-4-ol Drug Info IC50 = 450 nM [4]
2-(4-Phenyl-butyl)-1,2-dihydro-indazol-3-one Drug Info IC50 = 780 nM [3]
2-Benzyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 360 nM [3]
2-Biphenyl-4-yl-N-hydroxy-N-methyl-acetamide Drug Info IC50 = 360 nM [6]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 270 nM [3]
2-Methyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 1300 nM [3]
2-Naphthalen-1-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 610 nM [3]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 970 nM [3]
2-Phenethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 550 nM [3]
2-Phenyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 310 nM [3]
2-Pyridin-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 3100 nM [3]
2-Pyridin-3-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 1500 nM [3]
2-Pyridin-4-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 2400 nM [3]
2-Thiazol-5-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 1800 nM [3]
2-Thiophen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 400 nM [3]
3,4-Dihydroxy-10H-anthracen-9-one Drug Info IC50 = 4000 nM [10]
3-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acrylamide Drug Info IC50 = 100 nM [6]
3-Benzoyl-N-hydroxy-benzamide Drug Info IC50 = 7900 nM [6]
3-Biphenyl-3-yl-N-hydroxy-N-methyl-acrylamide Drug Info IC50 = 70 nM [6]
3-Biphenyl-4-yl-N-hydroxy-N-methyl-acrylamide Drug Info IC50 = 130 nM [6]
4,5-Dihydroxy-10H-anthracen-9-one Drug Info IC50 = 4000 nM [10]
4,5-Dimethoxy-10H-anthracen-9-one Drug Info IC50 = 8000 nM [10]
4-(1H-indol-3-yl)-1-morpholinobutan-1-one Drug Info IC50 = 2060 nM [2]
4-Bromo-N-hydroxy-benzamide Drug Info IC50 = 14000 nM [6]
4-Butoxy-N-hydroxy-N-methyl-benzamide Drug Info IC50 = 490 nM [6]
4-Hydroxy-5-methoxy-10H-anthracen-9-one Drug Info IC50 = 2000 nM [10]
4-Pentadeca-1,3,6-trienylsulfanyl-butyric acid Drug Info IC50 = 7200 nM [7]
5,8-Dihydroxy-1,4-naphthoquinone Drug Info IC50 = 3000 nM [10]
5-Chloro-N-(4-ethylphenyl)benzo[d]oxazol-2-amine Drug Info IC50 = 950 nM [5]
5-Chloro-N-phenylbenzo[d]oxazol-2-amine Drug Info IC50 = 4500 nM [5]
5-Methoxy-N-phenylbenzo[d]oxazol-2-amine Drug Info IC50 = 7880 nM [5]
5-Methyl-2-p-tolyl-thiazol-4-ol Drug Info IC50 = 1200 nM [4]
5-Methyl-N-phenylbenzo[d]oxazol-2-amine Drug Info IC50 = 4600 nM [5]
A-78773 Drug Info IC50 = 298 nM [12]
Acetic acid 2-phenyl-5-propyl-thiazol-4-yl ester Drug Info IC50 = 660 nM [4]
Acetic acid 5-butyl-2-phenyl-thiazol-4-yl ester Drug Info IC50 = 500 nM [4]
Anthracene-2-carboxylic acid hydroxyamide Drug Info IC50 = 980 nM [6]
ANTHRONE Drug Info IC50 = 2000 nM [10]
Avastin+/-Tarceva Drug Info IC50 = 17000 nM [10]
BAICALEIN Drug Info IC50 = 10000 nM [3]
Biphenyl-3-carboxylic acid hydroxyamide Drug Info IC50 = 6000 nM [6]
Biphenyl-4-carboxylic acid hydroxyamide Drug Info IC50 = 4100 nM [6]
Hexanoic acid 2,5-diphenyl-thiazol-4-yl ester Drug Info IC50 = 500 nM [4]
Ibuproxam Drug Info IC50 = 4840 nM [8]
N-(2-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Drug Info IC50 = 5660 nM [5]
N-(3-Bromophenyl)-5-methoxybenzo[d]oxazol-2-amine Drug Info IC50 = 2030 nM [5]
N-(4-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Drug Info IC50 = 120 nM [5]
N-(4-Ethylphenyl)benzo[d]oxazol-2-amine Drug Info IC50 = 1210 nM [5]
N-Hydroxy-2-methyl-3-naphthalen-2-yl-acrylamide Drug Info IC50 = 1800 nM [6]
N-Hydroxy-2-naphthalen-2-yl-acetamide Drug Info IC50 = 19000 nM [6]
N-Hydroxy-3-naphthalen-2-yl-acrylamide Drug Info IC50 = 950 nM [6]
N-Hydroxy-3-naphthalen-2-yl-N-p-tolyl-acrylamide Drug Info IC50 = 280 nM [6]
N-Hydroxy-3-naphthalen-2-yl-N-phenyl-acrylamide Drug Info IC50 = 52 nM [6]
N-Hydroxy-3-naphthalen-2-yl-propionamide Drug Info IC50 = 9700 nM [6]
N-Hydroxy-3-phenyl-acrylamide Drug Info IC50 = 12000 nM [6]
N-hydroxy-4-(naphthalen-1-yl)benzamide Drug Info IC50 = 180 nM [6]
N-Hydroxy-4-iodo-benzamide Drug Info IC50 = 15000 nM [6]
N-Hydroxy-4-isobutyl-benzamide Drug Info IC50 = 6000 nM [6]
N-Hydroxy-4-naphthalen-2-yl-benzamide Drug Info IC50 = 330 nM [6]
N-Hydroxy-N-methyl-2,3,3-triphenyl-acrylamide Drug Info IC50 = 2700 nM [6]
N-Hydroxy-N-methyl-2-naphthalen-2-yl-propionamide Drug Info IC50 = 590 nM [6]
N-Hydroxy-N-methyl-3-naphthalen-1-yl-acrylamide Drug Info IC50 = 210 nM [6]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-acrylamide Drug Info IC50 = 100 nM [8]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-propionamide Drug Info IC50 = 380 nM [6]
N-Hydroxy-N-methyl-3-phenanthren-2-yl-acrylamide Drug Info IC50 = 130 nM [6]
N-Hydroxy-N-methyl-3-phenanthren-3-yl-acrylamide Drug Info IC50 = 100 nM [6]
N-Hydroxy-N-methyl-3-phenanthren-9-yl-acrylamide Drug Info IC50 = 120 nM [6]
N-Hydroxy-N-methyl-benzamide Drug Info IC50 = 14000 nM [6]
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea Drug Info IC50 = 600 nM [9]
N-Phenylbenzo[d]oxazol-2-amine Drug Info IC50 = 8910 nM [5]
NAFAZATROM Drug Info IC50 = 6000 nM [7]
Naphthalene-2-carboxylic acid hydroxyamide Drug Info IC50 = 14000 nM [6]
Phenanthrene-2-carboxylic acid hydroxyamide Drug Info IC50 = 1900 nM [6]
Phenanthrene-3-carboxylic acid hydroxyamide Drug Info IC50 = 1200 nM [6]
PYROGALLOL Drug Info IC50 = 4000 nM [10]
REV-5901 Drug Info IC50 = 3000 nM [3]
TEBUFELONE Drug Info IC50 = 3000 nM [11]
TZI-41127 Drug Info IC50 = 110 nM
References
REF 1 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 2 Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling. Bioorg Med Chem Lett. 2007 May 1;17(9):2414-20.
REF 3 Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity. J Med Chem. 1991 Mar;34(3):1028-36.
REF 4 4-hydroxythiazole inhibitors of 5-lipoxygenase. J Med Chem. 1991 Jul;34(7):2158-65.
REF 5 Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors. Bioorg Med Chem. 2010 Nov 1;18(21):7580-5.
REF 6 Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships. J Med Chem. 1990 Mar;33(3):992-8.
REF 7 Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes. J Med Chem. 1990 Apr;33(4):1163-70.
REF 8 In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase. J Med Chem. 1987 Nov;30(11):2121-6.
REF 9 Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. J Med Chem. 1997 Feb 28;40(5):819-24.
REF 10 Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity. J Med Chem. 1997 Nov 7;40(23):3773-80.
REF 11 New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflamm... J Med Chem. 1998 Mar 26;41(7):1124-37.
REF 12 (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-3... J Med Chem. 1998 May 21;41(11):1970-9.
REF 13 Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.

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