Target Validation Information
Target ID T93566
Target Name mRNA of human 5-lipoxygenase
Target Type
Discontinued
Drug Potency against Target 2,4,5-Triarylimidazole analogue Drug Info IC50 = 350 nM
Methyl 2-(Diallylamino)-1H-indole-3-carboxylate Drug Info IC50 = 6900 nM [1]
CMI-977 Drug Info IC50 = 117 nM [2]
L-702-539 Drug Info IC50 = 190 nM [3]
L-746530 Drug Info IC50 = 36 nM [4]
JASPAQUINOL Drug Info IC50 = 450 nM [5]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol Drug Info IC50 = 1400 nM [6]
METHYLHONOKIOL Drug Info IC50 = 1500 nM [6]
(N-(3-phenoxycinnamyl)-acetohydroxamic acid Drug Info IC50 = 38 nM [1]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info IC50 = 15000 nM [6]
Methyl 2-(Benzylamino)-1H-indole-3-carboxylate Drug Info IC50 = 3400 nM [1]
2,4'-Diacetoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info IC50 = 4500 nM [6]
HONOKIOL Drug Info IC50 = 4200 nM [6]
(-)-3,3'-bisdemethylpinoresinol Drug Info IC50 = 5900 nM [7]
Isojaspic acid Drug Info IC50 = 18000 nM [5]
(-)-pinoresinol Drug Info IC50 = 13800 nM [7]
(+)-3,3'-bisdemethyltanegool Drug Info IC50 = 9200 nM [7]
5,3'-Dipropyl-biphenyl-2,4'-diol Drug Info IC50 = 1700 nM [6]
N-(3-phenoxycinnamyl)-N-hydroxyacetamide Drug Info IC50 = 200 nM [8]
TEBUFELONE Drug Info IC50 = 3000 nM [9]
ISAINDIGOTONE Drug Info IC50 = 40 nM [10]
ZD-2138 Drug Info IC50 = 20 nM [11]
2-(benzyloxy)naphthalene Drug Info IC50 = 9500 nM [12]
PD-169316 Drug Info IC50 = 50 nM
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea Drug Info IC50 = 2500 nM [13]
KAEMPFEROL Drug Info IC50 = 2700 nM [7]
PUUPEHEDIONE Drug Info IC50 = 4600 nM [5]
Zileuton Drug Info IC50 = 500 nM [5]
PUUPEHENONE Drug Info IC50 = 680 nM [5]
L-689065 Drug Info IC50 = 22 nM [14]
References
REF 1J Med Chem. 2009 Jun 11;52(11):3474-83.Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.
REF 2J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 3J Med Chem. 1997 Aug 29;40(18):2866-75.Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
REF 4Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31. Epub 2006 Feb 7.Substituted coumarins as potent 5-lipoxygenase inhibitors.
REF 5J Nat Prod. 2009 Oct;72(10):1857-63.Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes.
REF 6Bioorg Med Chem. 2009 Jul 1;17(13):4459-65. Epub 2009 May 18.Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4-formation.
REF 7J Nat Prod. 2007 May;70(5):859-62. Epub 2007 Mar 23.Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.
REF 8J Med Chem. 2008 Sep 11;51(17):5449-53. Epub 2008 Aug 19.Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid.
REF 9J Med Chem. 1998 Aug 27;41(18):3515-29.New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.
REF 10J Nat Prod. 2001 Oct;64(10):1297-300.Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.
REF 11Bioorg Med Chem. 2010 Jun 1;18(11):3910-24. Epub 2010 Apr 18.Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
REF 12Nat Chem Biol. 2009 Aug;5(8):585-92. Epub 2009 Jun 28.Bioactivity-guided mapping and navigation of chemical space.
REF 13J Med Chem. 1997 Feb 28;40(5):819-24.Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
REF 14J Med Chem. 1993 Sep 17;36(19):2771-87.Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.

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