Target Validation Information
TTD ID	T93566
Target Name	LOX-5 messenger RNA (ALOX5 mRNA)
Type of Target	Discontinued
Drug Potency against Target		Drug Info	IC50 = 117 nM	[2]
	(+)-3,3'-bisdemethyltanegool	Drug Info	IC50 = 9200 nM	[4]
	(-)-3,3'-bisdemethylpinoresinol	Drug Info	IC50 = 5900 nM	[4]
	(-)-pinoresinol	Drug Info	IC50 = 13800 nM	[4]
	(N-(3-phenoxycinnamyl)-acetohydroxamic acid	Drug Info	IC50 = 38 nM	[7]
	2,4'-Diacetoxy-5,3'-di-(2-propenyl)-biphenyl	Drug Info	IC50 = 4500 nM	[6]
	2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl	Drug Info	IC50 = 15000 nM	[6]
	2,4,5-Triarylimidazole analogue	Drug Info	IC50 = 350 nM
	2-(benzyloxy)naphthalene	Drug Info	IC50 = 9500 nM	[8]
	4'-Methoxy-5,3'-dipropyl-biphenyl-2ol	Drug Info	IC50 = 1400 nM	[6]
	5,3'-Dipropyl-biphenyl-2,4'-diol	Drug Info	IC50 = 1700 nM	[6]
	BW A4C	Drug Info	IC50 = 200 nM	[5]
	HONOKIOL	Drug Info	IC50 = 4200 nM	[6]
	ISAINDIGOTONE	Drug Info	IC50 = 40 nM	[1]
	Isojaspic acid	Drug Info	IC50 = 18000 nM	[9]
	JASPAQUINOL	Drug Info	IC50 = 450 nM	[9]
	KAEMPFEROL	Drug Info	IC50 = 2700 nM	[4]
	L-689065	Drug Info	IC50 = 22 nM	[11]
	L-702-539	Drug Info	IC50 = 190 nM	[13]
	L-746530	Drug Info	IC50 = 36 nM	[3]
	Methyl 2-(Benzylamino)-1H-indole-3-carboxylate	Drug Info	IC50 = 3400 nM	[7]
	Methyl 2-(Diallylamino)-1H-indole-3-carboxylate	Drug Info	IC50 = 6900 nM	[7]
	METHYLHONOKIOL	Drug Info	IC50 = 1500 nM	[6]
	N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea	Drug Info	IC50 = 2500 nM	[12]
	PD-169316	Drug Info	IC50 = 50 nM
	PUUPEHEDIONE	Drug Info	IC50 = 4600 nM	[9]
	PUUPEHENONE	Drug Info	IC50 = 680 nM	[9]
	TEBUFELONE	Drug Info	IC50 = 3000 nM	[14]
	ZD-2138	Drug Info	IC50 = 20 nM	[10]
	Zileuton	Drug Info	IC50 = 500 nM	[9]
References
REF 1	Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives. J Nat Prod. 2001 Oct;64(10):1297-300.
REF 2	Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 3	Substituted coumarins as potent 5-lipoxygenase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31.
REF 4	Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti. J Nat Prod. 2007 May;70(5):859-62.
REF 5	Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid. J Med Chem. 2008 Sep 11;51(17):5449-53.
REF 6	Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxyge... Bioorg Med Chem. 2009 Jul 1;17(13):4459-65.
REF 7	Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. J Med Chem. 2009 Jun 11;52(11):3474-83.
REF 8	Bioactivity-guided mapping and navigation of chemical space. Nat Chem Biol. 2009 Aug;5(8):585-92.
REF 9	Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes. J Nat Prod. 2009 Oct;72(10):1857-63.
REF 10	Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. Bioorg Med Chem. 2010 Jun 1;18(11):3910-24.
REF 11	Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation ... J Med Chem. 1993 Sep 17;36(19):2771-87.
REF 12	Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. J Med Chem. 1997 Feb 28;40(5):819-24.
REF 13	Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics... J Med Chem. 1997 Aug 29;40(18):2866-75.
REF 14	New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflam... J Med Chem. 1998 Aug 27;41(18):3515-29.

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