Target Validation Information
TTD ID	T16042
Target Name	Arachidonate 15-lipoxygenase (15-LOX)
Type of Target	Patented-recorded
Drug Potency against Target	(+)-(5S,8S,10S)-20-methoxy-9,15-ene-puupehenol	Drug Info	IC50 = 1000 nM	[1]
	(+)-(5S,8S,10S)-20-methoxypuupehenol	Drug Info	IC50 = 7200 nM	[1]
	(+)-(5S,8S,9R,10S)-20-methoxypuupehenone	Drug Info	IC50 = 1700 nM	[1]
	(+)-3,3'-bisdemethyltanegool	Drug Info	IC50 = 760 nM	[3]
	(-)-3,3'-bisdemethylpinoresinol	Drug Info	IC50 = 520 nM	[3]
	(-)-pinoresinol	Drug Info	IC50 = 3500 nM	[3]
	2,3,4,5-Tetrabromo-6-(2,4-dibromo-phenoxy)-phenol	Drug Info	IC50 = 1800 nM	[2]
	3,4,6-Tribromo-2-(2,4-dibromo-phenoxy)-phenol	Drug Info	IC50 = 5000 nM	[2]
	3,4-Dibromo-2-(5-bromo-2-hydroxy-phenoxy)-phenol	Drug Info	IC50 = 11000 nM	[2]
	3,6,8-Tribromo-dibenzo[1,4]dioxin-1-ol	Drug Info	IC50 = 800 nM	[2]
	CHLOROPUUPEHENONE	Drug Info	IC50 = 830 nM	[1]
	Dimethylnordihydroguarierate acid	Drug Info	IC50 = 580 nM	[1]
	DYSIDENIN	Drug Info	Ki = 8000 nM	[4]
	Halisulfate 1	Drug Info	IC50 = 900 nM	[1]
	Hydrohalisulfate 1	Drug Info	IC50 = 500 nM	[1]
	IGERNELLIN	Drug Info	IC50 = 17000 nM	[1]
	Isojaspic acid	Drug Info	IC50 = 5300 nM	[5]
	ISOSCOPOLETIN	Drug Info	IC50 = 15100 nM	[3]
	JASPAQUINOL	Drug Info	IC50 = 19000 nM	[5]
	Jaspic acid	Drug Info	IC50 = 1400 nM	[1]
	KAEMPFEROL	Drug Info	IC50 = 2200 nM	[3]
	MANGOSTIN	Drug Info	IC50 = 3100 nM	[4]
	NSC-172033	Drug Info	IC50 = 9400 nM	[4]
	PD-146176	Drug Info	IC50 = 1120 nM	[3]
	Polybrominated diphenyl ether derivative	Drug Info	IC50 = 4000 nM	[2]
	PUUPEHEDIONE	Drug Info	IC50 = 7000 nM	[5]
	PUUPEHENONE	Drug Info	IC50 = 6000 nM	[5]
	SCOPOLETIN	Drug Info	IC50 = 16500 nM	[3]
	SPONGIADIOXIN A	Drug Info	IC50 = 900 nM	[2]
	Subersic acid	Drug Info	IC50 = 14500 nM	[1]
References
REF 1	Exploring sponge-derived terpenoids for their potency and selectivity against 12-human, 15-human, and 15-soybean lipoxygenases. J Nat Prod. 2003 Feb;66(2):230-5.
REF 2	Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase. J Med Chem. 2004 Jul 29;47(16):4060-5.
REF 3	Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti. J Nat Prod. 2007 May;70(5):859-62.
REF 4	Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries. Bioorg Med Chem. 2007 Nov 15;15(22):6900-8.
REF 5	Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes. J Nat Prod. 2009 Oct;72(10):1857-63.

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