Target Validation Information
TTD ID	T35527
Target Name	Arachidonate 12-lipoxygenase (12-LOX)
Type of Target	Literature-reported
Drug Potency against Target	(+)-(5S,8S,10S)-20-methoxy-9,15-ene-puupehenol	Drug Info	IC50 = 780 nM	[1]
	(+)-(5S,8S,10S)-20-methoxypuupehenol	Drug Info	IC50 = 280 nM	[1]
	(+)-(5S,8S,9R,10S)-20-methoxypuupehenone	Drug Info	IC50 = 260 nM	[1]
	(-)-7-N-methyldibromophakellin	Drug Info	IC50 = 10700 nM	[3]
	2,3,4,5-Tetrabromo-6-(2,4-dibromo-phenoxy)-phenol	Drug Info	IC50 = 700 nM	[2]
	3,4,6-Tribromo-2-(2,4-dibromo-phenoxy)-phenol	Drug Info	IC50 = 6000 nM	[2]
	CHLOROPUUPEHENONE	Drug Info	IC50 = 2400 nM	[1]
	Dimethylnordihydroguarierate acid	Drug Info	IC50 = 3100 nM	[1]
	DYSIDENIN	Drug Info	Ki = 9000 nM	[4]
	Isojaspic acid	Drug Info	IC50 = 3100 nM	[5]
	Jaspic acid	Drug Info	IC50 = 7600 nM	[1]
	NEODYSIDENIN	Drug Info	Ki = 17000 nM	[4]
	Polybrominated diphenyl ether derivative	Drug Info	IC50 = 2300 nM	[2]
	PUUPEHEDIONE	Drug Info	IC50 = 18000 nM	[5]
	PUUPEHENONE	Drug Info	IC50 = 2400 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	An analysis of phakellin and oroidin structures stimulated by further study of an Agelas sponge. J Nat Prod. 2004 Aug;67(8):1256-61.
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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