Target Validation Information
TTD ID	T99840
Target Name	Gamma-secretase (GS)
Type of Target	Successful
Drug Potency against Target	E2012	Drug Info	IC50 = 1.3~58 nM
	(2S,3R)-2-(benzyloxy)-3-methoxycyclohexanone	Drug Info	IC50 = 13900 nM	[2]
	(5R,6S)-5,6-bis(benzyloxy)cyclohex-2-enone	Drug Info	IC50 = 1600 nM	[2]
	(5R,6S)-6-(benzyloxy)-5-methoxycyclohex-2-enone	Drug Info	IC50 = 10200 nM	[2]
	1-benzoyl-2-benzyl-1,2-dihydropyridin-3(6H)-one	Drug Info	IC50 = 1000 nM	[2]
	Drug 311383	Drug Info	IC50 = 14 nM	[1]
	Drug 311440	Drug Info	IC50 = 9 nM	[1]
	Drug 311951	Drug Info	IC50 = 16 nM	[1]
	Drug 311952	Drug Info	IC50 = 26 nM	[1]
Action against Disease Model	E2012	Drug Info	Among the six cell lines tested, only Jurkat and HepG2 showed a decrease in cell proliferation during 4 days of treatment with a gamma-secretase inhibitor	[3]
References
REF 1	Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase. J Med Chem. 2004 Jul 29;47(16):3931-3.
REF 2	Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3813-6.
REF 3	Acute effect on the A isoform pattern in CSF in response to -secretase modulator and inhibitor treatment in dogs. J Alzheimers Dis. 2010;21(3):1005-12.

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