Target Validation Information
TTD ID T99840
Target Name Gamma-secretase (GS)
Type of Target
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]
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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