Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T93105 | ||||
Target Name | Presenilin 1 (PSEN1) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | (2S,3R)-2-(benzyloxy)-3-methoxycyclohexanone | Drug Info | IC50 = 13900 nM | [3] | |
(5R,6S)-5,6-bis(benzyloxy)cyclohex-2-enone | Drug Info | IC50 = 1600 nM | [3] | ||
(5R,6S)-6-(benzyloxy)-5-methoxycyclohex-2-enone | Drug Info | IC50 = 10200 nM | [3] | ||
1-benzoyl-2-benzyl-1,2-dihydropyridin-3(6H)-one | Drug Info | IC50 = 1000 nM | [3] | ||
1-Chloro-4-(1-phenyl-cyclohexanesulfonyl)-benzene | Drug Info | IC50 = 461 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] | ||
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 | Aryl sulfones: a new class of gamma-secretase inhibitors. Bioorg Med Chem Lett. 2005 May 16;15(10):2685-8. | ||||
REF 3 | 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. | ||||
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