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Updated: Jul 12, 2026

Quantitative Measurement of γ-Secretase-mediated Amyloid Precursor Protein and Notch Cleavage in Cell-based Luciferase Reporter Assay Platforms
Published on: January 25, 2018
Thiazole-diamides as potent gamma-secretase inhibitors
Yuhpyng L Chen1, Kevin Cherry, Michael L Corman
1Department of Medicinal Chemistry, PGRD, Pfizer Inc., Connecticut, Groton, CT 06340, USA. yuhpyng888@yahoo.com
Abstract:
The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.
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