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Updated: Jun 1, 2026

08:49
Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase
Steven T Staben1, Michael Siu, Richard Goldsmith
1Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. stevents@gene.com
Bioorganic & Medicinal Chemistry Letters
|June 4, 2011
Abstract:
Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenograft model.
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