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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
A structural screening approach to ketoamide-based inhibitors of cathepsin K
David G Barrett1, John G Catalano, David N Deaton
1Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA.
Bioorganic & Medicinal Chemistry Letters
|April 20, 2005
Abstract:
Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P2 elements led to 100-fold enhancements in inhibitory activity. Modifications to one of these leads resulted in an orally bioavailable cathepsin K inhibitor.
