| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373450 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Graphical abstractOptimization of 1 afforded 4i (BX-517), a potent and selective inhibitor of PDK1.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Imadul Islam, Judi Bryant, Yuo-Ling Chou, Monica J. Kochanny, Wheeseong Lee, Gary B. Phillips, Hongyi Yu, Marc Adler, Marc Whitlow, Elena Ho, Dao Lentz, Mark A. Polokoff, Babu Subramanyam, James M. Wu, Daguang Zhu, Richard I. Feldman, Damian O. Arnaiz,