2pe1: Difference between revisions
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==Overview== | ==Overview== | ||
HTS screening identified 1 with micromolar inhibitory activity against | 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. | ||
==About this Structure== | ==About this Structure== | ||
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==Reference== | ==Reference== | ||
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: | Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity., Islam I, Bryant J, Chou YL, Kochanny MJ, Lee W, Phillips GB, Yu H, Adler M, Whitlow M, Ho E, Lentz D, Polokoff MA, Subramanyam B, Wu JM, Zhu D, Feldman RI, Arnaiz DO, Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. Epub 2007 Apr 27. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17531483 17531483] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
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[[Category: serine kinase]] | [[Category: serine kinase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:28:29 2008'' | ||
