2. Academic Validation
  3. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity

  • Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. doi: 10.1016/j.bmcl.2007.04.071.
Imadul Islam 1,  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
Affiliations

Affiliation

  • 1 Berlex Biosciences, 2600 Hilltop Dr. Richmond, CA 94804, USA.
PMID: 17531483 DOI: 10.1016/j.bmcl.2007.04.071
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13842
    ≥98.0%, PDK-1 Inhibitor