2. Academic Validation
  3. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. doi: 10.1016/j.bmcl.2011.01.071.
Qing Dong 1,  Douglas R Dougan,  Xianchang Gong,  Petro Halkowycz,  Bohan Jin,  Toufike Kanouni,  Shawn M O'Connell,  Nicholas Scorah,  Lihong Shi,  Michael B Wallace,  Feng Zhou
Affiliations

Affiliation

  • 1 Takeda San Diego, San Diego, CA 92121, USA.
PMID: 21310613 DOI: 10.1016/j.bmcl.2011.01.071
Abstract

A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for Cancer treatment.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13449
    98.31%, MEK Inhibitor
    MEK