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Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. doi: 10.1016/j.bmcl.2011.01.071. Epub 2011 Jan 22.

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

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  • 1Takeda San Diego, San Diego, CA 92121, USA.


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.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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