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Discovery and profiling of a selective and efficacious Syk inhibitor

Thoma, Gebhard, Smith, Alexander Baxter, Van Eis, Maurice, Vangrevelinghe, Eric, Blanz, Joachim, Aichholz, Reiner, Littlewood-Evans, Amanda, Lee, Christian, Liu, Hong and Zerwes, Hans-Guenter (2015) Discovery and profiling of a selective and efficacious Syk inhibitor. The Journal of Mecicinal Chemistry.


We describe the discovery of the potent and selective Syk inhibitor 11 which showed favorable PK profiles in rat and dog and was found to be active in a collagen induced arthritis model in rats. Compound 11 was selected for further profiling but, unfortunately, in GLP toxicological studies it showed liver findings in rat and dog. Consequently, compound 11 had to be abandoned. Nevertheless, 11 might be a valuable tool compound to study the biology of Syk in vitro and in vivo.

Item Type: Article
Keywords: Syk inhibitor
Date Deposited: 13 Oct 2015 13:11
Last Modified: 13 Oct 2015 13:11


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