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J Med Chem. 2015 Feb 26;58(4):1950-63. doi: 10.1021/jm5018863. Epub 2015 Feb 9.

Discovery and profiling of a selective and efficacious Syk inhibitor.

Author information

1
Global Discovery Chemistry, ‡Analytical Sciences & Imaging, §Autoimmunity, Transplantation and Inflammation Research, Novartis Institutes for Biomedical Research , 4056 Basel, Switzerland.

Abstract

We describe the discovery of selective and potent Syk inhibitor 11, which exhibited 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. Nevertheless, 11 could become a valuable tool compound to investigate the rich biology of Syk in vitro and in vivo.

PMID:
25633741
DOI:
10.1021/jm5018863
[Indexed for MEDLINE]

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