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Merck
CN
  • Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

Bioorganic & medicinal chemistry letters (2011-04-01)
Andrew S Rosenthal, Cordelle Tanega, Min Shen, Bryan T Mott, James M Bougie, Dac-Trung Nguyen, Tom Misteli, Douglas S Auld, David J Maloney, Craig J Thomas
摘要

Continued examination of substituted 6-arylquinazolin-4-amines as Clk4 inhibitors resulted in selective inhibitors of Clk1, Clk4, Dyrk1A and Dyrk1B. Several of the most potent inhibitors were validated as being highly selective within a comprehensive kinome scan.