2. Academic Validation
  3. 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)

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3152-8. doi: 10.1016/j.bmcl.2011.02.114.
Andrew S Rosenthal 1,  Cordelle Tanega,  Min Shen,  Bryan T Mott,  James M Bougie,  Dac-Trung Nguyen,  Tom Misteli,  Douglas S Auld,  David J Maloney,  Craig J Thomas
Affiliations

Affiliation

  • 1 NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.
PMID: 21450467 DOI: 10.1016/j.bmcl.2011.02.114
Abstract

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.

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