title: Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).
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.
authors: NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.
authors: Andrew S
authors: AS
authors: Rosenthal
authors: Cordelle
authors: C
authors: Tanega
authors: Min
authors: M
authors: Shen
authors: Bryan T
authors: BT
authors: Mott
authors: James M
authors: JM
authors: Bougie
authors: Dac-Trung
authors: DT
authors: Nguyen
authors: Tom
authors: T
authors: Misteli
authors: Douglas S
authors: DS
authors: Auld
authors: David J
authors: DJ
authors: Maloney
authors: Craig J
authors: CJ
authors: Thomas
mesh_terms: D004789:Enzyme Activation / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008958:Models, Molecular; D015394:Molecular Structure; D010766:Phosphorylation; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013379:Substrate Specificity; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000097603:Dyrk Kinases
chemical_list: D004791:Enzyme Inhibitors; D007527:Isoenzymes; D017346:Protein Serine-Threonine Kinases; D011505:Protein-Tyrosine Kinases; D011799:Quinazolines; D054852:Small Molecule Libraries; D013844:Thiazoles; D000097603:Dyrk Kinases; C487497:TG 003; C066780:Clk dual-specificity kinases