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Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency

  作者 Anderson, DR; Meyers, MJ; Kurumbail, RG; Caspers, N; Poda, GI; Long, SA; Pierce, BS; Mahoney, MW; Mourey, RJ; Parikh, MD  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-16;  页码  4882-4884  
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[摘要]Optimization of kinase selectivity for a set of benzothiophene MK2 inhibitors provided analogs with potencies of less than 500 nM in a cell based assay. The selectivity of the inhibitors can be rationalized by examination of X-ray crystal structures of inhibitors bound to MK2. (C) 2009 Elsevier Ltd. All rights reserved.

 
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