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Benzothiophene inhibitors of MK2. Part 1: Structure-activity relationships, assessments of selectivity and cellular potency

  作者 Anderson, DR; Meyers, MJ; Kurumbail, RG; Caspers, N; Poda, GI; Long, SA; Pierce, BS; Mahoney, MW; Mourey, RJ  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-16;  页码  4878-4881  
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[摘要]Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are presented. Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.

 
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