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

被引：40

作者：

Anderson, David R. ^{[1
]}

Meyers, Marvin J. ^{[1
]}

Kurumbail, Ravi G. ^{[1
]}

Caspers, Nicole ^{[1
]}

Poda, Gennadiy I. ^{[1
]}

Long, Scott A. ^{[1
]}

Pierce, Betsy S. ^{[1
]}

Mahoney, Matthew W. ^{[1
]}

Mourey, Robert J. ^{[1
]}

Parikh, Mihir D. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, St Louis Labs, Chesterfield, MO 63017 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

MK2; MAPKAP-K2; Kinase inhibitor;

D O I：

10.1016/j.bmcl.2009.02.017

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

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.

引用

页码：4882 / 4884

页数：3

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