Small kinase assay panels can provide a measure of selectivity

被引：19

作者：

Brandt, Peter ^{[1
]}

Jensen, Annika Jenmalm ^{[2
]}

Nilsson, Jonas ^{[3
]}

机构：

[1] Beactica AB, SE-75122 Uppsala, Sweden

[2] Karolinska Inst, MBB Chem Biol, SE-17177 Stockholm, Sweden

[3] i3 Innovus, SE-11164 Stockholm, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 20期

关键词：

Kinase panels; Ligand selectivity; Promiscuity; Multivariate analysis; PLS; Partial least squares; INTERACTION MAP; INHIBITORS; DESIGN;

D O I：

10.1016/j.bmcl.2009.08.083

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this Letter, a novel strategy for assessment of ligand promiscuity is described. By using a carefully selected small set of kinases together with multivariate statistical methods, a measure of selectivity can be estimated. This will facilitate an appropriate selection of compounds for further development in lead generation and optimization. (C) 2009 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5861 / 5863

页数：3

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