The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The K
d
for the inhibitor compound is derived based on the K
d
of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides novel active site probes suitable for use with the screening method.
该发明提供了一种新型筛选检测方法,可应用于蛋白激酶
基因家族的广泛成员。该检测方法使用一系列标记的活性位点探针,这些探针可以被
抑制剂代替。
抑制剂化合物的Kd是基于探针对激酶的Kd和
抑制剂代理的剂量反应推导出来的。该发明还提供了适用于筛选方法的新型活性位点探针。