Enzyme selectivity of compound 3
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
Table 7
As shown in Table 7, analog 3 exhibited exquisite selectivity over other kinases. It was at least 200-fold selective over Tec family kinases and over 55-fold selective against other kinases tested. In addition, 3 showed ATP competitive kinetics.
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