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. 2019 Sep 13;10(10):1443–1449. doi: 10.1021/acsmedchemlett.9b00243

Table 3. Alkoxy Substituent SAR for the Kinase Selective Dihydropyridopyrazinone Scaffold.

graphic file with name ml9b00243_0007.jpg

Cmpd R TAF1(2)a (μM) BRD4(1)a (μM)
13 OMe 0.016 0.037
14 H 0.34 0.19
15 O-iPr 0.089 0.13
16 O-cycloPent 0.031 0.048
a

AlphaScreen IC50s from quadruplicate measurement.