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. 2019 May 23;10(6):978–984. doi: 10.1021/acsmedchemlett.9b00170

Table 1. Early SAR of Hit Scaffold.

graphic file with name ml-2019-00170c_0006.jpg

compd Y R1 X SMYD3 IC50 (μM)a
4 O Et Cl 4.78 ± 0.026
5 O Me Cl 123 ± 0.047
6 O nPr Cl 0.37 ± 0.044
7 O nBu Cl 0.36 ± 0.030
8 CH2 nPr Cl 1.52 ± 0.016
9 O –(CH2)2NH2 Cl 132.5 ± 0.06
10 CH2 –(CH2)2NH2 Cl >750
11 O Et H >750
12 O Et Me >750
a

Data represent mean value of duplicate experiments.