Table 1. Early SAR of Hit Scaffold.
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 |
Data represent mean value of duplicate experiments.