Table 2.
RIPK2 and ALK2 kinases, and NOD2 cell (HEKBlue) signaling inhibitory activities of 21- 28.
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|---|---|---|---|---|---|
| Compound | R1 | R2 | Kinase IC50 (μM) | RIPK2/NOD2 Cell Assay IC50 (μM) |
|
| RIPK2 | ALK2 | ||||
| 21 | H | Me | 0.0105 ± 0.002 | 0.284 ± 0.356 | 0.014 ± 0.004 |
| 22 | H | Et | ~ 30 nM | 0.004 ± 0.005 | 0.015 ± 0.005 |
| 23 | H | CH2CH2OH | ~ 30 nM | 0.018 ± 0.024 | 0.27 ± 0.22 |
| 24 | 2,6-di-Cl | CH2CH2OMe | 0.128 ± 0.001 | 0.018 ± 0.019 | 0.013 ± 0.007 |
| 25 | 2,6-di-Cl | CH2Ph | 0.021 ± 0.003 | 0.008 ± 0.004 | 0.009 ± 0.003 |
| 26 | 2,6-di-Cl | i-Bu | 0.005 ± 0.002 | 0.009 ± 0.005 | 0.003 ± 0.0005 |
| 27 | 2,6-di-Cl | CH2Ph-3-SO2Me | 0.025 ± 0.008 | 0.092 ± 0.005 | 0.005 ± 0.005 |
| 28 | 2,6-di-Cl | CH2Ph-4-SO2Me | 0.021 ± 0.007 | ND | 0.094 ± 0.004 |
ND: Not determined; IC50 values are shown as the mean of two or more determinations ± standard deviation, unless otherwise indicated.
