Table 1.
RIPK2 and ALK2 kinases, and NOD2 cell (HEKBlue) signaling inhibitory activities of 14 and 15 – 20.
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|---|---|---|---|---|
| Compound | R1 | Kinase IC50 (μM) | RIPK2/NOD2 Cell Assay IC50 (μM) |
|
| RIPK2 | ALK2 | |||
| 14 | 2,6-di-Cl | 0.013 ± 0.004 | 0.021 ± 0.016 | 0.037 ± 0.004 |
| 15 | 2,4-di-Cl | 0.016 ± 0.0036 | NI | 0.16 ± 0.024 |
| 16 | 2-Cl | 0.017 ± 0.008 | 0.062 ± 0.080 | 0.004 ± 0.0005 |
| 17 | 4-Cl | 0.013 ± 0.0006 | 2.940 ± 1.633 | 0.95 ± 0.35 |
| 18 | 4-t-Bu | 0.105 ± 0.047 | NI | 1.98 ± 1.73 |
| 19 | 4-OH | 0.025 ± 0.014 | 0.059 ± 0.065 | 0.005 ± 0.002 |
| 20 | 4-OMe | 0.021 ± 0.0016 | NI | 0.51 ± 0.12 |
NI: No inhibition observed at 100 μM; IC50 values are shown as the mean of two or more determinations ± standard deviation.
