Table 1.
compound | R' | R | JNK3 IC50 (µM) |
JNK1 IC50 (µM) |
c-jun IC50 (µM) |
bmouse [plasma] |
(µM) [brain] |
---|---|---|---|---|---|---|---|
3 | 0.09 | 0.05 | 0.31 | 17.8 | 7.17 | ||
8a | 0.05 | 0.04 | 0.12 | 42.9 | 1.31 | ||
8b | 0.7 | nt | nt | nt | nt | ||
8c | 4.4 | nt | nt | nt | nt | ||
8d | 0.21 | nt | nt | 26.7 | 8.1 | ||
8e | 0.73 | nt | nt | nt | nt | ||
8f | >20 | nt | nt | nt | nt | ||
8g | 0.05 | nt | 0.04 | nt | nt | ||
8h | 0.06 | 0.1 | 0.29 | 13.1 | 1.37 |
JNK3 biochemical IC50 values are the averages of four or more experiments, and the JNK1 and cell-based IC50 values are the averages of two or more experiments. All standard deviations are ≤44% for the biochemical and ≤81% for the cell-based assays.
10 mg/kg ip 2h.
nt = not tested.