Table 2. SAR Studies for Other Parts of Lead Compounds.
biochemical
inhibition IC50 (μM)a |
|||||
---|---|---|---|---|---|
compd | R | JNK3 | JNK1 (R)b | JNK2 (R)b | p38α (R)b |
18 | 0.002 | 0.258 (129) | 0.029 (15) | 0.024 (12) | |
19 | 0.005 | 1.24 (248) | ndc | 0.065 (13) | |
20 | 0.03 | 2.42 (80) | 1.02 (33) | 0.286 (9) | |
21 | 0.024 | 4.73 (197) | 0.414 (17) | 0.481 (20) | |
3 | 0.005 | 0.69 (139) | ndc | 0.086 (17) | |
22 | 0.002 | 0.26 (130) | 0.074 (37) | 0.057 (28) | |
4 | 0.006 | 0.94 (157) | 0.256 (43) | 0.26 (43) | |
23 | 0.002 | 0.213 (106) | 0.052 (26) | 0.106 (50) | |
24 | 0.012 | 0.872 (73) | 0.14 (11) | 0.38 (31) | |
25 | >10 | >10 | ndc | >10 | |
26 | 2-Cl-3-F | 0.169 | >10 (>59) | ndc | 1.42 (8) |
27 | 2-Cl-4-F | 0.079 | 6.0 (76) | ndc | 0.49 (51) |
28 | 2-Cl-5-F | 1.07 | >10 | ndc | 2.89 |
29 | 2-Cl-6-F | 0.005 | 0.387 (77) | 0.074 (15) | 0.106 (21) |
The average of ≥2 experiments with errors within 30% of the average.
R: ratio of IC50 values for JNK1, JNK2, and p38α over JNK3.
Not determined.