Table 2.
Kinase inhibitory activities of compounds 10–29 against PAK4.
![]() | ||||||||
---|---|---|---|---|---|---|---|---|
Compd. | R2 | PAK4 Ki (μmol/L)a | Compd. | R2 | PAK4 Ki (μmol/L)a | Compd. | R2 | PAK4 Ki (μmol/L)a |
10 | ![]() |
0.623 | 17 | ![]() |
0.157 | 24 | ![]() |
0.298 |
11 | ![]() |
0.223 | 18 | ![]() |
0.242 | 25 | ![]() |
0.189 |
12 | ![]() |
0.355 | 19 | ![]() |
0.212 | 26 | ![]() |
0.083 |
13 | ![]() |
0.291 | 20 | ![]() |
0.396 | 27 | ![]() |
>10 |
14 | ![]() |
7.455 | 21 | ![]() |
0.173 | 28 | ![]() |
0.680 |
15 | ![]() |
0.217 | 22 | ![]() |
0.709 | 29 | ![]() |
1.109 |
16 |
![]() |
0.105 | 23 | ![]() |
0.230 | |||
PAK4 kinase inhibition was determined using a homogeneous time-resolved fluorescence (HTRF) assay. The Ki values are the average of two independent experiments, reported as the mean value.