Table 8. Selectivity profiles of JNK inhibitors across the Nek family.
Compound | JNK-IN-1 a | JNK-IN-2 b | JNK-IN-7 a | JNK-IN-8 a | JNK-9L c | JNK-IN-11 a | JNK-IN-12 a |
% control (10 μM) | |||||||
Nek1 | 100 | 63 | 77 | 81 | 57 | 100 | 100 |
Nek2 | 100 | 1.1 | 86 | 100 | 94 | 93 | 99 |
Nek3 | 99 | 17 | 6.8 | 73 | 0.8 | 99 | 100 |
Nek4 | 100 | 100 | 83 | 79 | 100 | 100 | 100 |
Nek5 | 51 | 2.2 | 7.8 | 92 | 1.4 | 98 | 100 |
Nek6 | 44 | 2.8 | 17 | 100 | 76 | 100 | 100 |
Nek7 | 20 | 9.8 | 7 | 100 | 45 | 100 | 100 |
Nek9 | 100 | 22 | 48 | 100 | 63 | 100 | 63 |
Nek11 | 78 | 100 | 86 | 99 | 100 | 100 | 100 |
# kinases ≤10% control | 26 | 45 | 35 | 14 | 53 | 63 | 9 |
a Data taken from Zhang et al., 2012.
b HMS LINCS Dataset 20048.
c HMS LINCS Dataset 20078.