Table 1 Comparison of chosen kinase panel profiling between compound 1c and compound 2d.
From: Positioning of an unprecedented spiro[5.5]undeca ring system into kinase inhibitor space
Kinase | % Residual Activity at 30 μMa | |
|---|---|---|
Compound 2d | Compound 1cb | |
ARK5/NUAK1 | 88.9 ± 6.7 | 70.8 ± 0.1 |
CDK1/cyclin B | 59.0 ± 0.5 | 46.0 ± 0.8 |
CDK2/cyclin O | 54.3 ± 0.1 | 43.1 ± 1.0 |
CDK3/cyclin E | 60.3 ± 1.9 | 59.3 ± 1.2 |
DAPK1 | 74.6 ± 1.7 | 45.4 ± 0.1 |
DAPK2 | 110.2 ± 0.6 | 120.1 ± 0.6 |
GSK3β | 2.2 ± 0.8 | 107.5 ± 1.9 |
Haspin | 70.9 ± 0.9 | 66.4 ± 0.5 |
JNK1 | 82.7 ± 0.1 | 35.8 ± 0.3 |
JNK2 | 80.0 ± 0.4 | 58.3 ± 0.7 |
JNK3 | 95.4 ± 0.1 | 72.0 ± 2.0 |
MST3/STK24 | 91.8 ± 3.4 | 58.3 ± 0.7 |
P38b/MAPK11 | 109.9 ± 0.5 | 87.0 ± 1.1 |
PKCa | 62.6 ± 0.5 | 45.6 ± 1.2 |
PKN2/PRK2 | 99.5 ± 3.3 | 63.5 ± 1.8 |
RIPK5 | 85.0 ± 1.6 | 59.3 ± 1.0 |
ROCK1 | 103.3 ± 3.1 | 97 ± 2.9 |
ROCK2 | 99.4 ± 1.5 | 103.9 ± 2.4 |
STK25/YSK1 | 62.2 ± 1.6 | 66.9 ± 0.1 |
TLK1 | 81.7 ± 0.5 | 58.0 ± 0.9 |
TRKA | 117.3 ± 2.6 | 98.3 ± 0.1 |
TRKB | 102.2 ± 1.3 | 94.1 ± 1.7 |
TRKC | 105.4 ± 3.9 | 97.9 ± 0.2 |
ZIPK/DAPK3 | 87.9 ± 1.3 | 101.8 ± 0.8 |
