Table 2.
Percentage (%) of inhibition of compound 4 at 0.1 and 10 μM against a panel of 20 different PKs and open targets platform-based scores.
| Rank | Kinase | Kinase Inhibition %a | Overall Nervous System tauopathy like diseases score |
|
|---|---|---|---|---|
| 0.1 μM | 10 μM | |||
| 1 | DYRK1A(h) | 14 | 92 | 0.89 |
| 2 | CDK5/p25(h) | 86 | 97 | 0.84 |
| 3 | FYN(h) | 100 | 100 | 0.60 |
| 4 | GSK-3β(h) | 94 | 100 | 0.59 |
| 5 | GSK-3α(h) | 96 | 100 | 0.45 |
| 6 | SAPK2a(h) | 13 | 27 | 0.42 |
| 7 | MAPK1(h) | 19 | 67 | 0.38 |
| 8 | MAP4K4(h) | 14 | 99 | 0.36 |
| 9 | JNK1α1(h) | 11 | 80 | 0.32 |
| 10 | PKA(h) | 9 | 88 | 0.31 |
| 11 | cSRC(h) | 96 | 96 | 0.30 |
| 12 | CDK1/cyclinB(h) | 62 | 99 | 0.16 |
| 13 | Yes(h) | 98 | 100 | 0.05 |
| 14 | Lck(h) activated | 58 | 97 | 0.04 |
| 15 | CK1δ(h) | 6 | 73 | 0.03 |
| 16 | DYRK1B(h) | 10 | 88 | 0.02 |
| 17 | CK1ε(h) | 0 | 83 | 0.02 |
| 18 | CK2(h) | 5 | 75 | 0.01 |
| 19 | DYRK3(h) | 19 | 90 | 0 |
| 20 | DYRK2(h) | 16 | 77 | 0 |
Kinases are ranked according to the reported overall strength of a given target–disease association from the Open target Platform (https://platform.opentargets.org) [27]. Panel of selectivity data are shown according to the following color scale: green color is associated with a high % of inhibition values; orange is associate with a modest % of inhibition; red color corresponds to a low % of inhibition.
a
Data are reported as the mean of two independent experiments.