Table 2. Activity of novel indole compounds against DYRK1A and related kinases relative to ID-8.
| Compound | R1 | R2 | R3 | IC50 (μM) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| DYRK1A | DYRK1B | DYRK2 | CLK1 | CLK4 | GSK3α | GSK3β | LRRK2 | PIM1 | PIM3 | ||||
| ID-8 | 6-OH | NO2 | p-OCH3 | 0.104 | 0.040 | NC | 1.37 | 1.05 | 0.428 | 0.153 | 0.100 | 0.376 | 0.176 |
| 34 | 6-OCOCH3 | NHCOCH3 | p-OCH3 | NC | NC | NC | NC | NC | NC | NC | NC | NC | NC |
| 28 | 6-OCH3 | NO2 | p-OCH3 | 0.346 | 0.695 | NC | NC | 2.23 | 2.36 | 3.44 | 0.854 | 0.176 | 0.259 |
| 29 | 6-OCH2C6H5 | NO2 | p-OCH3 | 6.52 | 3.57 | NC | NC | NC | 18.0 | 14.3 | 8.16 | 18.5 | 8.28 |
| 30 | 6-OCOCH3 | NO2 | p-OCH3 | 0.680 | 0.299 | NC | NC | 11.95 | 22.15 | 1.71 | 0.891 | 4.15 | 1.21 |
| 45 | 6-OH | NO2 | p-OH | 0.122 | 0.060 | 2.30 | 0.364 | 0.163 | 0.375 | 0.233 | 0.046 | 0.243 | 0.180 |
| 48 | 6-OH | NO2 | m-OCH3 | 0.594 | 0.257 | NC | 13.0 | 4.77 | 2.32 | 0.692 | 2.17 | 0.654 | 0.593 |
| 49 | 6-OH | NO2 | o-OCH3 | 0.829 | 0.341 | 41.9 | 10.7 | 8.59 | 6.12 | 3.82 | 1.98 | 1.44 | 0.892 |
| 51 | 5-NO2 | NO2 | p-OCH3 | NC | NC | NC | NC | NC | NC | NC | NC | 7.62 | 4.57 |
| 38 | H | NO2 | p-OCH3 | NC | NC | NC | NC | NC | NC | NC | NC | NC | 20.74 |