Table 1.
In vitro evaluation of compounds 4, 14–16.
| Compound | IC50 hAChE (nM) 1 | IC50 hBuChE (nM) 1 | DYRK1a Inhibition (%) 1,2 | Propidium Iodide Displacement Inhibition (%) 3 |
|---|---|---|---|---|
| 2a 2 | 37.1 ± 0.1 | 1440.2 ± 286 | 0 | - |
| 14 | 81.4 ± 0.4 | 482 ± 21 | 5 | 26 ± 1 |
| 15 | >10,000 | 6400 ± 714 | 6 | - |
| 4 | 1023.1 ± 72.1 | 961 ± 22 | 8 | 4 ± 2 |
| 16 | >10,000 | >10,000 | 7 | - |
| Indy | >10,000 | >10,000 | 92 | - |
| Donepezil | 15.3 ± 1.7 | - | - | 18 ± 1 |
| Tacrine | - | 17.1 ± 0.1 | - | - |
1 Mean value of duplicate. 2 Percentage of DYRK1A inhibition at 1 μM (10 μM ATP concentration). 3 Mean value of triplicate.