Table 1. Inhibitory Activity of the Compound on BACE1 and GSK3β.
| compound | inhibitiona(%, hBACE1) | inhibitionb(%, hGSK3β) | compound | inhibitiona(%, hBACE1) | inhibitionb(%, hGSK3β) |
|---|---|---|---|---|---|
| A1 | 34 ± 1 | 35 ± 1 | B6 | 13 ± 1 | 37 ± 1 |
| A2 | 55 ± 1 | 34 ± 1 | B7 | 60 ± 1 | 34 ± 1 |
| A3 | 30 ± 1 | 36 ± 1 | B8 | 33 ± 2 | 34 ± 1 |
| A4 | 38 ± 1 | 35 ± 1 | C1 | 36 ± 1 | 38 ± 1 |
| A5 | 24 ± 1 | 36 ± 1 | C2 | 33 ± 1 | 39 ± 1 |
| A6 | 12 ± 1 | 36 ± 1 | C3 | 46 ± 1 | 38 ± 1 |
| A7 | 46 ± 1 | 33 ± 1 | C4 | 40 ± 1 | 38 ± 1 |
| A8 | 46 ± 1 | 37 ± 1 | C5 | 26 ± 1 | 40 ± 1 |
| A9 | 33 ± 1 | 36 ± 1 | C6 | 42 ± 1 | 38 ± 1 |
| B1 | 34 ± 1 | 34 ± 1 | C7 | 31 ± 1 | 39 ± 1 |
| B2 | 29 ± 1 | 35 ± 1 | C8 | 40 ± 1 | 38 ± 1 |
| B3 | 34 ± 1 | 35 ± 1 | C9 | 40 ± 1 | 40 ± 1 |
| B4 | 34 ± 1 | 34 ± 1 | C10 | 41 ± 1 | 40 ± 1 |
| B5 | 54 ± 1 | 37 ± 1 | C11 | 62 ± 1 | 44 ± 1 |
| notopterolc | 45 ± 1 | 30 ± 1 | LY2811376d | 52 ± 1 | inactive |
| staurosporinee | inactive | 62 ± 1 |
a
Inhibition percentage of hBACE1 at 20 μM.
b
Inhibition percentage of hGSK3β at 10 μM.
c
The concentration of notopterol for hBACE1 is 20 μM, and for hGSK3β is 10 μM.
d
The concentration of LY2811376 is 5.0 μM.
e
The concentration of staurosporine is 1.0 μM.