Table 1. Inhibitor activity and selectivity of conjugates 4a (n=1), 4b (n=2), 5a (n=1), 5b (n=2) toward AChE, BChE and CaE.
Compound |
IC50±SEM (µM), n=3 |
Selectivity |
|||
IC50 AChE / |
IC50 CaE / |
||||
AChE |
BChE |
CaE |
|||
4a |
6.27 ± 0.12 |
0.835 ± 0.066 |
84.0 ± 6.7 |
7.5 |
100 |
4b |
2.29±0.18 |
0.10±0.01 |
2.82 ± 0.25 |
22.9 |
28.2 |
5a |
2.47 ± 0.07 |
0.0069 ± 0.0006 |
>100 |
360.0 |
>14500 |
5b |
0.36 ± 0.03 |
0.0064 ± 0.0006 |
33.9 ± 3.1 |
56.8 |
5300 |
Tacrine |
0.60 ± 0.05 |
0.0295 ± 0.0002 |
>100 |
20.3 |
>3400 |
BNPP |
n.a. |
n.a. |
1.80 ± 0.11 |
-* |
- |
Note: n.a. - not active; * - not determined