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 BChE

IC50 CaE /
IC50 BChE

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