Table 3.
Apparent human AChE inhibition constant (Ki and Ki′) values, equine butyrylcholinesterase (BChE) inhibitory activity and selectivity for AChE for the most active compounds.
Compound | Human AChE | Equine BChE | Selectivity | |
---|---|---|---|---|
Ki /µM | Ki′ /µM | IC50 /µM a | for AchE b | |
7 | 40 | 59 | 108 ± 18 | 2.0 |
10 | 31 | 47 | 59 ± 12 | 1.4 |
13 | 113 | 165 | 71 ± 14 | 0.8 |
14 | 56 | 92 | 81 ± 18 | 1.1 |
a Values are expressed as mean ± SEM; b Selectivity is defined as IC50 (BChE)/IC50 (AChE); values for IC50 (AChE) are shown in Table 2.