Table 3. Characterization of inhibitors.
| IC 50-values of reversible inhibitors, μM (95% CI) | ki-values of covalent inhibitors, μM-1 min-1 (95% CI) | ||||||
|---|---|---|---|---|---|---|---|
| Enzyme | Donepezil | C7653 | C5685R | C5685S | Ethopropazine | Propoxur | Eserine |
| AgAChE1 | 0.24 (0.19–0.30) | 0.44 (0.29–0.67) | >30 | >30 | 8.3 (5.8–11.8) | 1.11 (1.02–1.21) | 27.3 (23.8–30.8) |
| AaAChE1 | 0.28 (0.18–0.43) | 0.36 (0.26–0.49) | >30 | >30 | 4.6 (3.98–5.3) | 1.20 (1.05–1.35) | 24.8 (18.1–31.5) |
| hAChE | 0.008 (0.0071–0.0085) | 0.36 | 1.3** | 1.4** | ~1 mM | 0.081 (0.071–0.092) | 2.66 (2.28–3.05) |
| mAChE | 0.007 (0.0063–0.008) | 0.2* | 0.7** | 0.7** | ~1 mM | 0.092 (0.068–0.117) | 1.36 (1.15–1.56) |
| AgAChE1-G119S | 0.31 (0.25–0.38) | 1.3 (0.8–2) | >30 | >30 | ~1 mM | n. d. | 1.18 (0.63–1.72) |