Table 4 Inhibition of rPpAChE F290V and F331W mutants by different classes of AChE inhibitors
Compound | IC50 (F331W), nM (95% CI) | RR F331W | IC50 (OPR), nM F290V (95% CI) | aRR F290V | RR G119S | |
|---|---|---|---|---|---|---|
Acylation site inhibitors | ||||||
Eserine | 85 (68–105) | 17 | 12 (9–16) | 9.2 | 27 | |
Propoxur | 1874 (2399–2510) | 13 | 17,420 (13,020–23,310) | 405 | 19,213 | |
Carbofuran | 644 (450–921) | 29 | 2897 (2347–3576) | 93 | 5167 | |
1 | 8678 (668–11,280) | 271 | 2447 (1750–3423) | 129 | 16,914 | |
2 | 845 (651–1,095) | 42 | 1884 (1584–2240) | 331 | 3419 | |
3 | 392 (327–470) | 25 | 195 (148–257) | 31 | 18 | |
4 | 1679 (1394–2022) | 44 | 434 (329–572) | 3.5 | 64 | |
5 | 6438 (5206–7961) | 29 | 1,286 (1029–1607) | 16 | 28 | |
Peripheral site inhibitors | ||||||
Tubocurarine | 160,800 (99,730–259,200) | 6.7 | 26,040 (21,770–31,140) | 1 | 4.6 | |
Ethidium bromide | 14,200 (10,220–19,730) | 1.2 | 2969 (2419–3643) | 0.2 | 0.4 | |
Bivalent inhibitor | ||||||
Donepezil | 253 (181–354) | 4 | 552 (404–753) | 9.7 | 5 | |