Table 3 Inhibition of rPpAChE1 and rPpAChE1-G119S by different classes of AChE inhibitors
Compound | Inhibitor class | Wild type rPpAChE1 aIC50 (95% CI) | G119S rPpAChE1 aIC50 (95% CI) | cRR |
|---|---|---|---|---|
Paraoxon | Acylation site | 290 | 380,000 | 1310 |
Maloxon | Acylation site | 44 | 20,000 | 455 |
Eserine | Acylation site | 3.2 (2.6–4.0) | 86 (73–102) | 27 |
Propoxur | Acylation site | 220 (147–329) | 4227,000 (–)b | 19,213 |
Carbofuran | Acylation site | 24 (17–33) | 124,000 (–) | 5167 |
1 | Acylation site | 14 (10–19) | 236,800 (7404–7575,000) | 16,914 |
2 | Acylation site | 36 (28–48) | 123,100 (–) | 3419 |
3 | Acylation site | 13 (9.4–19) | 235 (164–336) | 18 |
4 | Acylation site | 75 (36–152) | 4775 (3,048–7482) | 64 |
5 | Acylation site | 76 (50–117) | 2128 (1,267–3573) | 28 |
Tacrine | Choline binding site | 67 (56–81) | 388 (318–473) | 5.8 |
6 | Bivalent | 0.42 (0.35–0.52) | 2.7 (2.3–3.2) | 6.4 |
7 | Bivalent | 14 (13–15) | 35 (28–42) | 2.5 |
Donepezil | Bivalent | 52 (39–70) | 262 (202–341) | 5 |
Tubocurarine | Peripheral site | 143,200 (94,630–216,700) | 661,800 (290,000–1511,000) | 4.6 |
Ethidium bromide | Peripheral site | 17,100 (13,890–21,060) | 6433 (4380–9448) | 0.4 |