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Table 1 Inhibition of rPpAChE1 and rPpAChE1-G119S by different classes of AChE inhibitors

From: Acetylcholinesterase of the sand fly, Phlebotomus papatasi (Scopoli): construction, expression and biochemical properties of the G119S orthologous mutant

Compound Inhibitor class Wild type rPpAChE1 G119S rPpAChE1 Resistance Ratio
aIC50(95% CI) aIC50(95% CI)
Paraoxon acylation site 2.863 (1.862–4.401) 3,819 (3,205–4,550) 1336
Malaoxon acylation site 4.361 (3.184–5.972) 1,972 (1,665–2,340) 452
Eserine acylation site 3.2 (2.6–4.0) 86 (73–102) 27
Propoxur acylation site 220 (147–329) 4,227,000 (−−)b 19,213
Carbofuran acylation site 24 (17–33) 124,000 (−−) 5,200
1 acylation site 14 (10–19) 236,800 (7,404–7,575,000) 17,000
2 acylation site 36 (28–48) 123,100 (−−) 3,400
3 acylation site 13 (9.4–19) 235 (164–336) 18
4 acylation site 75 (36–152) 4,775 (3,048–7,482) 64
5 acylation site 76 (50–117) 2,128 (1,267–3,573) 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) 5.0
Tubocurarine peripheral site 143,200 (94,630–216,700) 661,800 (290,000–1,511,000) 4.6
Ethidium Bromide peripheral site 17,100 (13,890–21,060) 6,433 (4,380–9,448) 0.4
  1. aIC50 = inhibitor concentration producing 50% inhibition of activity (in nM), where (95% CI) = 95% confidence interval.
  2. b(−−) denotes wide confidence limits from incomplete inhibition of rPpAChE1-G119S.