|
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
|
- aIC50 = inhibitor concentration producing 50% inhibition of activity (in nM), where (95% CI) = 95% confidence interval.
- b(−−) denotes wide confidence limits from incomplete inhibition of rPpAChE1-G119S.
