Compound Structures AChE IC50 (nM)a BChE IC50 (nM)a Selectivity Index (IC50AChE/ IC50BChE)<sup>b</sup>
Group 1
1
> 3000 1149 (977.6, 1349)   Not applicable
Group 1
4
Not done 947 (735.8, 1219)   Not applicable
Group 2
6
> 3000 936.0 (824.2, 1063)   Not applicable
Group 2
10
> 3000 660.7 (495.5, 881)   Not applicable
Group 2
24
ND e 1634 (1483, 1801)   Not applicable
Group 3
39
597.5 (469.7, 760.1) > 3000   Not applicable
Group 3
40
1077 (911.3, 1272) > 3000   Not applicable
Group 3
41
292.2 (253.3, 337.1) > 3000   Not applicable
Group 5
47
224.1 (191.0, 263.0) 8.6 (6.6, 11.1)   26
Group 5
48
≈ 3000 1298 (1153, 1462)   Not applicable
Group 6
49
8.8 (6.5, 11.8) 15.2 (13.4, 17.2) 0.58
Group 6
50
40.8 (31.7, 52.6) 81.5 (62.6, 106.2) 0.50
Group 6
51
  5.6 ( ±  1.9)
Ki : 1.8 nMc
  321 ( ± 114)
Ki 36.3 nMc
0.02
Group 6
52
1175 (911.9, 1515) >3000 Not applicable
Group 6
53
869.4 (701.8, 1077) ≈ 3000 Not applicable
Group 6
54
1384 (1138, 1682) > 3000 Not applicable
Tacrine 184.1 (158.1, 210.0) 6.7 (5.7, 7.6) 27.5
Donepezil   6.2 (4.39, 7.92) 1746 (1210, 2281) 0.0036
aIC50values were determined by GraphPad Prism v4.03 from at least three independent experiments. 95% Confidence intervals are given in brackets. bRatios were obtained only for those compounds with experimentally determined IC50values. Compounds which had estimated IC50values were not considered.
Table 2: AChE and BChE inhibitory IC50values of selected compounds in Groups 1,2, 5 and 6.