Table 1.
Entry | No | Structure | GIVA cPLA2 | GVIA iPLA2 | GV sPLA2 | ClogP | ||
---|---|---|---|---|---|---|---|---|
% Inhibitiona | X I(50) | % Inhibitiona | X I(50) | % Inhibitiona | ||||
1 | 10e | 68.2 ± 2.7 | 69.4 ± 12.2 | 27.5 ± 0.9 | 6.51 | |||
2 | 12e | 78.4 ± 3.5 | <25 | <25 | 5.63 | |||
3 | 17a | >95 | 0.00008 ± 0.00001 | <25 | <25 | 6.76 | ||
4 | 20 | <25 | <25 | 41.0 ± 0.2 | 6.82 | |||
5 | 17b | >95 | 0.00289 ± 0.00043 | <25 | 52.6 ± 5.3 | 5.46 | ||
6 | 16c | <25 | <25 | <25 | 4.58 | |||
7 | 19 | 27.3 ± 4.8 | <25 | <25 | 3.87 | |||
8 | 17d | >95 | 0.00068 ± 0.00007 | <25 | <25 | 4.78 | ||
9 | 17e | > 95 | 0.00007 ± 0.00001 | 25 | <25 | 6.68 | ||
10 | 17f | > 95 | 0.000078 ± 0.00001 | 65 ± 3.4 | <25 | 4.70 | ||
11 | 17g | > 95 | 0.0065 ± 0.002 | 84 ± 1.5 | <25 | 4.25 | ||
12 | 17h | > 95 | 0.0010 ± 0.0003 | 94 ± 1.4 | <25 | 4.17 | ||
13 | 10a | <25 | 72 ± 4 | <25 | ||||
14 | 10b | 55 ± 4.0 | > 95 | 0.0052 ± 0.0007 | <25 | 3.81 | ||
15 | 4 | >95 | 0.00008 ± 0.000005c | 8.50 |
a% Inhibition at 0.091 mole fraction of each inhibitor. bIC50 4.3 nM in a vesicle assay32.