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. 2017 Aug 1;7:7025. doi: 10.1038/s41598-017-07330-5

Table 1.

In vitro inhibitory potency and selectivity of 2-oxoesters.

Entry No Structure GIVA cPLA2 GVIA iPLA2 GV sPLA2 ClogP
% Inhibitiona X I(50) % Inhibitiona X I(50) % Inhibitiona
1 10e graphic file with name 41598_2017_7330_Figa_HTML.gif 68.2 ± 2.7 69.4 ± 12.2 27.5 ± 0.9 6.51
2 12e graphic file with name 41598_2017_7330_Figb_HTML.gif 78.4 ± 3.5 <25 <25 5.63
3 17a graphic file with name 41598_2017_7330_Figc_HTML.gif >95 0.00008 ± 0.00001 <25 <25 6.76
4 20 graphic file with name 41598_2017_7330_Figd_HTML.gif <25 <25 41.0 ± 0.2 6.82
5 17b graphic file with name 41598_2017_7330_Fige_HTML.gif >95 0.00289 ± 0.00043 <25 52.6 ± 5.3 5.46
6 16c graphic file with name 41598_2017_7330_Figf_HTML.gif <25 <25 <25 4.58
7 19 graphic file with name 41598_2017_7330_Figg_HTML.gif 27.3 ± 4.8 <25 <25 3.87
8 17d graphic file with name 41598_2017_7330_Figh_HTML.gif >95 0.00068 ± 0.00007 <25 <25 4.78
9 17e graphic file with name 41598_2017_7330_Figi_HTML.gif  > 95 0.00007 ± 0.00001 25 <25 6.68
10 17f graphic file with name 41598_2017_7330_Figj_HTML.gif  > 95 0.000078 ± 0.00001 65 ± 3.4 <25 4.70
11 17g graphic file with name 41598_2017_7330_Figk_HTML.gif  > 95 0.0065 ± 0.002 84 ± 1.5 <25 4.25
12 17h graphic file with name 41598_2017_7330_Figl_HTML.gif  > 95 0.0010 ± 0.0003 94 ± 1.4 <25 4.17
13 10a graphic file with name 41598_2017_7330_Figm_HTML.gif <25 72 ± 4 <25
14 10b graphic file with name 41598_2017_7330_Fign_HTML.gif 55 ± 4.0  > 95 0.0052 ± 0.0007 <25 3.81
15 4 graphic file with name 41598_2017_7330_Figo_HTML.gif >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.