Skip to main content
. Author manuscript; available in PMC: 2012 Oct 12.
Published in final edited form as: Chem Rev. 2011 Sep 12;111(10):6130–6185. doi: 10.1021/cr200085w

Table 11.

Comparison of GIIA and Group IB PLA2 Inhibition by Varespladib and Analogues Using the Chromogenic Assay

graphic file with name nihms324958t9.jpg
Compound R1 R2 IC50 (µM)
hGIIA PLA2 hGIB PLA2 pGIB PLA2
23a C6H5CH2 CH3 0.011 ± 0.004 0.761 0.015
23b 2-(C6H5)C6H4CH2 CH3 0.006 ± 0.001 0.364 0.097
23c 3-(C6H5)C6H4CH2 CH3 0.009 ± 0.001 0.57 0.007
23d 1-naphthylCH2 CH3 0.009 ± 0.004 1.2
23e n-C8H17 CH3 0.008 ± 0.003 0.78
23f 2-(C6H5CH2)C6H4CH2 CH2CH3 0.004 ± 0.001 0.062
23g 3-ClC6H4CH2 CH2CH3 0.007 ± 0.002 0.390 0.003
24 C6H5CH2 CH2CH3 0.009 ± 0.001 0.228 0.048