. Author manuscript; available in PMC: 2010 Oct 28.

Published in final edited form as: J Med Chem. 2008 Jul 8;51(15):4708–4714. doi: 10.1021/jm800422v

Table 4.

IC₅₀ Values of Substituted Indolizine Inhibitors against Human and Mouse sPLA2s^a




			IC₅₀ (nm)

comp	R1	R2	hGIB	mGIB	hGIIA	mGIIA	hGIID^b	mGIID	hGIIE	mGIIE	hGIIF	mGIIF	hGV	mGV	hGX	mGX
Indoxam			700±30	1000±60	60±10	150±40	>1300	>1600	10±2	35±15	>1600	>1600	100±5	170±10	>1600	900±300
16a			>1600	>1600	>1600	>1600	>1300	>1600	>1600	>1600	970±50	1100±200	>1600	>1600	>1600	>1600
16b			>1600	1200±110	30±10	>1600	>1300	>1600	90±15	410±20	>1600	>1600	>1600	>1600	>1600	>1600
16c			>1600	320±20	35±2	>1600	>1300	>1600	50±10	230±110	>1600	>1600	>1600	>1600	>1600	>1600

IC₅₀ values are reported as the mean of duplicate or triplicate analysis with standard deviations. Each compound was screened at 1660 nM and reported as >1600 nM if the inhibition was <50%.

IC₅₀ values obtained using E. coli membrane assay. Each compound was screened at 1330 nM and reported as >1300 nM if the inhibition was <50%.