A novel approach for the discovery of chemically diverse anti-malarial compounds targeting the Plasmodium falciparum Coenzyme A synthesis pathway

Table 1 Overview of compound IC ₅₀ against Plasmodium falciparum and HEK293 cells

	Compound ID	IC50 [μM]			IC50 [μM]			SI
		(3D7; n = 3)			(HEK293; n = 3)
		Mean	+ SEM	- SEM	Mean	+ SEM	- SEM
80% rescue at 2 μM	MMV665820/5534045	0.58	0.16	0.13	3.6	0.47	0.42	6.2
	MMV000304/Amb636705	1.21	0.30	0.24	1.00	0.33	0.25	0.8
	Amb4317088	1.23	0.12	0.11	2.33	0.24	0.22	1.9
	STK 668036	1.30	0.16	0.14	11.92	2.59	2.13	9.2
	Amb2368822/(MMV665980)	6.31	2.08	1.56	> 40			> 6.3
	Amb1541406	85% inhibition at 40 μM			> 40			ND
50% rescue at 2 μM	STK 740987	0.38	0.11	0.09	> 40			> 105
80% rescue at ~ IC₈₀	Amb180780	0.12	0.03	0.02	~ 40			~ 333
	MMV011438/STK039514	0.43	0.05	0.05	> 40			> 93
	MMV000570/C614-0191	0.74	0.08	0.07	~ 40			~ 54
50% rescue at ~ IC₈₀	SPB03400	0.45	0.09	0.07	> 40			89
	Amb3377585	0.15	0.02	0.02	2.75	0.36	0.32	18
Not con-firmed	5964083	0.50	0.09	0.08	> 40			> 80

The selectivity index (SI) of the compounds was calculated by dividing the HEK293 IC₅₀ value by the P. falciparum IC₅₀ value.
SEM: standard error of mean.
ND: not determined, since no IC₅₀ values could be obtained.

ISSN: 1475-2875