TABLE 2.

IC₅₀ values and K_i values for diphenylurea derivatives containing a sulfonic acid group

Walter Reed compound	Plasmepsin inhibition (Ki [μM])		IC50 (μg/ml)				Protease selectivity (Ki [μM])
			P. falciparum drug susceptibility		Mammalian cell toxicity
	P. falciparum	P. vivax	Strain W2	Strain D6	Neuronal cells	Macrophage cells	Human cathepsin D
WR100392	0.09	0.08	16	30	15	10	3.5
WR101653	0.12	0.43	20	21	78	65	35
WR100484	0.20	0.05	6.6	7.1	43	39	3.3
WR103412	0.05	0.25	15	20	36	22	83
WR100081	0.18	0.08	6.5	13	27	72	26
WR099444	0.68	0.15	16	25	30	>100	16
WR099445	0.19	0.27	20	26	73	>100	191
WR100080	0.06	0.06	16	23	6.2	4.0	2.7
WR100400	0.11	0.59	21	20	27	43	157