Table 1.

Summary of in vitro and in vivo PfA-M1 inhibitors properties

	Structure	Ki rPfA M1 (nM)	Ki rPfA M17 (nM)	IC50 in vitro (µM)	In vitro strain	In vivo model	In vivo parasitaemia reduction (%)	References
CHR-2863		1413.41 ± 123.74	75.96 ± 22.86	0.37	3D7	P. c. chabaudi/C57/BL6j	43% (25 mg/kg)	[46]
				0.376	K1
							52% (50 mg/kg)
							66% (100–50 mg/kg)
Bestatin		1673.00 ± 238.05	613 ± 201.33	5	3D7	P. c. chabaudi/8 weeks old C57/BL6j	34% at 100 mg/kg, twice a day	[46, 47]
				12–21	Dd2
			25 ± 1.2	11–15	D10
				8–14	3D7
Malarone		NA	NA	–	–	P. c. chabaudi/C57/BL6j	100% at 14 mg/kg	[46]
Chloroquine		–	–	10.1 ± 3.8	3D7	P. c. chabaudi/8 weeks old C57BL/6j	85% at 5 mg/kg	[47]
				138.0 ± 21.1	FcB1
Compound 4		79	13.2 ± 0.5	20–40	Dd2	P. c. chabaudi/8 weeks old C57BL/6j	92% at 100 mg/kg, twice a day	[31, 47]
				46–75	D10
				24–62	3D7
T5		50	> 100 µM	11.2 ± 3.4	3D7	P. c. chabaudi/BALB/c	44 and 40% at 12 and 24 mg/kg/day	this work
				6.5 ± 2.4	FcB1

NA data not available