Skip to main content
. Author manuscript; available in PMC: 2020 Jul 12.
Published in final edited form as: J Med Chem. 2020 May 26;63(11):6179–6202. doi: 10.1021/acs.jmedchem.0c00539
T31 T111 (26)
In vitro IC50 vs. blood-stage P. falciparum D6/Tm90-C2B: 0.022/228 0.028/5.6
In vivo ED50/ED90 (mg/kg/d) vs. blood-stage P. yoelii: 1.0/1.6 0.045/0.098
In vivo cure (mg/kg×4 days) vs. blood-stage P. yoelii: 80 10
In vivo full protection/cure (mg/kg×3 days) vs. liver-stage P. berghei: 4.0 4.0
In vitro metabolic stability vs. human/mouse (t1/2, min): 12/21 >60/50
In vivo PK (mouse, po): plasma/liver half-life (t1/2, h): 6.00/4.63 23.6/14.0
hERG (% inhibition at 10 μM): 57 5.7
hERG (% inhibition at 10 μM): 57 5.7