Inhibition of Plasmodium falciparum plasmepsin 2 using EDANS-CO-CH2-CH2-CO-ALERMFLSFP-Dap(DABCYL)OH as substrate measured after 60 mins by fluorescence assay
Inhibition of Plasmodium falciparum plasmepsin 4 using EDANS-CO-CH2-CH2-CO-ALERMFLSFP-Dap(DABCYL)OH as substrate measured after 60 mins by fluorescence assay
Selectivity ratio of IC50 for inhibition of Tracer Red binding to human ERG expressed in membranes to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7
Antimalarial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mouse assessed as inhibition of parasitemia at 3 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured on day 4 by Peter's 4 day test relative to control
Antimalarial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mouse assessed as inhibition of parasitemia at 10 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured on day 4 by Peter's 4 day test relative to control
Antimalarial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mouse assessed as inhibition of parasitemia at 30 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured on day 4 by Peter's 4 day test relative to control
Plasma concentration in NIH mouse infected with chloroquine-resistant Plasmodium chabaudi ASCQ at 3 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured 1 hr post-last dose by LC-MS analysis
Plasma concentration in NIH mouse infected with chloroquine-resistant Plasmodium chabaudi ASCQ at 10 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured 1 hr post-last dose by LC-MS analysis
Plasma concentration in NIH mouse infected with chloroquine-resistant Plasmodium chabaudi ASCQ at 30 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured 1 hr post-last dose by LC-MS analysis