OSM: hERG, IC50 uM (Essen Bioscience): IonWorks patch clamp electrophysiology. 8 point concentration-response curves were generated using 3-fold serial dilutions from the maximum final assay concentration of 33 uM.
OSM: Mice are infected intravenously with parasitized red blood cells on day 0 (2 x 107 parasitized erythrocytes per ml). Experimental mice are generally treated at 4, 24, 48, and 72 hours post-infection with an oral dose of the compound (50 mg/kg, 4-day test by Peters) and are compared to an infected control group for reduction in parasitaemia on day 4 (96 hours post-infection) as a percentage.
GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM
GSK_TCMDC: Inhibition of Plasmodium falciparum Dd2 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM
GSK_TCMDC: Inhibition Frequency Index (IFI). The number of non-kinase HTS assays where a compound showed > 50 % inhibition, expressed as a percentage of the number of such assays in which the compound was tested
ST_JUDE_LEISH: Cytotoxicity at 2uM final concentration against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro