Biological Evaluation of Compounds

(Data originally posted in Similarity of Series 4 Compounds to KAI407 since relevant to comparison with Novartis compound KAI407)

As part of an evaluation of the mechanism of action of OSM Series 4, two inherited compounds MMV669844 and MMV670944 were evaluated vs Pb liver schizonts. The Novartis imidazopyrazines are known to be active vs. PI4K, not PfATP4, and are active against liver schizonts. The two Series 4 triazolopyrazines showed weak activity (data attached), i.e. at a level lower than would be expected based on their blood potency. These data support the hypothesis that the Novartis compounds and OSM Series 4 have distinct mechanisms of action.

(These are the same compounds as those evaluated for hERG hERG Data for MMV669844 and MMV670944)

(Data originally obtained from Paul Willis Feb 1st 2014)

(Post - MHT)