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24th April 2014 @ 23:33

(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.

MMV669844 and MMV670944

(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)

Attached Files
4th April 2014 @ 03:26

hERG data were obtained by MMV from Essen Bioscences. Report attached.

Summary:

MMV669844 and MMV670944 were both active in this assay with pIC50 values of 5.2 and 5.6.

And solubility issues were observed for compound MMV669844 at 33 uM in the final assay plate.

 

MMV669844 MMV670944 OSM-S-175

Preparation of OSM-S-175

Series 4 wiki

Data discussed briefly during OSM Online Project Meeting 7 (27th March 2014)

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Attached Files