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24th April 2013 @ 01:40

Biological evaluation of OSM-S-117 through 138 (also OSM-S-107) performed in Vicky Avery's lab by Sabine Fletcher.


Data for previous OSM-S compounds can be found here - OSM Compound List


Unfortunately only two (OSM-S- 137 and 138) were active on 3D7.

The summary also contains information about the solubility: several of the compounds turned opaque when diluted down to 4% DMSO, which suggests poor solubility in this condition. I made sure to mix the compounds very well before the final 1:10 dilution step in the assay plate.

One compound (OSM-S-134) did not dissolve well in 100% DMSO. It still contained many needle-like crystals after shaking over night, which means that we do not know the actual concentration of the dissolved compound in the assay. As tested here, it was completely inactive.

 

Click for larger image

Click for larger image


2013_04_23 summary report Sydney cpds batch 5+6.xlsx
2013_04_23 Sydney batch 5.pdf
2013_04_23 Sydney batch 6.pdf

Depictions of Data including cLogP values and comments on solubility:

Activities of hit vs simple analogs

Hit compound vs simple analogs

Variation of amine to morpholine

fig2.png

Variation in amine component

Variations in Amine

Comparison with known other TCMDC hits

Comparisons with TCMDC compounds

 



Linked Posts
Attached Files
2013_04_23 summary report Sydney cpds batch 5+6.xlsx
2013_04_23 Sydney batch 6.pdf
2013_04_23 Sydney batch 5.pdf
testing_Mar13_data_page1.png
testing_Mar13_data_page2.png
Variations in Amine
Comparisons with TCMDC compounds
Hit compound vs simple analogs
fig2.png