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OpenSourceMalaria / Series5

Open Source Malaria Series Five. 1-substituted isoquinolines
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Discrepancy with literature potencies #6

Open edwintse opened 3 years ago

edwintse commented 3 years ago

We previously sent the compounds from Helen for in vitro assay at Dundee (#5) and all compounds came back as inactive against P. falciparum. This was a bit surprising considering 2 of the compounds had reported uM activity in the literature (10.1039/C3RA46791K). I ended up resynthesising these 2 reported actives and had them retested. We've gotten the results back and the potencies of these are in line with Helen's compounds (i.e. inactive). Untitled Wiley-18

I'm not really too sure where to go from here? It seems like this series won't be too fruitful based on this

MFernflower commented 3 years ago

I'm also a bit curious whether these S5 compounds are PAINS?!?!?!?

@edwintse @drc007

MFernflower commented 3 years ago

@edwintse see issue #3 aswell