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3rd February 2014 @ 10:59

Data obtained at the outset of Series 4 included potency and PK data, but no formal record of how the data were obtained - i.e. details of assays. Paul Willis wrote on 3rd Feb 2014 by email to provide the following methods:

 

1. Parasite assay - In Vitro EC50 (uM) (Erythrocyte assay - NF54 with 3H-Hypoxanthine at 72hr time point)

 

2. Rat and human liver microsomes - Test compound is incubated with pooled human (or rat) liver microsomes in 100 mM phosphate buffer (pH 7.4) at 37°C in the presence of NADP cofactor. The incubation volume is 0.1 mL. Test compounds are tested at 1 mM.

 

These assays will need to be linked with the data upon upload to ChEMBL following assignment of OSM numbers.

 

Inherited Data on Series 4 Amides

Collected Amides in the TP Series (Triazolopyrazines, Series 4)

A New Triazolopyrazine Series for OSM - Series 4

MMV triazolopyrazine data

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