State-of-the-art NanoTemper biophysical instruments – utilising the techniques of MST and Temperature Related Intensity Change (TRIC) – are at the core of Domainex’s fragment screening platform FragmentBuilder. We also use these instruments for screening and characterising compounds arising from our LeadBuilder virtual screens and subsequently through lead optimisation campaigns.
In our hands MST/TRIC is a very rapid and cost-effective approach to undertaking medium throughput compound screening. We take great care to perform high-throughput buffer screens to deliver optimised assays in a fast and efficient manner.
Our G9a case study demonstrates how we successfully used MicroScale Thermophoresis to screen a sub-set of our fragment library against the lysine methyl transferase, G9a, with a hit rate of 5.3 %. By using a saturating concentration of SAM, we ensured that the co-factor binding pocket was not available for fragment binding, and so we specifically identified substrate-competitive hits.
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