What improvements were made to the SARS-CoV-2 Mpro high-throughput screening (HTS) assay?

Label:chem

Topic
Previous high-throughput screens (HTS) for Mpro inhibitors have relied on FRET-based peptide substrates to monitor protease activity. However, these substrates have shown inconsistent findings regarding the identification of potential Mpro inhibitors, highlighting the need for an improved assay with better performance and consistency.
Answer
The study developed an improved 5-carboxyfluorescein (FAM)-based FRET substrate that is better suited for HTS. This substrate is less susceptible to interference and false positives compared to existing substrates. The improved substrate provides a higher signal dynamic range and a better Z0-factor, making it more effective for identifying potential Mpro inhibitors.
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