Identification of SARS-CoV-2 Helicase Inhibitors Part 2

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NSP13 helicase is a critical component of coronavirus replication, yet notoriously difficult to target due to its conformational dynamics. In this second part, we share how IRBM’s covalent fragment platform was applied to this enzyme. This approach led to the identification and characterization of hits using a functional assay to monitor the enzymatic activity of the target protein, binding specificity was conducted by LC/MS analysis and peptide mapping allowed the identification of the cysteine residues binding sites. A preliminary SAR of one of the hit compounds enabled the optimization of activity and binding, open prospectives for future developability. This is Part 2 of the study—if interested, do not forget to download Part 1 for the full context.