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Covalent Inhibitors: How We Can Find Them in an Early Stage of a Drug Discovery Program

IRBM poster 24014, preview
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In this poster, we present IRBM’s assay cascade for identifying novel covalent pharmacophores against an undisclosed target. Using a homogeneous assay, we screen covalent fragment libraries and confirm hits through LC/MS analysis and peptide mapping. Our approach, including biochemical characterization and cell-based assays, effectively uncovers selective inhibitors targeting specific cysteine residues.

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