Integrated Strategic Design and In Situ Click Chemistry Approach to Rapid Discovery of Novel Potent Covalent TEAD Inhibitors

Key Points

• This research aims to develop a rapid method for discovering potent TEAD inhibitors using integrated design strategies.
• Utilized structure-based design and CuAAC (copper-catalyzed azide-alkyne cycloaddition) for synthesis.
• Implemented in situ screening techniques to evaluate the effectiveness of the inhibitors.
• Focused on targets with structurally defined pockets to optimize discovery efforts.
• Successfully identified novel TEAD inhibitors through the integrated approach.
• Demonstrated increased efficiency in the discovery process compared to traditional methods.

Abstract