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The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

Atli Thorarensen, Paul Balbo, Mary Ellen Banker, Robert Czerwiński, Max Kühn, Tristan S. Maurer, Jean‐Baptiste Telliez, Fabien Vincent, Arthur J. Wittwer

2020Bioorganic & Medicinal Chemistry66 citationsDOI

Topics & Concepts

ChemistryCovalent bondDrug discoveryIC50EnzymeSubstrate (aquarium)Combinatorial chemistrySmall moleculeComputational biologyBiochemistryIn vitroOrganic chemistryOceanographyBiologyGeologyClick Chemistry and ApplicationsMonoclonal and Polyclonal Antibodies ResearchProtein Degradation and Inhibitors
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization | Litcius