Methods for kinetic evaluation of reversible covalent inhibitors from time-dependent IC<sub>50</sub> data
Lavleen Mader, Jeffrey W. Keillor
Abstract
data. The application of these new methods is demonstrated by the evaluation of a known inhibitor, saxagliptin, providing results consistent with those obtained by other known methods. This work introduces two new practical methods of evaluation for time-dependent reversible covalent inhibitors, allowing for rigorous characterization to enable the fine-tuning of their binding and reactivity.
Topics & Concepts
Covalent bondChemistryIC50Enzyme inhibitionCombinatorial chemistryEnzymeBiochemistryOrganic chemistryIn vitroClick Chemistry and ApplicationsChemistry and Chemical EngineeringChemical Synthesis and Analysis