Using Biophysical Methods to Optimize Compound Residence Time
Geoffrey A. Holdgate, Philip B. Rawlins, Michał Biśta, Christopher J. Stubbs · 2017
Incorporating binding kinetics into the considerations for compound optimization has gained interest recently. Biophysical methods are well placed to deliver kinetic data on target–compound interactions. This chapter will highlight the use of biophysical methods to measure binding kinetics, as well as discuss the factors affecting binding kinetics and the rationale for attempting to integrate information derived from kinetic studies in modifying kinetic profiles during lead optimization.