Enzymatic assays for fragment-based screening using enthalpy arrays

• Drug Discovery Chemistry: Fragment-based Techniques

Enthalpy arrays are arrays of nanocalorimeters that enable measurements of the thermodynamics of molecular interactions using small sample volumes and short measurement times. The technology provdes a label-free assay to determine the kinetic parameters of enzymatic reactions and the mechanism of action of inhibitors. In this talk we will discuss the application of enthalpy arrays to confirm and rank fragment hits based on their ligand efficiencies.

citation

Recht, M. I. ; Torres, F. ; De Bruyker, D. ; Bell, A. G. ; McRee, D.; Bruce, R. H. Enzymatic assays for fragment-based screening using enthalpy arrays. Drug Discovery Chemistry: Fragment-based Techniques; 2009 April 6-8; San Diego, CA.