Automated Compound Profiling Applications for the Assessment of Lead Compound Off-target Effects

Profiling lead compounds against other enzymes within the same target class has become increasingly important in the drug discovery process. Drugs must demonstrate specificity for the target enzyme, or run the risk of generating adverse health effects among patients. This process involves generating IC50 or EC50M values with a variety of enzymes in order to determine specificity. In this application note profiling applications for two important drug target classes, kinases and histone deacetylases, using an 8-channel liquid handler and hybrid multi-mode microplate reader are demonstrated. Assay optimization and profiling data demonstrate the validity of each automated process.