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Automated Compound Profiling Applications for the Assessment of Lead Compound Off-target EffectsDownload
July 01, 2011
Authors: Brad Larson, Peter Banks, Andreas Rieger, BioTek Instruments, Inc., Winooski, Vermont, USA
Profiling lead compounds against other enzymes within the same target class has become increasingly important in the drug discovery process. Drugs must demonstrate specifi city 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 specifi city. Here we demonstrate profi ling applications for two important drug target classes, kinases and histone deacetylases, using an 8-channel liquid handler and hybrid multi-mode microplate reader. Assay optimization and profiling data demonstrate the validity of each automated process.