Analyzing Kinase Inhibitor Residence Times using the Transcreener ADP Assay

Analysis of inhibitor residence times is increasingly being incorporated into lead development efforts because longer engagement with the target can result in improved efficacy, increased therapeutic window and reduced side effects. Though residence time can be determined using immobilized ligand methods such surface plasmon resonance, conjugation of drugs can affect their binding. In this webinar, we described a “jump dilution” approach for measuring residence time for protein kinase inhibitor drugs using the Transcreener® ADP Kinase Assay to continuously monitor the recovery of enzyme activity as the inhibitor compound dissociates from the kinase. A longer residence time causes a slower recovery of activity. Transcreener is the only kinase assay method that allows direct, continuous detection of ADP formation, enabling facile incorporation of residence time and other kinetic measurements into routine secondary screening. The one-hour webinar covers: How the Transcreener® HTS platform enables direct, homogenous detection of ADP and other nucleotides. An overview of drug residence times as a lead development parameter. How to employ the jump dilution method to measure kinase inhibitor dissociation rates using the Transcreener® ADP assay. Data analysis considerations and methods.