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.
Measuring Kinase Inhibitor Residence Times with the Transcreener® ADP2 FP Assay provides a protocol, experimental examples, and data analysis guidelines for using the Transcreener® ADP2 FP Kinase Assay to determine dissociation rates and residence times for kinase inhibitors using simple HTS-compatible methods.
In Measuring Phosphodiesterase Inhibitor Residence Times with the Transcreener® AMP2/GMP2 FP Assay, BellBrook Labs scientist, Meera Kumar, used a jump-dilution method with the Transcreener® AMP2/GMP2 FP Assay to determine the residence times for PDE inhibitors.
- Webinar: View the Webinar or Download the Slides from our Kinase Inhibitor Residence Time webinar
- Blog Post: Tuning Kinase Drug Residence Times for Reversible Covalent Inhibitors posted June 30, 2015
- Poster: Determination of Drug Residence Time in an HTS Format using Kinetic Analysis with the Transcreener® ADP2 Assay (DOT 2015)