Binding Kinetics: High Throughput Assay for Kinase Inhibitors

Drug development is a costly and lengthy process with high attrition rates. More than half of the drug candidates entering Phase 2 clinical trials fail, mainly because of lack of effectiveness.

Efficacy and safety of drug candidates is dependent on their binding kinetics – how fast they associate (kon) and dissociate (koff) from their targets, and for how long they can occupy them. Ideally, these kinetic parameters should be determined during the preclinical stages of development, creating the need for high-throughput methods to profile hundreds of compounds in an efficient way.

Download this app note to discover:

• How kon and koff values were determined for a panel of 40 cancer drug targets against kinase inhibitors
• The relationship between binding parameters and clinical success
• A high-throughput assay that aids the selection of new drug candidates for development according to their binding properties