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 (k_on) and dissociate (k_off) 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 k_on and k_off 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