Kinase Binding Assays for inactive or low-activity kinases and for determining Structure-Activity Relationships (SAR)

With the discovery of Gleevec® as an inhibitor of mutant Abl kinase, there is an increasing need for a technology that allows screening of mutant kinases and low-activity kinases. DiscoveRx HitHunter Kinase Binding Assays provide a unique platform to address these previously intractable kinase targets. HitHunter Kinase Binding Assays use synthetic probes (ED-inhibitor) that bind to the ATP binding pocket of active or unactive kinases. This unique assay addresses a key need in the industry for a simple solution that effectively measures inhibitor binding, even without active enzyme.

• Non-radioactive
• Gain-of-signal readout
• Ready-to-go assays available for p38, c-Kit/Src/Abl, Lck, and PKC/GSK3alpha/CamKII
• Custom labeling and binding profiling services are also available

These simple competitive binding assays are ideal for low-activity kinases where a functional assays is not feasible. In addition they can aid in Structure Activity Relationship programs where potential drug leads can be ranked by measuring relative binding of known kinase inhibitors against the lead compound and analogs.

Click on the article webpage to view an evaluation of the technology by Astra Zeneca.