As part of our hit-to-lead/lead optimization services we offer, in collaboration with Carna Biosciences, a kinase profiling service for the discovery and characterization of kinase inhibitors. Through this profiling service, our customers gain access to more than 150 active protein kinases - representing all major branches of the human kinome. We ensure the rapid and reliable profiling of hit molecules by using robust, validated assays that have been well characterized with known kinase inhibitors. Additionally, we can reliably determine IC50 values of your hits against the full set of kinases using state-of-the-art assays.

Successful profiling early in the drug discovery process speeds up the later stages of development and ensures that only those compounds with the most promising profile are further optimized. Combined with our medicinal chemistry services, this profiling service results in a better understanding of your compounds’ SAR.

 

Our kinase profiling service adds value to these stages of drug development:
• Hit finding
• Selectivity profiling
• Lead identification and optimization
• Mode-of-action studies

 

Advantages

 

Comprehensive
With more than 150 kinases, all major branches of the human kinome represented

 

Minimal cross reactivity
Highly purified, active kinases with negligible contaminating kinase activity

 

Flexible
Robust (ELISA, IMAP) assay platforms

Precise
Quantitative IC50 values to optimize potency and selectivity of hit and lead molecules

 

Rapid
Less than three week turnaround time complements medicinal chemistry timelines

 

Reliable
Data performed in triplicate on validated kinases to ensure reliable results

 

 

Offering
A variety of kinase panels are available, including:

• TK screening panel - 20 tyrosine kinases
• Comprehensive TK panel - 77 tyrosine kinases
• STK screening panel - 30 serine/threonine kinases
• MAPK cascade panel - 30 MAPK pathway kinases
• Select panel - customized kinase panel
• Complete panel - more than 150 kinases

We provide the following profile services, primarily using either the IMAP or ELISA format:

• Screening at one concentration in triplicate for a panel of kinases
• IC50 measurements performed in triplicate using at least six concentrations
• ATP and/or substrate competition; Ki determination
• MAPK cascade panel - 30 MAPK pathway kinases

 

 

Contact us to learn more about our kinase profiling service.

BioFocus® is a registered trademark of Galapagos NV and/or its affiliates