Kinases in Drug Discovery
Experience and unmatched expertise in kinase drug discovery.Drug discovery efforts are usually centered on a single target against which compounds are optimized for therapeutic efficacy. However, developing a selective kinase inhibitor is particularly challenging, because of conserved active sites and high structural homology between kinases. Broad profiling, for many, has become a requirement of new kinase inhibitor programs for better understanding structure/activity relationships, helping to avoid targets with toxic liabilities, and, ultimately, to select better drug candidates. The last five years have seen eight anti-cancer kinase inhibitors receiving FDA approval, increasing recognition of kinases as a vital drug target class.
Through the combined expertise of Cerep, Panlabs, KinaseProfiler™, and SignalProfiler™ services, Eurofins offers an unmatched portfolio of biochemical and cellular kinase assays.
Figure 1. Visualization of selectivity and potency of p38 and JNK inhibitors.
p38 (top panel) and three JNK (bottom panel) inhibitors were profiled against 234 wild-type human receptors by activity assays using Eurofins's KinaseProfiler™ service as part of a screen of 158 kinase inhibitors published in Biochemical Journal (2013 Apr 15;451(2):313-28). Lines stretching to the perimeter indicate interactions that have the highest potency.
*The guarantee must be requested at the time of ordering and is available for most projects, including KinaseProfiler™, IC50 Profiler™, and PhosphataseProfiler™. Eligible projects are activated each Friday and data reports are delivered on or before the following Friday.
**Services mentioned in report for Cerep, EMD Millipore and Ricercia Biosciences are now operated by Eurofins