Sphingosine Kinase 1 Inhibitor

Kinase Inhibitor Selectivity Profiling Using Differential Scanning Fluorimetry

and widely used approach is the direct measurement of the effect of the added ligands on its activity. A variety of enzymatic assay formats have been successfully applied for inhibitor screening of protein kinases. However, enzymatic assays require an active

Fluorescence Labels in Kinases: A High-Throughput Kinase Binding Assay for the Identification of DFG-Out Binding Ligands

-binding site contributes to poor inhibitor selectivity, issues which have particularly hampered the development of novel kinase inhibitors. We developed a high-throughput screening technology that can discriminate for inhibitors which stabilize

High-Throughput Automated Confocal Microscopy Imaging Screen of a Kinase-Focused Library to Identify p38 Mitogen-Activated Protein Kinase Inhibitors U

generation through preclinical candidate selection. In this chapter we describe the development, validation, and implementation of an HCS assay to screen compounds from a kinase-focused small-molecule library to identify inhibitors of the p38 pathway using