Applications:
- Measure cellular permeability and target engagement for a test compound
- Measure cellular potency and compare with in vitro biochemical potency
- Measure irreversible mode of inhibition for a test compound
- Measure potency for a prodrug inside cells
- Screen compound sets against a specific target kinase inside cells
- Measure selectivity inside cell for a test compound by using a kinase profiling panel
Cell-based KinaseSeeker-TE™ Assays
Target engagement (TE) assays are desirable for the generation of lead candidates and chemical probes. TE assays report on the direct binding of a drug to the target protein in a complex cellular environment. Luceome offers a wide range of cell-based TE assays for kinases using our popular KinaseSeeker platform technology. These TE assays allow measurement of compound binding to their specific target kinase inside a cell. Compounds can be screened and profiled for selectivity and their potencies and compared to in vitro assays.
In the Cell-based KinaseSeeker-TE™ assay, the target kinase is expressed as a fusion protein to a luciferase fragment. Binding of a cell-permeable CID-probe to the target kinase brings about reassembly of the two complementary luciferase fragments thereby restoring luciferase activity, resulting in luminescence. Competitive displacement of the CID-probe by a test compound can be quantified in a dose dependent fashion by measuring loss of luminescence signal.
A Reversible Inhibition of BTK with Das
B Irreversible Inhibition of BTK with Ibru
