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Cell-based KinaseSeeker-TE Panel

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
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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.

cell based kinase 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

A Reversible Inhibition of BTK with Das

B Irreversible Inhibition of BTK with Ibru

B Irreversible Inhibition of BTK with Ibru

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