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Kinase Screening & Profiling with Cellular Assays

On the journey of drug screening against kinases, cellular assays hold the advantage of testing compounds in a more physiological environment and provide more value in reducing costs due to discovery failure in the later stages. While biochemical assays screen compounds based on their direct inhibitory potent on the enzymatic activity of kinases, cellular assays provide a more complex but real context where compounds can be examined for their true potential.

Many compounds that show high potency in biochemical assays fail to provide the same promising results in cellular assays. This could be due to many reasons including the following:

  • Poor permeability through the cell membrane
  • Stability or binding issues under physiological pH, ion concentrations, etc.
  • Interference by other proteins (off-target effects) which cannot be revealed in a biochemical assay
  • Performance difference related to protein structure or post-translational modifications

Creative Biogene, with over 20 years hard work in cell lines and stable cell line generation, takes the advantage of its rich experience and large collection of stable cell lines, and provides kinase screening and profiling services with cellular assays.

Cell-based Kinase Activity Assay:

This assay utilizes living cells expressing endogenous or exogenous kinases to test compounds for their inhibitory potency on the enzymatic activity of the kinases. The phosphorylation of the kinase substrate in the cells is measured and quantified by ELISA or AlphaLISA after compound exposure.

Cell-based Kinase Binding Assay:

This assay tests the binding affinity of a compound with its kinase target in living cells. The cells used in this assay expresses an exogenous kinase with luciferase labels, The compound-kinase binding affinity is measured by the changes of the luminescence readouts with and without compound exposure.

Cell-based Cell Proliferation Assay:

This assay is suitable to screen compounds targeting oncogenic driver kinases such as EGFR, or to evaluate off-target effects of the compounds. Creative Biogene has a comprehensive list of cell lines expressing wild-type EGFR or EGFR mutants. By measuring the cell proliferation and survival, the inhibitory potency of the test compounds on the kinases can be evaluated.

Advantages of kinase cellular assays at Creative Biogene:

  • Fast turnaround time
  • A broad collection of cell lines for cellular assay
  • Wide target portfolio
  • Competitive price
  • IC50 curve with raw data and report
  • Years of professional experience in kinase cellular assays

Contact us now to discuss your project with our experts and get the exact support you need.

* For research use only. Not intended for any clinical use.
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