Activity-based Biochemical Screening/Profiling Assay Services

Once compounds are identified, Mechanism of Action studies are necessary to characterize and compare the potential drug candidates. In cooperation with Carna Biosciences, we offer activity-based kinase profiling and screening services for assessing the potency and selectivity of your compounds. We offer to test at higher ATP concentration (1mM) to provide insight into compound inhibition and potency under more physiologically relevant conditions, in addition to our ~ATP km assay services.

Features of our profiling and screening assays:

  • Massive Kinome Coverage
  • Activity-Based Profiling & Screening
  • Confirm your results at higher ATP concentrations to identify potential Type II/III inhibitors
  • Build your own panel or consider our unique pre-selected panels.

Mobility Shift Assay(MSA)/IMAP™ Kinase Assay Services

Mobility Shift Assays/IMAP™ assays directly monitor phosphorylation by measuring the non-phosphorylated and phosphorylated substrate in the kinase reaction. The technology is based on microfluidics on a microchip involving the electrophoretic separation and quantification of the fluorescently labeled substrate and the phosphorylated product. The potency and selectivity of your compounds are assessed against the target kinases you select. All kinases utilized in our assays are produced and guaranteed to be of the highest quality, enabling us to deliver high-quality data to you. The ATP concentration in our assays is set around the Km value. For an enhanced understanding of selectivity and allosterism, many assays have also been validated using 1mM ATP. For slow-binding compounds, we offer assays pre-incubating the kinase with your compounds. 

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Kinase Screening Kinase Profiling

ADP-Glo™ Kinase Assay for Lipid Kinase Screening & Profiling

For Lipid kinase screening and profiling we use the ADP-Glo™ assay platform.  The potency and selectivity of your compounds is measured via ADP formed from a kinase reaction. The ADP is converted into ATP, which is used to generate light in a luciferase reaction. The luminescence (RLU value) generated correlates with kinase activity. The ATP concentration of our lipid kinase assays is set at the approximate Km for each kinase.

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