Kinase Biology for Drug Discovery
We offer a large portfolio of ready-to-use bioluminescent biochemical and cellular kinase assays that can measure a compound’s effect on kinase activity, affinity or cellular signaling, including degradation. This portfolio includes many of our flagship assays and technologies, including ADP-Glo™, NanoBRET® TE, Lumit® and HiBiT technologies that are amenable to high-throughput applications.
We also offer cellular kinase selectivity profiling services and custom assay development services:
Biochemical Kinase Assays
Simplifying Kinase Activity Measurements
The ADP-Glo™ Kinase Assay is a luminescent kinase assay that measures ADP formation, a direct product of kinase reactions. The assay has a high dynamic range and produces a strong signal at low ATP-to-ADP conversion, making it a great option for high-throughput screening (HTS) applications in drug discovery. It is ideally suited for low-activity kinases, such as growth factor receptor tyrosine kinases. To complement the ADP-Glo™ assay, we offer 360+ Kinase Enzyme Systems that are optimized for use with ADP-Glo™ assays and contain all the components needed to run the assay.
ADP-Glo™ Kinase Assay Benefits
- Easy to use and automation-compatible: Streamlines the kinase inhibitor screening process, compatible with high-throughput screening.
- High sensitivity and flexibility: Suitable for a wide range of kinases.
- Robust and reliable: Delivers consistent results across various conditions.
- Over 360 Kinase Enzyme Systems available: All optimized for use with ADP-Glo™ Assays.
Kinase Target Engagement in Cells
Simplifying Kinase-Compound Affinity Measurements
NanoBRET® Target Engagement (TE) Kinase Assays are a live-cell, addition-only luminescent assay platform that provides precise compound affinity measurements for your target kinase and off-target kinases. NanoBRET® TE Kinase Assays help prioritize compounds during drug development by eliminating uncertainty in determining the cellular affinity of compounds. These scalable, multiwell plate assays accelerate hit-to-lead workflows by helping to reveal novel pharmacophores for your target kinase or new interacting kinases for your compound.
Key Benefits of NanoBRET® TE Kinase Assays
- Ready-to-use assays: Access 340+ live-cell kinase binding assays with detailed application notes to ensure you get started quickly.
- Quantitative cellular data: Determine intracellular compound affinity (Kiapp) and fractional occupancy using full-length kinases, yielding accurate target engagement results.
- Reliable results: Achieve reproducible BRET assay data with excellent Z’ values, providing confidence in your decisions.
Cellular Kinase Selectivity Profiling
Pinpoint Kinase Selectivity with Cellular NanoBRET® TE Kinase Profiling
NanoBRET® TE Kinase selectivity profiling uses hundreds of live-cell NanoBRET® TE Kinase assays in a single experiment to quantify compound occupancy, using kinases broadly spanning the kinome. This live-cell method can reveal interactions missed with biochemical methods, and it yields reproducible results that correlate with downstream signaling events. By providing kinase researchers with accurate insights into intended and unintended compound interactions, this advanced approach can reduce costly errors in developing drugs or chemical probes.
Lab-Ready Cellular Kinase Selectivity Profiling
- Quantify kinase selectivity in live cells in your lab: Profile 192 kinases simultaneously with high precision using a single, streamlined experiment.
- Ready to use: Experience efficient workflows with the easy, addition-only format—perfect for getting rapid profiling results.
Learn more about NanoBRET® TE Kinase Selectivity Profiling:
Services for Cellular Kinase Selectivity Profiling
- Diverse kinase panels: Choose panels with 192 or 300 full-length kinases, broadly representing the kinome.
- Simple ordering with schedule to fit your needs: Monthly and on-demand runs.
- Hit follow-up made easy: Determine compound affinity for individual kinase hits in live cells.
Learn more about Kinase Selectivity Profiling Services:
Cellular Pathway (Phosphorylation) Analysis
No-Wash, One-Plate Immunoassays for Phosphoprotein Analysis
The Lumit® Immunoassay Cellular Systems is a sensitive luminescent antibody detection method to examine phosphorylation and study inhibitors that target specific nodes of the major kinase signaling pathways. This no-wash bioluminescent immunoassay measures native target analytes directly in cell lysates—no need to engineer your cells. Choose from complete kits with optimized antibody pairings, or build your own assay for your protein of interest.
Lumit® Immunoassay Cellular Systems Benefits
- Simplified workflow: No wash steps required, reducing the complexity and time of the assay process.
- Detect endogenous targets: Eliminates the need for cell engineering; assays are compatible with any cell type, including primary cells.
- High sensitivity and specificity: Detects low-abundance proteins with excellent specificity.
- Complete kits available: Alternatively, build your own cellular Lumit® Immunoassay for your protein of interest.
Cellular Kinase Protein Levels
Easily Track Total Kinase Protein Levels in Degradation or Stabilization Studies
Explore versatile solutions for assessing compound effects on kinase protein expression in cells. Use the Lumit® Immunoassay Cellular Systems for rapid detection of non-engineered kinases in any cell type, or the HiBiT CRISPR cell lines to track real-time changes in kinase levels within live cells. Choose the right tool for your research needs.
Lumit® Immunoassays: Track Endogenous Kinase Protein Levels in Cells
- Monitor native kinase levels with ease: No cell engineering required.
- Universal compatibility: Works with any cell type, including primary cells.
- Streamlined method: Fast, homogeneous microplate format compatible with automation for quick, efficient, high-throughput protein detection results.
- Flexible options: Target-specific Application Notes provide a quick-start guide, while custom assay development tools are available.
HiBiT CRISPR Cells: Real-Time Tracking of Kinase Degradation
- Correlate luminescence with target protein levels: HiBiT fusion protein luminescence reflects cellular levels.
- Real-time monitoring: Track HiBiT-tagged protein levels dynamically by co-expressing LgBiT.
- Measure kinetic parameters: Quantify degradation metrics like Dmax and degradation rates.
Learn more about CRISPR knock-in cells for kinase target analysis:
