Why Kinases Assays Matter for Therapeutic Development
Protein kinases regulate critical cellular signaling pathways and represent one of the most intensively targeted protein families in drug discovery. Dysregulated kinase activity drives diseases including cancer, inflammation, neurodegeneration, and metabolic disorders, making robust kinase assays essential for therapeutic development.
The Challenge in Kinase Inhibitor Discovery
Most kinase programs are slowed by the same obstacles: fragmented vendor workflows that drive up cost and delay timelines, incomplete kinome coverage that leaves clinically relevant mutants and disease-relevant kinases out of reach, rigid assay conditions that fail to reflect compound mechanism of action, and slow turnaround that holds up critical decisions.
Eurofins Discovery removes these bottlenecks with a single, integrated kinase profiling ecosystem – combining comprehensive kinome coverage, gold-standard validated platforms, flexible assay design, expert data interpretation, and rapid turnaround – so your team can make confident decisions from early screening through lead optimization.
Eurofins Discovery Kinase Platforms: KINOMEscan® and KinaseProfiler™
Eurofins Discovery’s industry leading kinase inhibitor discovery platforms, KINOMEscan® and KinaseProfiler™, of over 500 kinases leverages automation-compatible biochemical, cell-based and biophysical assays for rapid determination of kinome-wide potency, selectivity, and mechanism-of-action of pharmacophores.
KINOMEscan and KinaseProfiler assay platforms used by leading pharma, biotech and AI-driven drug discovery teams, offer the following advantages:
- Enable informed decision-making with binding affinity (Kd) and functional activity (IC50) data on therapeutic molecules
- Support programs from early discovery and hit finding through lead optimization and candidate selection
- Optimal for investigating allosteric, covalent, noncovalent, or bifunctional inhibitors and degraders
- Amenable to screening small molecules, peptides, conjugate and multi-functional therapeutics
- Provide integrated drug discovery workflow from compound management to data analysis with TREEspot visualization dashboards
- Deliver rapid turn-around times to support SAR, rank-ordering, and aggressive project timelines
Additionally, Eurofins DiscoverX kinase products provides 750+ recombinant kinases and cell-based functional, binding, and activity assays for discovery through development and for QC lot-release testing.
TREEspot™ – Powerful Visualization for Kinase Profiling Data
TREEspot is a proprietary software platform that converts complex kinase profiling data into an intuitive, graphical representation. By mapping compound activity from KINOMEscan and KinaseProfiler onto a phylogenetic tree of the human kinome, TREEspot provides a rapid, at-a-glance interpretation of selectivity data. Included with our standard kinase profiling services, TREEspot enables you to:
- Rapidly assess selectivity across the kinome
- Simplify interpretation of large, complex kinase datasets
- Generate communication-ready visuals for reports, presentations, and publications
Eurofins Discovery Kinase Services: A Solution for Your Drug Discovery Goals
No matter your assay format or readout goals, we offer comprehensive kinase screening services and kinase profiling solutions spanning the full kinome to support your drug discovery program. Reference the table below to identify the service that will meet your kinase needs or contact us for personalized program pharmacology guidance. Beyond standardized panels, we offer custom kinase profiling to support hypothesis-driven discovery and in-depth MoA studies. For programs that require more than standalone services, Eurofins Discovery’s Integrated Drug Discovery team streamlines kinase programs through a single, end-to-end partnership.
| GOAL | SOLUTION | METHOD | |
|---|---|---|---|
| BIOCHEMICAL | Investigate Kinase Catalytic Domain and Kinase SH2 Domain Affinity Binding
Classify Type I and Type II Binding Modes for Kinase Catalytic Domain Inhibitors |
KINOMEscan | Quantitative PCR, No ATP |
| Evaluate Kinase Activity at 10µM, Km and 1mM ATP | KinaseProfiler | Radiometric, luminescence With ATP, TR-FRET | |
| Evaluate ATP competition/cooperation
Evaluate reversibility Evaluate ligand type (classical or slow binder) Evaluate Kinact, Kon and Koff |
Biochemistry Assays | Radiometric, luminescence With ATP, TR-FRET | |
| CELL-BASED | Measure Cellular Functional Activity (Dimerization, Phosphorylation, SH2 Recruitment) | Tyrosine Kinase Assays | Chemiluminescent
(Enzyme Fragment Complementation) |
| Determine Drug-Target Engagement | TE Cell Based Assays | Bioluminescence Resonance Energy Transfer (BRET) | |
| Assess Drug-Target Engagement and Protein Thermal Stability | InCELL Pulse | Chemiluminescent
(Enzyme Fragment Complementation) |
|
| Explore Drug-Target Engagement and Protein Turnover and Stabilization | InCELL Hunter | Chemiluminescent
(Enzyme Fragment Complementation) |
|
| BIOPHYSICAL | Evaluate affinity constants (KD)
Determination of allosteric binders (ATP competition) Evaluate the Kinetic Parameters Determination of binding stoichiometry |
Biophysical Assays | Surface Plasmon Resonance (SPR)
Spectral Shift (SpS) MST-TRIC Spectral shift Microscale Thermophoresis (MST) Isothermal Titration Calorimetry (ITC) |
| SAFETY PHARMACOLOGY | Identify Drug Safety Liabilities, Mitigate Off-Target Effects, Predict Clinical Adverse Effects | In Vitro SAFETY Panels | Radiometric,
Chemiluminescent (Enzyme Fragment Complementation) |
FAQs about Kinases in Drug Discovery
- What are kinase assays?
- Kinase assays measure protein kinase activity and how it changes in response to compounds. They typically assess substrate phosphorylation, ATP use, kinase dependent cellular signaling changes, or compound binding, using either biochemical or cell-based formats to support screening and drug development.
- Why are kinases important in drug discovery?
- Kinases control critical pathways like cell proliferation, survival, metabolism, and immune function. Their dysregulation drives diseases such as cancer and inflammation, making them highly validated and druggable targets in therapeutic development.
- What are the main differences between biochemical and cellular kinase assays?
- Biochemical assays measure enzyme activity in a controlled, cell-free system providing direct, high precision measurements of inhibitor potency and are ideal for potency and screening. Cellular assays measure kinase signaling in living cells, capturing biological biologically relevant factors such as cell permeability, ATP competition, and pathway regulation.
- How do kinase selectivity and profiling support lead optimization?
- Selectivity profiling tests compounds across kinase panels to identify off-target effects early. This helps improve safety, refine chemistry, and optimize therapeutic windows, especially given the similarity across kinase families.
- How can kinase assays be tailored to specific disease areas or signaling pathways?
- Kinase assays can be customized using disease-relevant targets, mutations, or cell models. This ensures results align with the biology and therapeutic goals, including inhibitor or degrader development.
- What is the difference between binding and functional kinase assays – and when should I use each?
- Binding and functional kinase assays answer different but equally important questions about compound-kinase interactions. Used together, they provide a comprehensive and orthogonal view of potency, selectivity and mechanism and are most powerful when used together.
- Binding assays quantify the direct physical interaction between a compound and a kinase, reporting affinity (Kd) independent of enzymatic activity or ATP turnover. They isolate target engagement from assay context, and provide a clean, mechanism-agnostic readout of compound-target interaction.
Functional assays measure enzymatic inhibition and generate IC50 values under defined ATP conditions. They provide a context-dependent assessment of inhibitory activity. - What is KinaseProfiler?
- KinaseProfiler™ is the gold standard functional, activity-based platform for kinase inhibition determination, with 30+ years of track record. Covering 450+ kinases including lipid kinases, the platform combines radiometric, FRET, and luminescence technologies with a guaranteed 6-day TAT for standard panels and <1% false positive/negative rates.
- What is KINOMEscan?
- KINOMEscan® is Eurofins Discovery’s proprietary, high-throughput platform that quantifies kinase binding affinity (Kd) across 450+ kinase targets, including clinically relevant mutants. Specialized, customizable panels deliver rapid, scalable solutions for early- and late-stage selectivity profiling.
