Kinase Selectivity Profiling That Shows You More Than % Inhibition
KinSight™ profiles your compounds against 400+ validated kinases using continuous, real-time assays — delivering true selectivity data, TDI detection, and MOA insights that endpoint platforms systematically miss.
400+
Wild-type kinases available
n=2
All assays run in duplicate
Customizable
Design your own panel
2 wks
Detailed report turnaround
Four Steps From Compound to Kinetic Insights
A streamlined process designed to get you high-confidence profiling data with minimal friction — from submission to annotated report in two weeks.
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1
Submit your compound and select a panel
Choose from six predefined panels or work with our team to build a custom target list. Single concentration or dose-response available.
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2
We run continuous assays at your ATP conditions
ATP Km for maximal potency insight, 1 mM for physiological relevance, or both. Every well generates a full progress curve — actual rates from multiple data points.
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3
Expert review and annotation
Our scientists review every result and annotate TDI signals, unusual kinetics, and MOA insights. Not just a data dump — a report you can act on.
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4
Full data package delivered in two weeks
Waterfall plots, kinome tree visualization, tabular % inhibition data, and annotated progress curves — ready to share with your team and advance your program.
What's in your data package?
- ✓Waterfall plots ranked by % inhibition across all targets
- ✓Annotated kinome tree visualization
- ✓Tabular % inhibition data export
- ✓Progress curves for every well (not just endpoint)
- ✓TDI, slow-binding, and unusual kinetics flagged by scientists
- ✓MOA insights and selectivity score summary
Standard turnaround: 2 weeks
Rush timelines available on request. No minimum compound quantity required for feasibility discussion.
Start Your ProjectWhy Continuous Profiling Outperforms Radiometric & Fluorescence Endpoint Methods
Most kinase profiling platforms take a single snapshot at the endpoint — an assumption that silently drops more than you'd think. PhosphoSens® measures the full reaction trajectory, revealing what endpoint-only assays are structurally blind to.
Calculated from the linear region of the progress curve — not after equilibration, product inhibition, or enzyme degradation have distorted the signal. What you measure is actual catalytic rate.
Time-dependent inhibition reveals itself as curvature in the progress curve — invisible at a single endpoint read. KinSight flags TDI activity across every target in your panel, not just your primary.
Run at ATP Km for maximal potency insight, 1 mM for physiological relevance, or both. Endpoint platforms lock you into a single ATP concentration — often 10 µM — that systematically overestimates potency.
Progress curves distinguish competitive, slow-binding, irreversible, and mixed-mechanism inhibitors across the panel. That mechanistic resolution is the difference between a selectivity profile and a selectivity map.
Continuous profiling does more than rank kinases by % inhibition — it reveals whether the assay is linear, curvy, delayed, or time-dependent. That's the difference between data you can act on and data that looks right until it isn't.
See What Continuous Profiling Reveals That Endpoints Miss →Kinase Selectivity Panels
| Panel Name | Panel Size | ATP Options | Use Case | |
|---|---|---|---|---|
| Wild-Type Protein Kinase Panel | 401 | ATP Km and 1 mM | Broad selectivity, safety tox, off-target ID | View Panel → |
| Full Proteome Kinase Panel | 450 | ATP Km and 1 mM | Comprehensive off-target screening | View Panel → |
| Tyrosine Kinase (TK) Panel | 83 | ATP Km and 1 mM | RTK / non-RTK selectivity profiling | View Panel → |
| Cyclin-Dependent Kinase (CDK) Panel | 32 | ATP Km and 1 mM | Cell cycle & oncology selectivity | View Panel → |
| Mutant Protein Kinase Panel | 53 | ATP Km and 1 mM | Resistance mutation profiling | View Panel → |
| KiNode Panel | 69 | ATP Km and 1 mM | Focused selectivity screening | View Panel → |
| Custom Panel Design Your Own | 1–150 | ATP Km and 1 mM | Any program-specific target list | Contact Us → |
* Kinase selectivity profiling is conducted on a biweekly schedule, with assays run at the appropriate ATP Km (by available research pathway assessments) or at 1 mM ATP (in approximate physiological conditions). Alternative ATP concentrations can be accommodated upon request.
Don't See the Right Fit?
Work directly with our scientists to design a custom panel around your program's specific targets — any combination of 1–150 kinases, any ATP condition, any concentration format.
How KinSight Compares
Most kinome profiling platforms compress an entire enzyme reaction into a single number at one timepoint. KinSight measures the full reaction in real time — revealing not just which kinases are inhibited, but how and how confidently.
| Features | KinSight | Competition Binding | Radiometric Assay | Mobility Shift |
|---|---|---|---|---|
| Measures kinase activity Not just binding or indirect signal — actual enzyme velocity | ✓ | ✗ | ✓ | ✓ |
| Real-time progress curve per well Full reaction trajectory, not a single endpoint read | ✓ | ✗ | ✗ | ✗ |
| Detects TDI & slow-binding inhibitors Kinetic behaviors invisible to endpoint assays | ✓ | ✗ | ✗ | ✗ |
| Built-in reaction QC per well Curve shape reveals artifacts, instability, interference | ✓ | ✗ | ✗ | ✗ |
| Versatile ATP Concentrations Profile at ATP Km to maximize potency or 1 mM for physiological relevance | ✓ | ✗ | Partial | Partial |
| Native Peptide Sequences. Real Enzyme Behavior. PhosphoSens substrates are derived from authentic biological peptide sequences | ✓ | ✗ | Varies | Varies |
| Expert MOA annotation in report Scientists flag TDI, unusual kinetics, off-target liabilities | ✓ | ✗ | ✗ | ✗ |
* "Detects TDI & slow-binding inhibitors" requires a continuous readout by definition — time-dependent inhibition is a kinetic phenomenon that collapses to a single value at any endpoint read. "ATP Km conditions (Partial)" indicates the platform offers some ATP concentration flexibility but does not run at true enzyme-specific Km as standard. "Optimized substrate (Varies)" reflects that substrate selection and quality varies across kinases on those platforms. KINOMEscan (Eurofins/DiscoverX) measures binding displacement, not catalytic activity — a fundamentally different biological question.
Expand Your Selectivity Coverage
Kinase selectivity is only part of the picture. Phosphatases are emerging therapeutic targets — and off-target phosphatase activity can drive toxicity your kinase panel won't catch.
Phosphatase Selectivity Profiling
Continuous activity-based profiling across serine/threonine and tyrosine phosphatases — same real-time kinetic approach, applied to an underexplored target class critical for drug safety and efficacy.
Resources for Kinase Assay Scientists
Deep Kinetic Characterization: When IC50 Isn't Enough
A continuous assay, like our PhosphoSens assay, that measures the catalytic event of phosphorylation in real time enables determination of kinetic parameters that power your drug discovery research.
Continuous vs. Endpoint Kinase Assays: What You Need to Know
Kinome Profiling With a Continuous Assay
Have you ever heard of Anscombe’s Quartet? It emphasizes the significance of data visualization and teaches us that descriptive statistics may be misleading.
Ready to Profile Your Compound?
Tell us about your compound and goals. We'll recommend the right panel and ATP conditions — or scope the full project with one of our scientists directly.
Most projects start with a 20-minute scoping call. No commitment required.
Frequently Asked Questions
What is a PhosphoSens® kinase assay?
PhosphoSens® assays are continuous, real-time kinase activity assays that directly measure phosphorylation of a substrate peptide throughout the reaction. Unlike endpoint assays that capture a single time point, PhosphoSens generates a full progress curve — enabling true kinetic analysis including IC₅₀, Kᵢ, kobs, and time-dependent inhibition (TDI) from a single experiment.
How does a continuous kinase assay detect time-dependent inhibition (TDI)?
TDI compounds produce a characteristic change in the progress curve shape — the inhibition deepens over time as the compound slowly occupies or covalently modifies the enzyme. Because PhosphoSens monitors activity continuously, this curve deviation is directly visible. Endpoint assays that measure at a single time point will either miss TDI entirely or mischaracterize its potency, depending on when they sample the reaction.
Can't find my target in the catalog?
We offer custom assay development for kinase targets not currently in our catalog. Our team can design and validate a PhosphoSens substrate for your target, typically within 8–12 weeks. Contact us to discuss your target, timeline, and project requirements.
How is KinSight different from KINOMEscan, HotSpot, or KinaseProfiler?
KINOMEscan, HotSpot, and KinaseProfiler are all endpoint assays — they take a single read after a fixed incubation and report % inhibition or binding. KinSight uses continuous PhosphoSens® assays that monitor the full reaction in real time, generating a progress curve for every well. That means we detect TDI, slow-binding, and unusual kinetics that endpoint platforms will miss — and we can run at physiologically relevant ATP Km conditions rather than a fixed 10 µM ATP that systematically overestimates potency.
Can I design a custom kinase panel?
Yes — custom panels are a core part of what we do. You can specify any combination of 1–150 kinases from our catalog of 400+ validated targets. Our scientists will work with you to confirm availability, recommend complementary targets based on your program, and confirm ATP conditions. Contact us to get started — there's no minimum order for a custom panel feasibility conversation.
Can KinSight be used for safety/tox screening, not just drug discovery?
Yes, and it's increasingly used for exactly that. Broad-panel profiling at 1 mM ATP provides a physiologically relevant view of off-target kinase liabilities early — before they surface in cell-based or animal studies. The TDI detection capability is particularly relevant for tox screening, since time-dependent inhibition of off-target kinases can drive delayed or mechanism-based toxicity that endpoint assays miss entirely.
How do you identify off-target liabilities from the data?
Our scientists review every result — not just the hits. The report flags: (1) unexpected high-inhibition targets outside your intended pharmacology, (2) TDI signals that suggest irreversible or slow-onset binding, (3) kinases with structural similarity to your primary target that warrant follow-up, and (4) any results with unusual kinetics that might indicate assay artifacts vs. real biology. You get a curated interpretation, not a raw data dump.
What does the kinome tree visualization show me?
The kinome tree maps all human kinases in their evolutionary/phylogenetic relationships. Your profiling results are overlaid on this map — targets with high inhibition are shown as larger, colored circles, making it immediately visible whether your compound is hitting a tight cluster (suggesting on-target pharmacology with known selectivity) or scattered across unrelated families (suggesting promiscuity). It's the fastest way to communicate selectivity to internal stakeholders or in a partner presentation.
Can you profile phosphatase selectivity as well as kinases?
Yes. We offer phosphatase selectivity profiling as a companion service using the same continuous assay approach. This is especially valuable when your compound or program involves phosphatase-adjacent biology, or when you want a complete picture of off-target activity that kinase profiling alone won't capture. See our Phosphatase Profiling page for panel details.
How many compounds can I screen in a single run?
Profiling runs are scheduled biweekly. You can submit multiple compounds per run — contact us to discuss batch sizing, compound requirements (amount, concentration, solvent), and turnaround expectations. Single-compound rush submissions can be accommodated on a case-by-case basis.
Ready to Characterize Your Compound?
Talk to one of our scientists about your target, your workflow, and which assay format will get you the data you need.
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