ON-DEMAND WEBINAR | 44 MIN

Beyond Binding: real-time, activity-based kinome and phosphatome profiling

An endpoint read gives you one number at one time point. See what a progress curve in every well reveals about selectivity, mechanism and assay quality, across the kinome and the phosphatome.

Kinome Tree Graphic-1
WHY THIS MATTERS

Selectivity data decides which compounds advance. A single read can't tell the whole story.

Most panels rely on a binding readout or a single endpoint at low ATP. Binding tells you a compound engages a target, not how well it inhibits it. An endpoint tells you how much product formed, not whether the enzyme behaved as assumed or whether inhibition changed over the course of the assay. Activity-based profiling with continuous progress curves measures inhibition directly and shows you how it unfolds.

Same endpoint, four different stories
TTBK165% at endpointLinear: a confident readFGFR361% at endpointNoise: flags a QC checkBTK61% at endpointCurvature: time-dependent inhibitionHCK60% at endpointExtended lag phase
Uninhibited+ InhibitorEndpoint read
Schematic of the TTBK1, FGFR3, BTK and HCK examples shown in the webinar.

Topics covered in this session

What Daniel covers

Six things you'll take away from the session

01

One number, four stories

Why the same endpoint % inhibition can hide completely different kinase behavior, and how a progress curve in every well tells them apart.

02

Catch it in the primary screen

Spot time-dependent inhibition, lag phases and assay artifacts before they derail a candidate.

03

Binding is not inhibition

Why Kd doesn't translate one-to-one into activity, with a J. Med. Chem. example where hit rank order changed.

04

1 mM ATP or ATP Km?

How to choose your profiling condition, and what each tells you about selectivity.

05

Inside a KinSight™ report

Heat map, waterfall plot, kinome tree, and flagged progress curves for every compound.

06

Profiling the phosphatome

How the same real-time approach extends to 50 protein phosphatases, read by initial rates.

KINSIGHT™ PROFILING SERVICES

Activity-based profiling across the kinome and the phosphatome

The same PhosphoSens® assays Daniel walks through in the webinar, run as a service by the team that built them.

560+kinases

Wild-type and mutant, on one activity-based PhosphoSens® platform

50phosphatases

Protein phosphatase profiling from initial reaction rates, which few providers offer at all

1 mM or KmATP

Physiological ATP, ATP Km for the widest off-target view, or both side by side

10–15days

To a report with heat map, waterfall plot, kinome tree and flagged progress curves

1 · Scoping call

Tell us your targets, series and the decision the data needs to support.

2 · Study design

We recommend the panel, ATP condition and controls, and quote it.

3 · Kinetic report

Results in 10–15 days, with a straight path to IC50, Ki and kinact/KI.

Put this to work on your own compounds

Send us your targets and series, and we'll recommend a panel, ATP condition and follow-up kinetics.

Scope a panel

Working on a covalent or slow-binding inhibitor program?

Get direct scientific support characterizing your compounds — plus access to our Excel-Fit templates for streamlined kinact/KI and residence-time analysis.

A PREVIEW FROM THE RECORDING

One endpoint, four stories

Binding vs. inhibition

Profiling the phosphatome

Progress curves for AXL, FGFR4, CSK and BTK from the Beyond Binding webinar
One endpoint, four stories
Phosphatase profiling with initial reaction rates
Profiling the phosphatome
Beyond Binding webinar title slide
45-minute recording + slides
Daniel Urul, PhD
Daniel Urul, PhD | Senior Scientist, Discovery Technologies

Daniel runs AssayQuant's KinSight™ kinase and phosphatase profiling panels, working directly with pharma and biotech teams to turn selectivity data into mechanism: IC50, Ki, reversibility and time-dependent inhibition.

WATCH THE RECORDING

Get the full session and the slides

Daniel Urul, PhD, the scientist who runs our KinSight™ panels, shows why one endpoint number can hide four different stories, why binding is not the same as inhibition, and how activity-based profiling at 1 mM ATP or ATP Km catches time-dependent inhibition and lag phases in the primary screen. It ends with phosphatome profiling and a live Q&A, including how to choose your ATP condition. Fill in the form for instant access to the 44-minute recording and the slide deck.

Beyond Binding webinar title slide
▶ Full recording · 44 min
PDF
Slide deckAll 31 slides, including the kinome and phosphatome data

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