An understanding of compound selectivity is critical for kinase drug discovery. However, it's not enough to simply understand the potency of your compound (how strongly it inhibits its target). You also need to know what other kinases may be inhibited to identify potential off targets to address in counter screens.
AssayQuant's KinSight quantitative kinome profiling services are powered by our novel and proprietary PhosphoSens® technology — a continuous assay format. This assay directly quantifies the enzymatic activity of the target by reporting substrate phosphorylation during the entire reaction. A continuous format yields an actual reaction rate determined from dozens of data points, generating a progress curve in every well.
Our determination of the actual reaction rate makes it possible to use kinome profiling services at all stages of the pre-clinical drug discovery process. Kinome profiling enables identification of compounds with poor target profiles or those to further optimize. It can also offer confirmation or identification of off targets.
Our expert scientists use these deep data sets to create a detailed report for each of your compounds. This report includes important functional information about the enzymology of the kinases and nature of the compound. Guide improved drug development with these valuable and actionable kinetic insights.
Together, an industry-leading kinase panel, compound management, full automation, and in-depth kinetic analysis form unparalleled kinome profiling services. Our kinase panel encompasses a wide variety of kinases and includes over 400 wild-type kinases (and growing). Swiftly determine the kinome-wide selectivity of your compounds, gaining crucial insights into their MOA and relative potency. Delve deeper into insights, our fit-for-purpose services for potency assessment with reversible and irreversible inhibitors are at your disposal.
To request the use of our kinome tree, please contact us.
Yields an actual reaction rate determined with high confidence from dozens of data points. Each rate is gathered from duplicate wells, providing accurate and precise determinations. With a complete progress curve, we provide critical information for enzyme & drug performance. Potentially including the kinetics of time-dependent inhibition (A) and compound-enhanced lag (B).
Maximize your compound potency by performing profiling at the ATP Km concentration. Additionally, gain physiological insights by performing profiling at 1 mM ATP. Or, for significant potency and MOA insights, profile at both concentrations. Fulfill all your selectivity screening needs with ease.
Our technology is compatible with physiological levels of ATP, Mg2+, Mn2+, and Ca2+ and incorporates relevant activators and cofactors.
Our reports provide more than just a list of % inhibition values. Our enabling service gives you greater confidence in the data. This includes annotation of kinetic observations that may identify exploitable modes of action.
We focus on generating biologically relevant peptide substrate sequences optimized for performance with each target kinase.
Our growing panel of 400+ wild-type kinases was selected after testing preparations from multiple suppliers. We can include mutant kinases, kinase cascade assays, and custom panels upon request. New assays are continuously added.
We use a single platform for the entire kinase panel so you can directly compare your hits.
Screening complete in two weeks so you get results quickly and meet your deadlines.
Interested in exploring our full data report? Download a sample data report complete with known inhibitors and reference compounds. We tested them at variable compound concentrations with ATP concentrations at either Km or 1 mM for each of our 400+ kinases! Preview the possibilities of kinetic insights into selectivity and mechanism of action (MOA) for your drug discovery research.
Get a full view of the kinome with our expansive kinome panel. Our kinome panel contains 400+ wild-type kinases and two relevant mutant enzymes.
We can add mutants or create custom panels on demand.
Please inquire about our assay development services with >95% success rate.
Reach out to us to learn how we profile protein phosphatases and diacylglycerol lipid kinases (DGKs).