Expedite Lead Optimization with the Broadest Kinase Menu
With over 15 years of experience in kinase drug discovery, DiscoverX offers the largest collection of nearly 500 biochemical and cell-based kinase assays. KINOMEscan® technology, our novel kinase inhibitor binding platform, includes an industry leading set of kinase assays that allow rapid determination of kinome-wide compound potency and selectivity. Several high profile Nature Biotechnology papers have established KINOMEscan as the best-in-class platform for measuring kinase inhibitor potency and selectivity Combining EFC technology with kinase biology expertise, our TKscanSM menu includes a growing list of functional cellular assays that detect the activation of full-length kinases in whole cells. Used alone or in combination, these powerful platforms can be applied to all stages of drug discovery and are ideal for identifying potent and selective inhibitors.
scanMAX® Kinase Assay Panel - World’s Largest Collection
The KINOMEscan platform employs a novel and proprietary active site-directed competition binding assay to quantitatively measure interactions between test compounds and more than 480 kinase assays. The largest commercial kinase panel available, scanMAX panel, contains a set of 468 kinases covering AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid and atypical kinase families, plus important mutant forms. Kinome-wide annotation of compound selectivity enables informed decisions about therapeutic opportunities and potential off-target liabilities which could otherwise be missed in smaller kinase panels.
KdELECT® Kinase Assay – Broadest Dynamic Range
KINOMEscan assays do not require ATP and therefore report true thermodynamic interaction affinities, as opposed to IC50 values, which can depend on the ATP concentration. KdELECT service allows quantitate compound binding affinity determination against over 480 kinase assays. Inhibitor binding constants (Kd values) are calculated from duplicate 11-point dose-response curves. Measurements are made under optimized conditions that generate true thermodynamic Kd values which facilitate direct comparison of inhibitor affinity across kinases. KdELECT may be used as a follow-up study tool to quantify binding affinity of compound-kinase interactions identified in primary screens, to supplement existing data, or support lead optimization and SAR activity.
Mode of Action Kinetic Analysis
Kinase inhibitor drug discovery requires the optimization of several other drug-like properties such as cellular potency, pharmacokinetics and pharmacodynamics, and activity against clinically relevant mutant kinases. Several of these properties are affected by an inhibitor’s binding mode and association/dissociation kinetics – two parameters that have been traditionally challenging to measure routinely during lead optimization. DiscoverX offers scanMODE™ and scanKINETIC™ services – biochemical tools that classify inhibitor binding mode (Type I or Type II) and association/dissociation kinetics, respectively.
scanMODE™ assays consist of activated/ inactivated kinase assay pairs that biochemically classify inhibitors as having Type I or Type II binding modes. scanMODE™ assays thus provide structural insights without the requirement for co-crystal structures – a feature that enables rapid, real time structural feedback during lead selection and optimization.
scanKINETIC™ assays enable the classification of inhibitors as having rapid, slow, or irreversible binding inetics, which is essential for robust inhibitor characterization and to resolve potentially conflicting potency data measured in biochemical, cellular and in vivo assay models. For example, target inhibition is sometimes maintained for several hours, even after the inhibitor has been ‘washed out’ from cellular assays. In the absence of kinetic data, these pharmacology results can be difficult to interpret, particularly when multiple inhibitors are being compared. scanKINETIC™ is a semi-quantitative, broadly applicable tool that is currently available for more than 225 kinases and is the largest commercially available panel for this application.