Lead Discovery/Hit ID

High Throughput (HTS) Screening & Library Profiling Services

Kinase Drug Discovery and Development Process

Benefits

Select from over 450 validated kinase assays
Capacity to screen more than 100,000 wells/day
Flexible: screen any number of compounds against any number of kinases
Rapid data turnaround
Accurate, precise & reproducible data
Identify potent AND selective high quality leads in a single screen
Identify new target opportunities from existing chemical assets
Free internal resources to focus on other activities

High Throughput (HTS) Target Screening & Library Profiling Services

Overcoming screening bottlenecks while ensuring discovery programs remain on track and on budget in today's R&D climate requires innovative approaches and flexible solutions. Leverage the benefits of the industry's largest and highest throughput commercial kinase assay panel and KINOMEscan’s rich combination of kinase expertise and drug discovery experience to expedite your kinase inhibitor discovery program goals.

Enjoy the convenience of outsourced high-throughput screening and ready access to a portfolio of more than 450 highly validated and robust kinase assays that can be deployed for testing against compound collections of any size. Outsource with confidence knowing that KINOMEscan assays are performed under highly standardized conditions using best-in-class lab automation to provide exceptional assay performance and reproducible data. Save time and resources by eliminating assay development and free up internal resources to focus on other high value discovery activities.

From single target HTS to kinome-wide small molecule library profiling and follow-up services, KINOMEscan has the experience, capacity and capability to rapidly and reliably deliver accurate, precise and reproducible data that ensures project timelines are met and maximizes the discovery of potent & selective lead compounds for new drug discovery programs.

Services & Solutions

Rapidly screen hundreds or thousands of compounds against any KINOMEscan kinase assay panel or individual target from our broad portfolio of kinase assays.

A flexible 'a la carte' approach to personalized kinase profiling. Select from KINOMEscan's collection of 451 kinase assays and rapidly deploy a customized assay panel of any size comprised only of kinases relevant to your programs.

An economical approach to surveying the human kinome, scanEDGE includes 96 kinases distributed throughout the AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid, and atypical kinase families, plus important mutant forms and activation state-specific scanMODE assays that provide inhibitor binding mode information early in the drug discovery process.

The largest commercial kinase panel available, scanMAX contains a definitive set of 451 kinases covering AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid, and atypical kinase families, plus important mutant forms and activation state-specific scanMODE assays that provide inhibitor binding mode information early in the drug discovery process.

PathHunter® Cell-Based Kinase Screening & Profiling Services - New!

The PathHunter® Cell-Based Kinase Screening and Profiling Service leverages DiscoveRx's proprietary Enzyme Fragment Complementation (EFC) Assay Technology in a whole cell platform enabling customers to interrogate and characterize compounds in a more physiologically relevant context.

Accurate, precise & reproducible data

KINOMEscan screening partners have long recognized that accurate, precise and reproducible kinase profiling data are critical components of the discovery and development process and are the cornerstone of a successful screening partnership. All KINOMEscan assays undergo thorough validation prior to being released into production and assay performance is continually monitored to ensure data consistency & longitudinal concordance.

Data accuracy and precision have been demonstrated in several peer-reviewed publications from both the KINOMEscan team and from our partners.

Assay quality: Primary screen reproducibility

Outstanding screen to screen reproducibility
Enables data to be interpreted with confidence

Data Consistency

Profiling of the indicated compounds at 10uM in fourteen independent experiments against 442 kinases over a one year period. Correlation analysis was performed in a pair-wise comparison to calculate the correlation coefficient. The correlation coefficients range from 0.91 to 0.97 with an average of 0.95 [click graph to enlarge].

Assay Quality: Z’ values

Z’ values measure assay noise and predictive value
High Z’ values reproducibly measured across entire assay panel
High Z’ values ensure low false positive/negative rates

Assay Quality

Average Z’ values and standard deviations were calculated for each kinase based on fourteen control wells per experiment in over 135 independent experiments spanning a period of sixteen months. Average Z' = 0.71 [click graph to enlarge].

Detect multiple types of kinase inhibitors

Although the majority of kinase inhibitors developed so far have been type I or type inhibitors that fully or partially overlap the the ATP binding site, there are also examples of non-ATP competitive “allosteric” inhibitors that target the kinase active site and inhibit catalysis by repositioning key catalytic residues. Allosteric inhibition may represent a promising strategy for the development of highly potent & selective compounds. KINOMEscan affords investigators a flexible screening solution for detecting these multiple inhibitor types and to thereby extract the maximum value from their chemical assets. To learn more about the types of allosteric inhibitors detected in KINOMEscan assays, visit our Allosteric Inhibitor page.

Detection of Type I, II & Allosteric Inhibitors

Binding constant (Kd) determinations were measured for interactions between gefitinib, a known Type I inhibitor and EGFR (Kd = 3.4nM); imatinib, a known Type II inhibitor and KIT (Kd = 7.5nM); and CI-1040, a known non-ATP-competitive inhibitor and MEK1 (Kd = 120nM). These data illustrate the diversity of inhibitor types detected in KINOMEscan assays [click graph to enlarge].