Screening

Our screening and profiling services provide flexible, convenient access to our technology and expertise, to help drive your drug discovery programs. We can also perform validation and screening of client-provided assays or build a custom assay to fit your specific screening needs.

Capabilities

Library screening: Screen your library to identify high quality starting points for your program.

  • Deliverables: % of inhibition or activation.
  • Application: Hit finding.

Dose-response profiling: Efficiently explore and optimize Structure Activity Relationships (SAR).

  • Deliverables: Kd or IC50.
  • Application: hit-to-lead and lead optimization.

Kinetic profiling of reversible inhibitors: Boost decision-making with parallel Structure Activity (SAR) and Kinetic Relationship (SKR) iterations, understand PK/PD disconnects and build better models to define therapeutic windows.

  • Deliverables: Kd, kon, koff and residence time.
  • Application: hit-to-lead, lead optimization and candidate selection.

Kinetic profiling of irreversible inhibitors: Identify irreversible compounds, rank inhibitor binding and covalent bond formation (SAR), define selectivity and interpret in vivo target occupancy.

  • Deliverables: KI, kinact, Kinact/KI.
  • Application: hit-to-lead, lead optimization and candidate selection.

Mechanistic assays: Get a better understanding of the drug-target interaction on a molecular level.

  • Deliverables: Determination of the mechanism of inhibition (competitive, non-competitive or uncompetitive) and inhibition constants (Ki, aKi).
  • Application: lead optimization and candidate selection.

Features and Benefits

  • Flexible access to a wide range of assay readouts and technology formats:
    • Fluorescent Intensity.
    • Fluorescent Resonance Energy Transfer.
    • Time-Resolved Fluorescence (TR-FRET, HTRF®, Transcreener®).
    • Fluorescence Polarization (IMAP®).
    • AlphaLisa® & AlphaScreen® based chemiluminescence.
    • Luminescence (ADP-GLO®).
  • Reliable and quick turnaround times
  • Accurate, precise & reproducible data
  • Integration with custom assay development to provide novel solutions
  • Free internal resources to focus on other activities
  • A continuous interaction with our clients on the progress of a screening project

How can we help?

Our experienced project manager will work with you to identify the best way forward for your project.

Speak to an expert today