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.