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Qualified Hits Technologies

Get qualified hits according your predetermined and fully customizable Research Target Profile (RTP).

Discover:
  • Mode of Inhibition - Whether allosteric, orthosteric or covalent
  • Affinity - We measure KD, ligand efficiency and IC50.
  • Binding Kinetics - Essential binding kinetics such as Kon, Koff and residence time.
  • Selectivity - Determine the KD as well as off target interaction analysis.
  • Binding mode - Use either X-ray crystallography or Cryo-EM to structurally determine the binding mode.

The Qualified Hits Engine

QualifiedHits-diagram QualifiedHits-diagram

The Qualified Hits process

Analysis and Planning

  • Team Assembly
  • Target access assessment
  • Target analysis
  • HTS library selection
  • Screening cascade defined
  • Assays identified
  • Structural biology planning

Platform Establishment

  • Establishment of protein production
  • Establishment of assay systems
  • Establishment of structural biology

Library Screening

  • Fragment screening
    [3k hand-picked fragments]
  • Range Finder screening
    [fragment enriched 41k small molecule library]
  • Small molecule HTS
    [150k high-quality small molecules]
  • Reporter Displacement
  • Enzymatic Assays
  • SPR, MST, nanoDSF, nanoBRET, TSA

Hit Confirmation

  • Reporter displacement assays
  • Binding affinity and kinetic profiling via SPR
  • Enzymatic profiling of impact of inhibitors
  • MicroScale Thermophoresis binding assays
  • Label-free nanoDSF binding assays
  • nanoBRET target engagement
  • Luminescence interaction analysis using Alpha LISA Screening
  • Interaction thermodynamic analysis using Isothermal titration calorimetry

Hit Characterization

  • Reporter displacement assays
  • Enzymatic Assays
  • Luminescence interaction analysis using Alpha LISA Screening
  • Binding affinity and kinetic profiling via SPR
  • MicroScale Thermophoresis binding assays
  • Label-free nanoDSF binding assays
  • Interaction thermodynamic analysis using Isothermal titration calorimetry
  • nanoBRET target engagement

Structural Elucidation

  • X-ray crystallography
  • Cryo-EM

Qualified Hits

At the end of the process you will receive the deeply characterized qualified hits,

which meet the project specifications.