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Assays, Biophysics, Screening for innovative target-ligand interaction analysis

Assays, Biophysics & Screening service projects are typically very individual and require a high degree of customization. Simply get in touch with Proteros for your project demands and we will suggest a recommended assays, biophysics, and screening path.

Whether you are looking to probe binding sites and modes of action, analyze biochemical activity or determine and optimize kinetic profiles, we can develop the RIGHT assay using the RIGHT technologies so you can REACH RIGHT FASTER.

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Proteins, Structures and Assays

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Target ligand interaction

We deliver full biochemical and biophysical characterization of ligand-target interactions for even the most challenging drug discovery projects through the application of the RIGHT technologies and the RIGHT assays.

Proteros screening platform enables insight into various mode of inhibitions : 

  • Allosteric inhibitor screening
  • Protein-Protein-Interaction inhibitors and enhancers
  • High-throughput binding affinity and residence time quantification
  • Deconvolution of non-covalent and covalent binding contribution

Proteros opens avenues towards kinetically optimized drug candidates with increased efficacy and selectivity.

The Proteros synergistic Scientific Team "under-one-roof" is comprised of:
  • 17 assay, biophysics and screening experts led by 7 PhDs with superior drug discovery experience
  • 50+ Protein Scientists and 13 PhD's with structural biology and drug discovery background
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Proteros Assays, Biophysics and Screening Services

Assays - Enzymatic / Biochemical Services

  • Library screens
  • Orthogonal hit verification
  • Determination of inhibitor activity
  • Biochemical activity data:
    IC50, Ki, EC50
  • Selectivity assessment
  • Mode of inhibition
  • SAR determination

Please check our Gallery Assays database for your target of interest. If that is not available, please inquire for an individual, customized assay development/assay transfer project.

Assays
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Biophysics Services

  • Biophysical assays for target-ligand interaction analysis
  • Library screening (incl fragments)
  • Quantification of binding affinity and/or kinetics: Kd, kon, koff, residence time
  • Orthogonal hit verification
  • Site of ligand binding
Biophysics
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Screening Services

  • A variety of fragment and small molecules libraries are available at Proteros
  • Optionally, commercial third-party libraries and Customer libraries could also be considered for screening
  • Library screening (incl fragments) using enzymatic and biophysical assays
Screening
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Proteros Assay Technologies

Proteros Assay Technologies

  • Reporter Displacement Assay (RDA)
    • Library Screen
    • Time-Resolved Library Screen
    • Affinity Profiling
    • Kinetic Profiling (high precision mode)
    • Kinetic Profiling (high-throughput mode)
    • Profiling of covalent inhibitors
  • Enzymatic Profiling
    • Detection modes: FI, FRET, TR-FRET, FP, Absorbance, Luminescence, AlphaScreen/AlphaLISA
  • NanoBRET (Promega)

Proteros Biophysics Profiling Technologies 

  • Surface Plasmon Resonance (SPR)
  • nanoDSF (Prometheus - NanoTemper)
  • MicroScale Thermophoresis (MST - NanoTemper)
  • Thermoshift Assay (TSA)
  • Isothermal Calorimetry Titration (ITC)

Screening Libraries

  • 3k Proteros hand-selected fragment library
  • 41k fragment enriched small-molecule range finder library
  • 150 k diversity small molecule library
  • 191 k range finder + small molecule library

For Proteros library partnerships or options to screen your own or 3rd party libraries, please contact us.

Assays

Assays

Biophysics

Biophysics

Qualified Hits

Screening

Structure-kinetic relationship of CDK8/CycC "tool compounds" - Case Study


We probed the structure-kinetic relationship of CDK8/CycC using the Proteros RDA for a fragment screen using our Reporter Displacement Assay. The full information insight on binding affinity and binding kinetics allowed for rapid SAR and SKR otimization and allowed for a structure-guided approach to compounds with substantially lower Kd and extended residence time.

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Why use Proteros Assays, Biophysics and Screening

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