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Assays, Biophysics and Screening Technologies

 

Proteros can provide, full biochemical and biophysical characterization of ligand-target interactions for even the most challenging drug discovery projects.

Assays, Biophysics and Screening Technology

The Proteros Reporter Displacement assay (RDA)

 

Screenshot 2021-05-16 at 14.44.21

 

  • Objective: Identification of binders
  • Deliverables: probe displacement [%]
  • Time line: up to 100,000 compounds/week
  • Applications: Primary screen
  • Objective: Identification of binders + parallel separation of slow and fast binders
  • Deliverables: probe displacement [%] at 2 time points
  • Time line: up to 70,000 compounds/week
  • Applications: Primary screen identification of binders & separation of
    slow and fast binders
  • Objective: Quantification of binding affinities
  • Deliverables: Kd
  • Timeline: up to 1,000 compounds/week
  • Applications: Hit Profiling, orthogonal screening, lead optimization
  • Objective: Quantification of binding affinities and kinetics
  • Deliverables: Kd, kon, koff, residence time
  • Timeline: up to 200 compounds/week
  • Applications: Hit profiling, lead optimization, candidate selection
  • Objective: Identification of compounds with desired kon and residence time
    within large compound selections
  • Deliverables: Clustering of kon, koff, residence time
  • Timeline: up to 2,500 compounds/weeks
  • Applications: Kinetic profiling of entire hit compounds sets from HTS campaigns

Profiling of Covalent Inhibitors

Objective: Verification of covalent bond formation, kinact & Ki quantification

Deliverables: probe binding signal after cpd-target pre-incubation,  kinact & Ki

Applications: Hit profiling, lead optimization
Enzymatic Profiling and NanoBRET (Promega)
  • Technologies: FI, FRET, TR- FRET, HTRF, FP, Abs, Luminescence, AlphaLisa &
  • Alpha-Screen (PerkinElmer), Transcreener (BellBrook Labs), IMAP, ADP GLO (Promega) etc.
  • Deliverables: IC50, Ki, Lineweaver Burk analysis, mode of action studies, enzymology
  • Applications: Primary screen, hit profiling, lead optimization
  • Throughput: Screen: up to 100,000 ligands/week, IC50: up to 1,000 ligands/week
  • Technologies: nanoBRET
  • Deliverable: EC50
  • Applications: Primary screen, hit profiling, lead optimization,
  • cellular target engagement
  • Throughput: Screen: up to 6,000 ligands/week, IC50: up to 600 ligands/week
  • Objective: Verification of covalent bond formation, kinact & Ki quantification
  • Deliverables: probe binding signal after cpd-target pre-incubation kinact & Ki
  • Applications: Hit profiling, lead optimization

Biophysics Technologies at Proteros
  • The Proteros Reporter Displacement Assay (RDA)
  • Gallery Assays
  • Enzymatic Profiling and NanoBRET (Promega)
  • Surface Plasmon Resonance (SPR / Biacore 8k+)
  • Isothermal Calorimetry Titration (ITC) / Malvern MicroCal PEAQ ITC
  • nanoDSF (NanoTemper)
  • TSA
  • MicroScaleThermophoresis (MST / NanoTemper)

Proteros in-house libraries in collaboration with Enamine

 

  • 3k hand-selected Fragment library
  • 41k fragment-enriched small molecules Range Finder Library
  • 150k high-quality small molecule Library
  • 191 k high-quality small molecule (fragment enriched) Range Finder & Small Molecule Library

Please inquire on our DNA-encoded library options regarding our collaboration with X-Chem !

  • 3k Proteros hand-selected fragments
  • Ro3 compliant, MW 160-
    300 g/mol, solubility
    checked
  • High diversity, max
    Tanimoto similarity of 0.66
  • High concentration collection (200 mM DMSO stock concentration
    -> up to 1 mM screening concentration)
  • Application: Fragment screening
  • Fragment enriched 41k small molecules library
  • Fragment enriched (25% MW
    < 300 g/mol
  • Sorted by size: 10,000 Fragments
    can be screened separately
  • High sp3 fraction,
    average sp3 fraction = 0.42
  • Applications:
    Combination of fragment and small molecule screen
    Screen of smaller library with high hit rates.
  • 150k high-quality small molecules
  • High diversity
  • Specific clustering concept (23,598 clusters, mean cluster size = 6)
  • Additional cluster members available by expansion into full range of Enamine compounds
  • Application: HTS
  • 191k high-quality small molecules (fragment enriched)
  • Combination of range finder and small molecule diversity library
  • Application: HTS

Please inquire !

Proteros Structural Biology Stats

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