Hitgen

Hit ID and Assay

Multiple methods, robust series

We have extensive experience of finding hits using target appropriate methodologies. From biochemical assays, DEL, ASMS, in silico screening, and fragment-based drug discovery (FBDD) – an area in which we are recognised world-leaders. Starting with these techniques, singly or in combination, we have identified hits that have been developed into leads and clinical candidates with our collaborators against a wide range of challenging drug targets.

Hit ID

  • Proprietary fragment library
    • NMR screening:
      • Ligand observed NMR
        • STD, water-LOGSY and relaxation filtered binding experiments
        • 19F relaxation filtered experiments
      • Protein observed NMR
    • SPR screening with Biacore T200 and 8K:
      • Direct binding
      • Affinity In Solution
    • X-ray crystallographic screening
  • Proprietary covalent fragment library
    • Mass spectroscopy screening
  • Photoactivated Capture Fragment DNA Encoded Library (PAC-FragmentDEL)
    • Overcomes limitations of fragment screen by DEL
    • Please click here to learn more about this advanced screening methodology
  • DEL and OpenDEL™ screening
  • MTS screening library (50k lead-like chemical space)
    • Biochemical screening
  • Custom kinase focused library
    • Biochemical and biophysical screening

Assay Technologies

Biochemical Assays

  • TR-FRET (LanthaScreen™, HTRF, LANCE)
  • FRET
  • Fluorescence Polarization
  • Luminescence
  • AlphaScreen™ / AlphaLISA™
  • Absorbance

Biochemical assay development

  • Enzymatic and protein-protein interaction assays
  • Difficult multiprotein complexes
  • Low activity proteins or coupled assay systems
  • Selectivity screening
  • Medium-throughput biochemical screening
  • Mechanistic studies for small molecules, using a range of assay formats
  • Vernalis designed dyes and reporter probes

New technology development

  • Site specific chemical modification of proteins

Meet our colleagues

Hayley Angove DPhil
Senior Team Leader, Assay Technology
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