Fragment screen

screen

Gene2Lead has established a robust thermal shift assay protocol for fragment screening

  • Ligand-induced thermal stabilization; difference in melting points of the protein and protein-ligand complex is measured
  • No further assay development needed
  • Fast – cherry picked fragment library of 560 compounds screened and verified within few weeks
  • Reliable – low number of false positives
  • Other methods such as NMR, SPR, X-ray screening or high-concentration screening can be performed as either primary or secondary assays
Melting curves in the absence or presence of ligand
Fragment Screening by Protein Stability Measurements
Two methods to detect thermal denaturation
─ Fluorescence-based method
─ Light-scattering based method (entirely label-free)
Generic assays that require very little optimization (if any)