Tools for fragment based drug discovery

TINS

< Fragment Screening

TARGET IMMOBILIZED NMR SCREENING


TINS_ani

TINS has been validated on a wide range of targets including viral proteins, proteases, kinases, Protein-Protein Interaction targets, molecular chaperones and membrane proteins such as GPCRs.

TINS uses a single sample of the target and a reference protein that have been immobilized on sepharose based resin. Screens are carried out by repeated cycles of i) fragment application, ii) assaying for binding and iii) fragment removal.

 

KEY FEATURES

  • Applicable to a broad range of targets, including unstable proteins and membrane proteins.
  • Requires only a single sample of the target, between 10-20 nmol.
  • Targets are functionally immobilized using various conjugation techniques.
  • Comparative technique, i.e. use of a reference protein: high level of ligand specificity.
  • Direct detection of binding, no deconvolution required.
  • Fast: 1,500 compounds screened in 3-4 days, complete hit discovery project finished within 1-2 months.
  • Possibility to screen a customers library.

 

PUBLICATIONS


< Fragment Screening