Advanced cell-based assays to shape the profile of your hits
We routinely utilise an array of specialised assays to narrow down an existing list of hits or to further characterise a selected number of hits already advanced in the hit-to-lead process:
- Off-target and species selectivity assays
- NanoBRET/Nano-Glo target engagement for a wide variety of membrane or intracellular targets
- Tag-lite binding for GPCRs
- Cellular thermal shift assays (CETSA) for label-free target engagement in cells
- Kinetic probe competition assays (kPCA) for different target types, such as enzymes, protein–protein interactions or GPCRs
- Residence time assays using high-content analysis
- Rescue experiments on different assay platforms. For example, in a protein degrader project, determining whether the observed protein level decrease is due to proteasomal degradation can be achieved by running the degradation assay in the presence of specific proteasome or E3-ligase inhibitors.