Targeted Protein Degraders - PROTACS

Our chemistry team has extensive experience in the design and synthesis of Proteolysis Targeting Chimeras (PROTACs), including the development of various E3-ligase ligands such as CRBNs, VHL and cIAP1. We can develop novel structural analogues, while ensuring drug-like characteristics.

Our PROTAC synthesis capabilities include:

  • Design and synthesis of PROTAC libraries around the target scaffolds
  • Development and functionalization of novel linkers
  • Optimization of physicochemical, PK-PD and toxicology parameters
  • In-house library of diverse linkers
  • Chemistry and integrated discovery support

Our in-house collection of novel linkers and E3 ligase ligands offers an efficient way to jump-start drug discovery programs.




Ternary complex formation

Target and E3 ligase engagement and ternary complex formation

Target Degradation

Target Ubiquitination

Our discovery biology expertise for PROTAC screening includes:

  • Binding- Fluorescence Polarization/TR-FRET
  • Ternary complex formation (cell-free)- ALphaLISA
  • Target engagement- NanoBRET
  • Ternary complex formation (cell-based)- NanoBRET
  • Target Ubiquitination- NanoBRET ubiquitination assay
  • Target degradation- NanoBiT system and western blot
  • Xenograft studies and other PD models