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.
Cell-Free
Cell-Based
Binding
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