Protein Degraders
WuXi AppTec utilizes state-of-the-art techniques to support drug discovery teams focused on targeted protein degradation. Our services include a broad range of ligand-finding methods, such as DEL, fragment screening, ASMS, and virtual screening. We provide custom linker design and complex synthesis for new linkers and E3 ligase ligands. To support lead optimization efforts, our platform offers cell-based assays and advanced biophysical and biochemical methods for measuring binary/ternary complex formation and target ubiquitination/degradation.
Bifunctional Molecules: Synthesis, Analysis, Screening
- More than 900 chemists with extensive experience in the synthesis of linkers, E3 ligase ligands, and target protein ligand synthesis since 2016
- >50 methods of prep-HPLC and chiral-SFC for purification
- Comprehensive in-vitro/in-vivo testing platform
- Expertise in versatile linkers synthesis; 100+ linkers readily available
- Novel linker synthesis with high productivity, quality, speed
- Deep experience in CRBN/VHL/IAP/MDM2 and novel E3 ligase ligand synthesis; 30+ CRBN/VHL ligands are readily available
- 30 series of target protein ligands coupled with various linkers
Molecule Synthesis
Scale: from mg to hundreds of kg
> 20,000 compounds synthesized
Library Synthesis
> 100 libraries; 1~5 step parallel synthesis
Rapid turn-around time
Readily available, in stock collection of linkers and E3 ligands
- Modular platform: More efficient synthesis of bifunctional molecules
- Customized synthesis : From mg scale to 200+ kg scale
- In-stock molecules: More than 350 in-stock linkers and E3 ligase ligands
Biochemical and Biophysical assays
WuXi AppTec biology, chemistry and structural biology platforms provide comprehensive solutions to support protein degradation drug discovery research.
Biochemical assays
- Binding/displacement
- Purified protein
- Labeled ligand/antibodies
- Assay formats: FP, FRET or AlphaLISA
Biophysical assays
- Kinetic binding of bifunctional molecules-target binary complex
- Kinetic binding of ternary complex
- Cooperativity measurements
- Assay format: SPR and ITC
Cellular assay
- Binary ligand binding (Target engagement and permeability studies)
- Ternary complex detection (NanoBRET assay in cell and in lysate)
- End point assays: HCS and WB
- Cell line-based validation assays
Binary/Ternary Complex Formation Assay Platform
- Binary/ternary binding assays; formats on TR-FRET, AlphaScreen, Fluorescence Polarization (FP), and radioactive assays.
- Biophysical analysis using SPR (Biacore 8K+) and thermo-shift assays;
- SPR assay measures the kinetics of binary/ternary complex formation and provides rationale for preferred-ternary-complex-formation in bifunctional molecule design and optimization.
PROTAC® is a registered trademark of Arvinas, Inc., and is used under license
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