PROTAC & Molecular Glue Services: Targeted Protein Degradation Solutions
PROTAC Platform
Overview
What Are PROTACs?
PROTACs (Proteolysis Targeting Chimeras) and molecular glues represent a new therapeutic frontier in targeted protein degradation (TPD). Unlike traditional inhibitors, these bifunctional or monofunctional degraders harness the body’s ubiquitin-proteasome system to remove disease-causing proteins entirely.
Why PROTAC Matters?
Enhanced Selectivity & Efficacy
Targeted degradation ensures precision by sparing healthy proteins
Resistance Mitigation
Effectively combats mutated proteins that evade traditional inhibitors
Broad Applications
From oncology to autoimmune disorders, PROTACs are reshaping drug discovery
Modality
Mechanism
Advantages
- PROTACs
- Molecular Glues
These modalities offer transformative potential in oncology, immunology, and neurodegenerative diseases.
our Promise
Medicilon’s Full-Stack PROTAC Drug Discovery Platform
Medicilon provides an integrated TPD service platform covering PROTACs, molecular glues, and novel modalities (DACs). Our services are designed to move clients from hit discovery to IND submission with speed, precision, and scientific rigor.
E3 Ligand Synthesis & Screening
150 novel ligase ligands (CRBN, VHL, and beyond)
Linker Design & Optimization
>300 linker chemotypes (PEG, spirocyclic, fused ring, acid- and amine-based) developed to fine-tune PROTAC performance
Custom PROTAC Assembly
Modular, block-based assembly enables rapid design and optimization cycles
Biophysical, Biochemical & Cell-Based Assays
Full assay suite for binary/ternary complex formation, degradation kinetics, and functional validation
Platform Capabilities
E3 Ligase Ligand Library
Medicilon developed 150+ novel ligands targeting CRBN and VHL, enabling SAR-driven optimization of selectivity, potency, and DMPK profiles. These ligands also supported the exploration of tissue-specific ligases to improve therapeutic index.
How Does Medicilon’s PROTAC Workflow Work?
Medicilon offers a seamless workflow from target validation to preclinical candidate nomination (PCC) and IND enabling.
Workflow Stages
- Target & E3 Selection
- Ligand & Linker Synthesis
- Custom PROTAC or Glue Design
- In Vitro Biochemical & Cellular Assays
- PK/PD & In Vivo Studies & Efficacy Models
- Preclinical Candidate (PCC) Nomination
- IND-Enabling Studies and Filing
Fast-Track Advantage: Our integrated approach delivers a 3x faster cycle time from lead to PCC.
Preclinical Services: In Vitro and In Vivo Evaluation
Case study
Case Study 1: EGFR-PROTAC Program
TB015, an EGFR-targeting PROTAC, demonstrated potent degradation across triple EGFR mutants, superior PK in multiple species, and tumor regression in CDX models.
TB015 shows potent EGFR degradation across single, double, and triple mutants, with low IC50 values and superior biochemical and cellular activity.
Case Study 2: Molecular Glue GT919 for IKZF1/3
GT919 is a molecular glue developed at Medicilon targeting transcription factors IKZF1 and IKZF3 via Cereblon (CRBN):
- Binds to CRBN and promotes IKZF1/3 ubiquitination and degradation
- Demonstrates anti-tumor and immunomodulatory effects
- Designed to overcome resistance to thalidomide analogs (lenalidomide, pomalidomide)
- Currently advancing in clinical trials with support from Medicilon’s chemistry and assay teams
Additional Molecular Glue Projects
Medicilon supports diverse glue targets across global biotech collaborations:
New Modality Highlight: Degrader–Antibody Conjugates (DACs)
DACs follow ADC principles but deliver degrader payloads for selective tumor targeting:
- Mechanism: Antibody delivers PROTAC/molecular glue to tumor; payload is released intracellularly
- Improves efficacy by enhancing tumor selectivity and minimizing systemic exposure
- Medicilon has developed and validated DAC constructs for multiple clients
Custom PROTAC Design & Optimization
Medicilon specializes in custom degrader design, tailoring PROTACs to novel oncology and immunology targets.
- SAR-guided linker engineering
- Optimization for potency, selectivity, and stability
- Novel modalities: Degrader–Antibody Conjugates (DACs)
Case Study 3: Novel Linker for Oncology Target
Medicilon optimized a spirocyclic rigid linker, improving degradation efficiency 3-fold compared to conventional PEG-based linkers.
PEG-based linkers
Spirocyclic rigid linkers
Validated Assay platforms for TPD
Medicilon’s integrated assay suite support every stage of degrader validation:
Assay Type | Techniques Included |
Biophysical | SPR (BiacoreTM 8000), TR-FRET, AlphaScreen, FP |
Biochemical | Ubiquitination & degradation assays, radioactive labeling |
Cell-Based | HiBiT, NanoBRET, Western blotting, in-cell Western, MSD, ELISA, degradation kinetics (DC50) |
Example: Degradation Kinetics Validation
Using HiBiT and in-cell Western assays, Medicilon demonstrated potent degradation of BRM degrader in MV-4-11 cells, correlating with strong anti-tumor efficacy.
In Vivo Proof-of-Concept
PK/PD Studies
Toxicology & Safety
END TO END Support
Medicilon’s Advantages in PROTAC & Molecular Glue Discovery
Experienced Team
200+ chemists, >40% MS/PhD, average >8 years’ TPD experience
IP & EHS Commitment
- Dedicated EHS department ensuring reaction/reagent safety
- Robust IP security policy and project confidentiality enforced
Track record
PCC nominations and IND-enabling studies delivered for global clients
State-of-the-art instrumentation
BiacoreTM 8000, UPLC-MS, NMR, SPR platforms
Frequently Asked Questions
FAQs on PROTAC Drug Discovery Services
What is the difference between PROTACs and molecular glues?
PROTACs are modular bifunctional degraders, while molecular glues stabilize natural E3 ligase–substrate interactions. Both enable targeted protein degradation but differ in design and discovery strategy.
What therapeutic areas are best suited for PROTAC technology?
Oncology, immunology, neurodegenerative diseases, and resistant cancer mutations are primary areas where PROTACs and molecular glues show strong promise.
How does Medicilon accelerate PROTAC programs compared to competitors?
Our integrated chemistry–biology platform, advanced assays, and track record of successful IND filings allow us to shorten discovery cycles by up to 3x.
Does Medicilon provide E3 ligase screening services?
Yes, Medicilon has developed and optimized >150 E3 ligase ligands and offers full screening, SAR optimization, and novel ligase exploration services.
Can Medicilon support custom PROTAC design for novel targets?
You can request a scientific consultation or custom CRO proposal to align with your project needs.
How can I engage Medicilon for a PROTAC project?
Our PROTAC studies are aligned with global regulatory requirements, providing robust data future innovation
Ready to consult Medicilon’s expertise in PROTAC?
Medicilon is ready to transform your research with its unparalleled PROTAC technology and expertise
