Synthesizing and screening a PROTAC library is time and resource intensive. Our direct-to-biology (D2B) approach enables the rapid exploration of chemical space, identification of hits, validation of biological activity and early DMPK analysis. What would previously take weeks or even months can now happen within days.
Using this streamlined approach, coupled with our partial PROTAC library, enables the rapid identification of potential degraders.
Why Use a Direct-to-Biology (D2B) Approach for PROTAC Discovery?
Used in combination with our partial PROTAC library, the semi-automated direct-to-biology (D2B) approach offers:
- Fast synthesis of a PROTAC library using your POI-Ligand
- Rapid biological evaluation of the crude reaction mixtures
- Initial ADME/DMPK screening
All conducted within a plate and reducing the cycle of PROTAC optimization to days.
Direct-to-Biology Workflow
Our concise D2B approach is customized and optimized to suit your PROTAC project’s needs before the workflow commences. Once optimized you can obtain hit finding results in as little as five days, depending on the chemistry and assays required. With hit finding accelerated, key decision points occur earlier than when using traditional methodologies, saving you both time and money.
This process means:
- Plates of compounds can be efficiently synthesized and screened
- Data is easily visible through a heat-map overview indicating the quality of the plate
- Hits can be identified and preliminary ADME / DMPK data can be obtained
By combining plate-based chemistry and our ability to quickly complete biological screening, results can be turned around swiftly. This process is made easier by all our labs being located “under-one-roof”, enabling easy collaboration between teams. By being able to walk the plates between departments, and sharing a plate if required, we don’t waste time preparing extra plates and shipping.
Read more about how our “under-one-roof” workflow has helped other projects in our case study.
D2B for PROTACs at Charnwood Discovery
Project and Data Management
Understanding that PROTAC compounds present particular challenges during aspects of the drug discovery process is key when developing a direct-to-biology approach. By having strong project management with expertise in the unique challenges TPD programs present, we ensure:
- Seamless Cross-Functional Collaboration: Our team coordinates chemistry, biology, and ADME/DMPK activities for a streamlined approach, keeping all stakeholders aligned and focused on your drug discovery goals.
- Efficient Timeline & Risk Management: We set clear milestones within the project team and address potential risks early, ensuring timely delivery of key results while maintaining the flexibility to adapt to new data or challenges.
- Transparent Communication: Regular, clear updates and actionable insights keep you informed.
- Robust Data Management & Decision-Making: Leverage data-driven insights to prioritize tasks and make informed decisions. Our streamlined data management ensures real-time access to critical project data, keeping all teams aligned and progressing the drug discovery program.
Direct-to-Biology Resources
Our recent posters the first outlines our integrated direct-to-biology approach using a HiBit assay with the second illustrating the use of the NanoLuc® assay for effective screening.
- Accelerating PROTAC Development: A Direct-to-Biology Approach for Rapid Synthesis and Profiling of PROTACs
- Speeding up PROTAC Development: A Direct-to-Biology Approach
We have a range of TPD and PROTAC resources some of which you can view here:
