
PROTACs and molecular glues introduce distinct design and optimization challenges, including molecular complexity, cellular activity and developability considerations. At Concept Life Sciences, our multidisciplinary team use advanced Computer Aided Drug Design (CADD) and Direct-to-Biology (D2B) workflows to drive coordinated design–make–test cycles, confident decision-making and faster progress.
Targeted Protein Degradation (TPD) is redefining what is druggable. By harnessing the cell’s ubiquitin-proteasome system, modalities such as PROTACs (proteolysis targeting chimeras) and molecular glues enable selective removal of disease-causing proteins, including targets previously considered undruggable.
Unlike traditional small molecule inhibitors that transiently block protein activity, PROTACs and molecular glues drive target protein degradation, offering improved potency and durability of response, access to non-enzymatic and scaffolding proteins and expanded therapeutic space beyond conventional binding pockets.
From rational PROTAC design to molecular glue discovery strategies, we help you unlock the full potential of targeted degradation biology.
TPD therapeutic discovery and development presents distinct challenges compared with small molecules, requiring unique capabilities and expertise.
Our approach is built around fully integrated workflows that combine medicinal chemistry, advanced computational chemistry (CADD), protein science, in vitro biology and DMPK expertise, and incorporates Direct-to-Biology (D2B) workflows to overcome PROTAC and molecular glue-specific challenges, streamline design–make–test cycles and reduce time to decision.
Direct to biology (D2B) is an approach for rapidly exploring chemistry space, identifying hits and validating biological activity quickly. Compared to conventional methods of PROTAC synthesis, D2B provides cost and time savings enabled by a 10-fold reduction in reaction scale combined with optimized processes.
View our poster to see how we applied a D2B approach to enable rapid exploration of linker intermediates, providing a time- and cost-effective route to PROTAC optimization.
Small changes to structure can have large, unpredictable effects on degradation. CADD helps navigate this complexity by enabling the team to focus on few, better designed PROTACs, accelerating early discovery.
By combining computational insight with experimental validation, we enable a more predictive and efficient approach to PROTAC discovery.
Bespoke screening strategies are used to identify glue-like degraders, supported by:
With specialist expertise and capabilities, we understand the unique challenges presented by TPD therapeutic discovery and development, and build sophisticated integrated workflows to directly address these.
Our multidisciplinary teams work in iterative design-make-test cycles to reduce timelines, de-risk decision-making and accelerate progression toward candidate nomination.
A: Targeted protein degradation (TPD) is a therapeutic approach that uses the cell’s ubiquitin–proteasome system to selectively remove disease-causing proteins. Modalities such as PROTACs and molecular glues enable degradation of targets that are difficult or impossible to inhibit with traditional small molecules.
A: PROTAC drug discovery is more complex because it depends on ternary complex formation between the target protein, PROTAC, and an E3 ligase. Small structural changes can significantly impact degradation, making optimization less predictable than traditional small molecule approaches.
A: Yes. Concept Life Sciences provides integrated support from hit identification and design through optimisation, mechanistic profiling, and developability, helping accelerate programs toward candidate selection.
A: D2B enables rapid synthesis and immediate biological testing of compounds, reducing reaction scale by up to 10× and delivering faster insight into functional degradation activity.
Discover how Concept Life Sciences can help you rapidly progress your targeted protein degraded program today. Contact us today for a confidential discussion with our team of expert scientists.