From Target Engagement to Function: An Integrated in vivo Platform for CNS Drug Discovery

Successful CNS drug discovery depends on understanding more than target engagement alone. To make informed decisions, researchers need to connect receptor occupancy and brain exposure with changes in neurochemistry and ultimately functional outcomes.

Building a complete picture of CNS pharmacology

Establishing clear links between target engagement, exposure, neurochemistry, and efficacy often requires multiple studies across different disciplines. Integrating these data streams can provide a more complete understanding of compound activity and support better-informed development decisions.

By bringing together complementary approaches within a single workflow, researchers can gain a more comprehensive understanding of compound activity and make better-informed decisions earlier in development.

Our integrated CNS platform combines:

• Receptor binding and occupancy studies to confirm target engagement
• Pharmacokinetic and brain exposure assessment
• Real-time neurochemical monitoring using in vivo microdialysis
• Behavioral profiling to assess pharmacological activity and potential liabilities
• Integrated analysis linking receptor occupancy, neurotransmitter modulation, and functional outcomes

Together, these capabilities support the identification of translational biomarkers, strengthen confidence in mechanism, and enable data-driven progression decisions.

Linking receptor occupancy to functional outcomes

Using antipsychotic compounds as an example, this work demonstrates how receptor occupancy data can be connected to neurochemical changes and behavioral responses. By combining these complementary datasets, researchers can better understand mechanism of action, strengthen confidence in candidate selection, and reduce development risk.

Accelerating smarter CNS drug discovery

Rather than evaluating target engagement, neurochemistry, and functional outcomes in isolation, an integrated approach enables a more holistic assessment of CNS-active compounds. The result is stronger decision-making, improved translational understanding, and greater confidence when advancing molecules through discovery and development.

Download the poster to explore how an integrated in vivo CNS platform enables informed decision making and de-risks CNS drug discovery programs.