Verify target
engagement in
live tissue
In vivo target engagement studies assess whether a compound binds its intended molecular target in relevant organs under physiological conditions. This phase focuses on selecting appropriate tissues, defining sampling windows, and interpreting engagement in relation to systemic exposure. Studies are designed with treated and control cohorts, predefined dose levels, and time points aligned to expected pharmacokinetics to ensure results are meaningful and comparable.
Experimental design decisions center on which tissues and anatomical sites best reflect the pharmacology of interest, as well as how dose levels and time points are chosen to characterize concentration–engagement relationships. Tissue handling procedures, matrix effects, and sources of biological variability are addressed upfront, alongside specificity controls and confirmatory analyses to distinguish true target engagement from nonspecific or artifactual signals.
Measure what matters: Targeted Profiling
CETSA can be applied in this phase to quantify target engagement on the native protein directly in tissues, providing effect sizes that can be compared across organs and conditions. These data help define thresholds for meaningful engagement at the site of action and support dose selection, endpoint choice, and progression decisions ahead of IND-enabling studies.
In vivo target engagement is enabled by our Targeted Profiling Service
Targeted Profiling
Validate mechanistic hypotheses and confirm that on-target engagement occurs in the intended cellular context.
Webinar: How AbbVie used CETSA to elevate their drug discovery
In this webinar, you’ll learn about flow-based CETSA, a powerful, high-throughput technique that enables single-cell target engagement analysis without cell lysis. In the second half of the webinar, you will learn about novel Alpha and MSD CETSA formats for whole blood, using RIPK1 as a proof-of-concept.
Is your compound actually therapeutic?
Learn how CETSA confirms target engagement across cell lines, animal models, and human primary cells—providing physiologically relevant insights that streamline drug discovery.
What is CETSA?
Why work directly in cells?
Are you using the right tools?
Why early target engagement matters
Let’s talk
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Send us a message or book a free scoping call with one of our experts.
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