Mechanism of action with cellular evidence
Mechanism of action (MoA) work focuses on understanding how a compound produces its biological effect and whether the intended target drives that effect. Establishing this link is crucial for assessing therapeutic relevance, anticipating potential safety risks, and informing decisions in lead optimization and subsequent development. This phase defines a working mechanistic model that connects target engagement to pathway modulation and observed phenotype.
A central challenge is distinguishing primary target engagement from downstream or compensatory biological responses. Studies are therefore designed to test causality rather than correlation, using appropriate model systems, dose-response experiments, and targeted perturbations. These approaches help clarify whether changes in pathway or phenotypic readouts are a direct consequence of target modulation or the result of alternative mechanisms.
See the full picture with Proteome Wide Profiling
CETSA can be applied in this phase to support direct cellular target engagement and place downstream biology in the correct context. When combined with targeted pathway markers or broader profiling, this approach helps refine MoA hypotheses, identify off-pathway effects, and define the level of evidence required to support progression.
Mechanism of action enabled by our Proteome Wide Profiling Service
Proteome Wide Profiling
Broader investigation of compound effects across the detectable proteome.
The power of Proteome-wide CETSA
Explore case studies on cancer therapies, antimalarial drug targets, and fungal-derived small molecules, showcasing CETSA’s ability to uncover novel targets.
Application of CETSA® to Study the Mechanism of Action of Brefeldin A
In this webinar, you will find the details of the project where CETSA® Explore was leveraged to study the biological mechanism of the fungal polyketide lactone Brefeldin A (BFA) in human THP-1 cells.
What is CETSA?
Why work directly in cells?
Are you using the right tools?
Why early target engagement matters
Let’s talk
For us, every project is a partnership.
Send us a message or book a free scoping call with one of our experts.
A mass spectrometry approach for target ID and compound profiling
In this webinar, you will find a presentation of various applications of CETSA® Explore, highli…
Is Your Hit on Target?
Validate Early with CETSA® Accelerate hit confirmation and lead optimization with CETSA® …
No Target, No Therapy – Target Engagement with CETSA®
Direct Insights into Target Engagement with CETSA® Discover how potency ranking with CETSA help…