Our Lead Optimization Services:
Potency Ranking
Potency ranking is essential in the lead optimization phase of drug discovery for selecting and refining compounds with strong target engagement.
CETSA measures how well a compound binds to its target in intact, biologically relevant cells, ensuring relevance to disease models. This helps establish a clear link between cellular target engagement and functional readouts, helping to establish a clear Structure-Activity Relationship (SAR) and ensuring that potency improvements translate into biological effects.
Key Benefits
- Biologically Relevant Potency Data – Measure target engagement in intact cells, ensuring potency rankings reflect real-world disease models.
- Stronger SAR Development – Establish a clear relationship between compound binding and functional biological effects.
- Reduced Late-Stage Attrition – Prioritize compounds with verified cellular target engagement to lower the risk of failures in later development stages.
Selectivity Profiling
Selectivity Profiling allows researchers to assess compound binding across individual proteins and entire biological pathways, offering insights beyond the limitations of conventional target panels. Given that many drug candidates interact with multiple physiological targets, our approach helps reveal off-target effects that traditional screening methods often miss.
Key Benefits
Flexible Service Options – Choose between fully customized profiling or a faster, standardized service in lysate.
Comprehensive Off-Target Detection – Unbiased, proteome-wide profiling reveals off-target interactions missed by conventional panels.
Enhanced Drug Safety and Efficacy – Ensure selective binding to the correct targets, minimizing potential liabilities early in development.
Target Deconvolution
This powerful approach allows for a comprehensive analysis of compound-target interactions in conditions that reflect actual cellular environments. Our methodology delivers key insights into target engagement, pathway modulation, and mechanistic action—empowering data-driven decision-making in phenotypic drug discovery tailored to your disease-relevant system.
Key Benefits
Minimized Off-Target Risks – Detect and reduce potential off-target effects early, improving the likelihood of therapeutic success.
Unbiased Target Identification – Comprehensive, proteome-wide profiling captures direct and indirect interactions in a physiologically relevant context.
Enhanced Mechanistic Insight – Clarify a compound’s mechanism of action, supporting informed decisions on candidate progression.
Mechanism of action
This data-driven approach enables a comprehensive understanding of compound-target interactions in a physiologically relevant context. Our methodology helps validate MoA hypotheses, refine drug candidates, and accelerate decision-making throughout preclinical and clinical development.
Key Benefits
Accelerated Candidate Validation – Make faster, data-driven decisions during preclinical and clinical development.
Precise Mechanistic Insight – Distinguish between primary target engagement and downstream effects for greater confidence in therapeutic relevance.
Comprehensive Interaction Profiling – Gain a clear understanding of compound activity across the proteome in biologically relevant conditions.
Translational studies
With Pelago Bioscience’s CETSA®-powered translational services, you can seamlessly extend your research from simplified systems to biologically relevant contexts. Our technology measures target engagement directly within cell lines, animal tissues, and human primary cells—providing a clear picture of how your compound performs in environments that better reflect real-world conditions. These insights help you make confident, evidence-based decisions, increasing the likelihood of clinical success and reducing the risks associated with trial failures.
Key Benefits
Streamlined Progression to Clinical Trials – Make informed, data-driven decisions that minimize costly trial failures and accelerate development timelines.
Physiologically Relevant Validation – Confirm target engagement across cell lines, animal tissues, and human-derived systems for reliable translational insights.
Reduced Development Risk—Validating efficacy in complex biological environments Strengthens confidence in your compound’s clinical potential.