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Hit-to-Lead Optimization:
A succesful Collaboration in Drug Discovery

At Pivot Park Screening Centre, we recently partnered with a customer on their hit-to-lead optimization project, providing key services that accelerated their path from hit identification to lead candidate selection. Our scope included validating target engagement, testing and monitoring improvements in potency and other pharmacological parameters, and addressing the novel hit analogs’ selectivity, specificity, and safety liabilities in structure-activity relationship (SAR) cycles.

Feasibility Study: Ensuring a Strong Start

Our involvement began with the development of a customized assay, followed by a detailed feasibility study assessing the suitability of various assay formats for hit-to-lead profiling. This initial step was crucial in ensuring that the project moved forward with the best possible experimental setup. By leveraging our experience with target-specific and phenotypic assays, we provided our customer with a clear plan for the profiling process, minimizing risks and maximizing the chances of success.

We have a wide range of read-out modalities (fluorescence intensity, luminescence, absorbance, etc., as well as mass spectrometry and high-content analysis) in-house, which enabled flexibility in our approach. Therefore, the assays could be adjusted as the project evolved. Besides, by optimizing the assays we ensured that we got robust and reliable data. 

Compound Profiling: Insights into Structure-Activity Relationships

Our profiling services focused on providing detailed structure-activity relationship (SAR) data. By testing the potency (IC50/EC50 values), specificity, and selectivity of hit analogs, we helped the customer identify the most promising compounds for further development.

We conducted regular profiling of the customer’s compound series, ensuring that any changes made by their medicinal chemists were quickly evaluated in the biological assays. This iterative process provided the data necessary for the customer to make informed decisions about which compounds to prioritize for lead development.

A Collaborative Success Story in Hit-to-Lead Optimization

Our customer successfully advanced the hit-to-lead optimization project by working together with Pivot Park Screening Centre. Our tailored assay solutions, detailed compound profiling, and data analysis provided the foundation for the customer’s medicinal chemistry team to refine their compounds and identify the most promising candidates for preclinical development.

Conclusion: Expertise and Flexibility for Your Hit-to-Lead Project

If you’re looking for a partner to support your hit-to-lead optimization efforts, Pivot Park Screening Centre can provide the expertise and flexibility needed for a successful outcome. Our services allow you to focus on what matters most – advancing your compounds to the next phase of drug discovery.

Contact us to learn how we can assist with your hit-to-lead optimization project.

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