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High-throughput purification platform in support of drug discovery
Min Liu1, Kuanchang Chen, Denny Christian
1Merck & Company, Rahway, New Jersey 07065, United States. min_liu@merck.com
ACS Combinatorial Science
|October 29, 2011
Summary
Parallel synthesis accelerates drug discovery by enabling rapid structure-activity relationship (SAR) development. A new high-throughput purification platform achieves over 95% purity for 90% of samples.
Area of Science:
- Medicinal Chemistry
- Analytical Chemistry
- Drug Discovery
Background:
- Parallel synthesis is crucial for exploring chemical space and generating structure-activity relationship (SAR) data in drug discovery.
- High-throughput purification is essential to support the large-scale sample processing demands of parallel synthesis.
Purpose of the Study:
- To describe a high-throughput purification platform implemented at Merck's research site.
- To detail the integrated workflow and laboratory information management system (LAF) used for efficient sample processing.
Main Methods:
- Evaluation of crude samples.
- Mass-directed high-performance liquid chromatography (HPLC) purification.
- Fraction analysis, compound registration, purity assessment, and assay distribution.
- Utilizing the Light Automation Framework (LAF) for sample tracking and data management.
Main Results:
- Successful implementation of a high-throughput purification platform.
- Achieved purity of 95% or greater for 90% of processed samples.
- Demonstrated the effectiveness of the integrated workflow and LAF system.
Conclusions:
- The described high-throughput purification platform significantly enhances the efficiency of drug discovery programs.
- The integrated workflow and LAF system are key to achieving high purity and managing large sample volumes.
