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Integrity profiling of high throughput screening hits using LC-MS and related techniques
Edward H Kerns1, Li Di, Jim Bourassa
1Chemical and Screening Sciences, Wyeth Research Princeton, NJ 08543-8000, USA. kernse@wyeth.com
Combinatorial Chemistry & High Throughput Screening
|September 24, 2005
Summary
Integrity profiling verifies high-throughput screening (HTS) hits, ensuring identity and purity for confident drug discovery. This review covers analytical methods for efficient, structure-based data crucial for early research.
Area of Science:
- Analytical Chemistry
- Drug Discovery
- Biochemistry
Background:
- High-throughput screening (HTS) identifies potential drug candidates.
- Verification of HTS hit identity and purity is critical for reliable structure-activity relationship (SAR) studies.
- Early confirmation of hit integrity enhances the efficiency of drug discovery pipelines.
Purpose of the Study:
- To review analytical techniques for integrity profiling of HTS hits.
- To assess methods for their suitability in high-throughput, low-material consumption workflows.
- To identify techniques providing structure-based data for hit verification.
Main Methods:
- Review of established and emerging analytical techniques.
- Evaluation of methods based on criteria: sample preparation, separation, detection, quantitation, and identity confirmation.
- Assessment of suitability for high-throughput screening (HTS) environments.
Main Results:
- Certain analytical techniques are well-suited for HTS hit integrity profiling.
- Methods vary in their ability to provide purity quantitation and identity confirmation.
- High-throughput, low-sample-consumption techniques are essential for early discovery.
Conclusions:
- Effective integrity profiling of HTS hits is vital for confident SAR development.
- The choice of analytical methodology impacts the reliability and speed of early drug discovery.
- Further optimization of analytical techniques can improve HTS hit validation.