Tackling the chemogenomic space by novel screening technologies.

Area of Science:

• Drug discovery and chemogenomics
• High-throughput screening (HTS) technologies
• Biochemical assay development

Background:

• The chemogenomic space has expanded significantly, increasing the need for efficient compound testing.
• Conventional screening technologies face limitations with certain drug targets.
• Advancements in screening necessitate novel readout technologies for drug discovery.

Purpose of the Study:

• To introduce two novel high-throughput screening (HTS) technologies developed by Novartis: NanoScreen and SpeedScreen.
• To demonstrate the capabilities of these systems in accelerating compound testing and enabling access to difficult drug targets.
• To highlight the impact of these technologies on chemogenomic research.

Main Methods:

• NanoScreen: A miniaturized, automated HTS/uHTS system with single-molecule and non-confocal detection for functional screening (1-5 microl/sample).
• SpeedScreen: A miniaturized, automated system for high-throughput affinity selection using size-exclusion chromatography and microbore RP-HPLC.
• Integration of advanced readout technologies for high-quality, multi-parameter data.

Main Results:

• Successful development and implementation of NanoScreen and SpeedScreen at Novartis Lead Discovery Center (LDC).
• Enabled screening of previously inaccessible targets, including expensive and 'orphan' drug targets.
• Facilitated sophisticated biochemical assays with high data quality through single-molecule detection.

Conclusions:

• NanoScreen and SpeedScreen represent significant advancements in HTS technology.
• These novel systems overcome limitations of conventional screening, expanding possibilities in drug discovery.
• The technologies enable novel approaches in chemogenomic research, previously unattainable.