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Updated: Jun 28, 2026
05:53
Candidate Gene Testing in Clinical Cohort Studies with Multiplexed Genotyping and Mass Spectrometry
Published on: June 21, 2018
Chemical genomics: massively parallel technologies for rapid lead identification and target validation
Uli Hacksell1, Norman Nash, Ethan S Burstein
1ACADIA Pharmaceuticals Inc., 3911 Sorrento Valley Boulevard, San Diego, CA, 92121, USA, uhacksell@acadia-pharm.com.
Cytotechnology
|November 13, 2008
Summary
This study showcases chemical genomics for drug discovery, linking genomic targets with small molecules. It highlights successful applications in identifying antipsychotic mechanisms and novel receptor agonists.
Area of Science:
- Pharmacology
- Genomics
- Drug Discovery
Background:
- Chemical genomics integrates genomic targets with small-molecule chemistry for efficient drug discovery.
- ACADIA's platform combines a large small-molecule library, genomic targets, and advanced assay technology.
Purpose of the Study:
- To demonstrate the utility of chemical genomics in target validation and lead compound identification.
- To present successful applications of the chemical genomics approach in drug discovery.
Main Methods:
- Utilized a chemical genomics platform with over 800,000 small molecules and >300 druggable genomic targets.
- Employed Receptor Selection and Amplification Technology (R-SAT™) for ultra-high throughput screening and profiling.
- Applied the platform to validate antipsychotic mechanisms and discover novel receptor agonists.
Main Results:
- Validated inverse agonism at serotonin 5-HT2A receptors as a potential antipsychotic mechanism.
- Discovered potent and selective 5-HT2A inverse agonists, now in preclinical development.
- Identified the first ectopically binding, subtype-selective muscarinic m1 agonist.
Conclusions:
- Chemical genomics is a powerful paradigm for accelerating drug discovery and development.
- The presented platform and examples demonstrate significant success in identifying novel therapeutic agents.
- The findings pave the way for new treatments targeting neurological and psychiatric disorders.
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