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Chemogenomic sets: valuable tools for early-stage drug discovery
Maura Q Schoppa1, David H Drewry1,2
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, U.S.A.
Essays in Biochemistry
|July 30, 2026
Summary
Chemogenomic sets expand small-molecule probe coverage for deeper proteome interrogation. These annotated collections identify therapeutic vulnerabilities and accelerate early-stage drug discovery using machine learning.
Area of Science:
- Biomedical Research
- Chemical Biology
- Drug Discovery
Background:
- Small-molecule chemical probes are vital for studying protein function but have limited proteome coverage.
- Existing tools face limitations in comprehensively interrogating biological systems.
- Chemogenomic sets offer a solution to expand proteome coverage and enable novel research approaches.
Purpose of the Study:
- To review the current landscape of chemogenomic sets.
- To highlight their applications in various research areas.
- To discuss their potential in advancing drug discovery.
Main Methods:
- Summarizing existing literature on chemogenomic sets.
- Categorizing sets by development (open-science, target-class, proteome-wide).
- Analyzing applications in phenotypic screening, target identification, and computational modeling.
Main Results:
- Chemogenomic sets, including open-science and industrial collections, offer expanded proteome coverage.
- These sets enable identification of therapeutic vulnerabilities through polypharmacology.
- Applications span phenotypic screening, target identification, and computational drug design.
Conclusions:
- Chemogenomic sets are powerful resources for target identification in disease pathways.
- Leveraging these sets with machine learning can significantly accelerate early-stage drug discovery.
- Future data generation will further enhance their utility in biomedical research.
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