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Review
. 2024 Oct;29(10):104144.
doi: 10.1016/j.drudis.2024.104144. Epub 2024 Aug 22.

Chemical coverage of human biological pathways

Haejin Angela Kwak  1 , Lihua Liu  2 , Claudia Tredup  3 , Sandra Röhm  3 , Panagiotis Prinos  2 , Jark Böttcher  4 , Matthieu Schapira  5
Affiliations
Free article
Review

Chemical coverage of human biological pathways

Haejin Angela Kwak et al. Drug Discov Today. 2024 Oct.
Free article

Abstract

Chemical probes and chemogenomic compounds are valuable tools to link gene to phenotype, explore human biology, and uncover novel targets for precision medicine. The mission of the Target 2035 initiative is to discover chemical tools for all human proteins by the year 2035. Here, we draw a landscape of the current chemical coverage of human biological pathways. Although available chemical tools target only 3% of the human proteome, they already cover 53% of human biological pathways and represent a versatile toolkit to dissect a vast portion of human biology. Pathways targeted by existing drugs may be enriched in unknown but valid drug targets and could be prioritized in future Target 2035 efforts.

Keywords: GPCRs; Reactome; chemical probes; chemogenomic compounds; human biological pathways; human proteome; kinases.

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