Chemical biology and proteomic strategies have rapidly emerged as cost effective yet powerful preclinical approaches for the discovery and identification of novel drugs and targets. Advances in the development and combination of novel chemical tools, bioorthogonal techniques, disease-relevant phenotypic systems, chemoinformatics, and chemical proteomics now provide robust and high-throughput workflows for interrogating drug-target-phenotype relationships. These efforts are poised to significantly enrich preclinical discovery programs and are illuminating a new paradigm for the development of novel drugs modulating novel targets.

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