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The concept Click chemistry was introduced by K. Barry Sharpless in 2001 and honored with the 2022 Nobel Prize in Chemistry, comprises a class of highly efficient, selective, and bioorthogonal reactions that facilitate the rapid construction of complex molecular architectures under mild conditions. This review examines the role of click chemistry throughout the drug discovery and development pipeline, ranging from fragment-based lead identification and combinatorial library generation to targeted drug delivery, fabrication of antibody–drug conjugates (ADCs), prodrug activation, chemical proteomics, and radiopharmaceutical applications. The mechanistic aspects of key click reactions—including copper-catalyzed azide–alkyne cycloaddition (CuAAC), strain-promoted azide–alkyne cycloaddition (SPAAC), tetrazine ligation, and thiol–ene reactions—are discussed, along with a critical assessment of their benefits, limitations, and progress toward clinical translation. Additionally, emerging areas such as DNA-encoded chemical libraries, covalent drug discovery, and in vivo bioorthogonal chemistry are highlighted.
Keywords:
Click chemistry, bioorthogonal chemistry, azide-alkyne cycloaddition, antibody-drug conjugates, drug delivery, chemical proteomics, fragment-based drug discovery
Cite Article:
"Application of Click Chemistry in Drug Discovery and Development", International Journal for Research Trends and Innovation (www.ijrti.org), ISSN:2456-3315, Vol.11, Issue 4, page no.a526-a528, April-2026, Available :http://www.ijrti.org/papers/IJRTI2604071.pdf
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ISSN:
2456-3315 | IMPACT FACTOR: 8.14 Calculated By Google Scholar| ESTD YEAR: 2016
An International Scholarly Open Access Journal, Peer-Reviewed, Refereed Journal Impact Factor 8.14 Calculate by Google Scholar and Semantic Scholar | AI-Powered Research Tool, Multidisciplinary, Monthly, Multilanguage Journal Indexing in All Major Database & Metadata, Citation Generator