HomeADC & BioconjugationIntroduction to Click Chemistry

Introduction to Click Chemistry

A "Click" Away from Discovery

The traditional process of drug discovery based on natural secondary metabolites has often been slow, costly, and labor-intensive. Even with the advent of combinatorial chemistry and high-throughput screening in past decades, the generation of leads is dependent on the reliability of the individual reactions to construct the new molecular framework.

Click Chemistry Mechanism

Click chemistry is a newer approach to the synthesis of drug-like molecules that can accelerate the drug discovery process by utilizing a few practical and reliable reactions. Sharpless and coworkers defined what makes a click reaction as one that is wide in scope and easy to perform, uses only readily available reagents, and is insensitive to oxygen and water. In fact, in several instances, water is the ideal reaction solvent, providing the best yields and highest rates. Reaction work-up and purification uses benign solvents and avoids chromatography.1

Click Chemistry Reaction Processes

  • Simple to perform
  • Modular
  • Wide in scope
  • High yielding
  • Stereospecific
  • Adheres to the 12 Principles of Green Chemistry by generating harmless byproducts, removable by nonchromatographic methods

Click Chemistry Reaction Characteristics1

  • Simple reaction conditions
  • Readily and easily available starting materials and reagents
  • Use of no solvent, a benign solvent (such as water), or one that is easily removed
  • Simple product isolation
  • Product should be stable under physiological conditions

Click chemistry involves the use of a modular approach and has important applications in the fields of drug discovery, combinatorial chemistry, target-templated in situ chemistry, and DNA research.1

Continue learning about click chemistry in drug discovery.



Kolb HC, Sharpless K. 2003. The growing impact of click chemistry on drug discovery. Drug Discovery Today. 8(24):1128-1137.
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