Combinatorial chemistry in drug discovery

Ruiwu Liu, Xiaocen Li, Kit Lam

Research output: Contribution to journalReview articlepeer-review

116 Scopus citations


Several combinatorial methods have been developed to create focused or diverse chemical libraries with a wide range of linear or macrocyclic chemical molecules: peptides, non-peptide oligomers, peptidomimetics, small-molecules, and natural product-like organic molecules. Each combinatorial approach has its own unique high-throughput screening and encoding strategy. In this article, we provide a brief overview of combinatorial chemistry in drug discovery with emphasis on recently developed new technologies for design, synthesis, screening and decoding of combinatorial library. Examples of successful application of combinatorial chemistry in hit discovery and lead optimization are given. The limitations and strengths of combinatorial chemistry are also briefly discussed. We are now in a better position to truly leverage the power of combinatorial technologies for the discovery and development of next-generation drugs.

Original languageEnglish (US)
Pages (from-to)117-126
Number of pages10
JournalCurrent Opinion in Chemical Biology
StatePublished - Jun 1 2017

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry


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