Identification and validation of bioactive small molecule target through phenotypic screening

Yoon Sun Cho, Ho Jeong Kwon

Research output: Contribution to journalArticlepeer-review

28 Citations (Scopus)


For effective bioactive small molecule discovery and development into new therapeutic drug, a systematic screening and target protein identification is required. Different from the conventional screening system, herein phenotypic screening in combination with multi-omics-based target identification and validation (MOTIV) is introduced. First, phenotypic screening provides visual effect of bioactive small molecules in the cell or organism level. It is important to know the effect on the cell or organism level since small molecules affect not only a single target but the entire cellular mechanism within a cell or organism. Secondly, MOTIV provides systemic approach to discover the target protein of bioactive small molecule. With the chemical genomics and proteomics approach of target identification methods, various target protein candidates are identified. Then network analysis and validations of these candidates result in identifying the biologically relevant target protein and cellular mechanism. Overall, the combination of phenotypic screening and MOTIV will provide an effective approach to discover new bioactive small molecules and their target protein and mechanism identification.

Original languageEnglish
Pages (from-to)1922-1928
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number6
Publication statusPublished - 2012 Mar 15

Bibliographical note

Funding Information:
The authors express their gratitude to Drs. Peter Karuso and James Chen for critical comments and members of chemical genomics NRL at Yonsei University. This study was partly supported by grants from the National Research Foundation (NRF) of Korea , the Korean Government (MEST; 2009-0092964, 2010-0017984, F01-2009-000-10183-0), the Translational Research Center for Protein Function Control and the National Junior Research Fellowship , NRF (2009-0083522, 2011-006165), the Center for Food and Drug Materials of Agriculture Science & Technology Development (2011-8-1178), the Rural Development Administration , and the Brain Korea 21 Project.

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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