Recent advances in chemical genomics

György Dormán, Péter Krajcsi, László G. Puskás, Zoltán Kovári, Zsolt Lorincz, László Ürge, Ferenc Darvas

Research output: Contribution to journalReview article

1 Citation (Scopus)


Chemical genomics, which utilizes specially designed small chemical compounds early in the discovery phase of new drugs to explore the life science at various levels, can address biological questions that are not amenable to genetic manipulation or functional genomics/proteomics approaches. Following the development of HT phenotypic assays and DNA expression analysis, the integration of cell-based assays with activity/ affinity-based approaches allows us to interrogate the cells by analyzing phenotypic alterations, changes of transcript signature or detecting the differences in protein expression levels. Furthermore, activity/affinity-based techniques directly provide a druggable subset of gene products which interact with small molecules, greatly reducing the complexity of analyzing the proteome. In this paper, we give an account of the recent advances (approaches and strategies) in the field of chemical genomics, and discuss how these approaches enable the investigator to obtain a novel therapeutically relevant target as well as drug candidates acting on them in a target-specific manner. This novel post-genomic discovery strategy, where target identification/ validation is carried out by interactions with small molecules, could significantly reduce the time-scale for early drug discovery, and increase the success rate of finding novel, druggable targets, as well as more specific drug candidates. All rights reserved -

Original languageEnglish
Pages (from-to)503-550
Number of pages48
JournalFrontiers in Medicinal Chemistry
Issue number1
Publication statusPublished - Jan 2006



  • Activity based probes
  • Affinity based approaches
  • Chemical genetics
  • Chemical genomics
  • Chemical proteomics
  • Chemogenomics
  • Chemoproteomics
  • High-throughput screening
  • Photochemical proteomics

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Organic Chemistry

Cite this

Dormán, G., Krajcsi, P., Puskás, L. G., Kovári, Z., Lorincz, Z., Ürge, L., & Darvas, F. (2006). Recent advances in chemical genomics. Frontiers in Medicinal Chemistry, 3(1), 503-550.