title: A practical view of 'druggability'.
abstract: The introduction of Lipinski's 'Rule of Five' has initiated a profound shift in the thinking paradigm of medicinal chemists. Understanding the difference between biologically active small molecules and drugs became a priority in the drug discovery process, and the importance of addressing pharmacokinetic properties early during lead optimization is a clear result. These concepts of 'drug-likeness' and 'druggability' have been extended to proteins and genes for target identification and selection. How should these concepts be integrated practically into the drug discovery process? This review summarizes the recent advances in the field and examines the usefulness of 'the rules of the game' in practice from a medicinal chemist's standpoint.
authors.affiliation: Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, 138670 Singapore. thomas.keller@novartis.com
authors.forename: Thomas H
authors.initials: TH
authors.lastname: Keller
authors.forename: Arkadius
authors.initials: A
authors.lastname: Pichota
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yin
mesh_terms: D015195:Drug Design; D004345:Drug Industry / Q000592:standards*; D017408:Guidelines as Topic; D006801:Humans; D004364:Pharmaceutical Preparations / Q000592:standards*; D011506:Proteins / Q000187:drug effects
chemical_list: D004364:Pharmaceutical Preparations; D011506:Proteins