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Drug Discov Today Technol. 2004 Dec;1(4):337-41. doi: 10.1016/j.ddtec.2004.11.007.

Lead- and drug-like compounds: the rule-of-five revolution.

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Pfizer Global R&D, Groton Labs, Eastern Point Road, MS 8200-36, Groton, CT 06340, USA. Electronic


Citations in CAS SciFinder to the rule-of-five (RO5) publication will exceed 1000 by year-end 2004. Trends in the RO5 literature explosion that can be discerned are the further definitions of drug-like. This topic is explored in terms of drug-like physicochemical features, drug-like structural features, a comparison of drug-like and non-drug-like in drug discovery and a discussion of how drug-like features relate to clinical success. Physicochemical features of CNS drugs and features related to CNS blood-brain transporter affinity are briefly reviewed. Recent literature on features of non-oral drugs is reviewed and how features of lead-like compounds differ from those of drug-like compounds is discussed. Most recently, partly driven by NIH roadmap initiatives, considerations have arisen as to what tool-like means in the search for chemical tools to probe biology space. All these topics frame the scope of this short review/perspective.

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