Ask the experts: Past, present and future of the rule of five

Jonathan Bayldon Baell, Miles Congreve, Paul Leeson, Celerino Abad-Zapatero

Research output: Contribution to journalLetterOther

Abstract

Coined in 1997, by Christopher Lipinki et al., the rule of five (Ro5) comprises a set of parameters that determine drug-likeness for oral delivery. The parameters are as follows: no more than five hydrogen bond donors (nitrogen or oxygen atoms with one or more hydrogen atoms); no more than ten hydrogen bond acceptors (nitrogen or oxygen atoms); a molecular mass less than 500 Da; and an octanol water partition coefficient log P no greater than 5. Future Medicinal Chemistry invited a selection of leading researchers to express their views on Lipinski s Ro5, which has influenced drug design for over a decade. Their enlightening responses provide an insight into the current and future role of Ro5, and other rules of thumb, in the evolving world of medicinal chemistry.
Original languageEnglish
Pages (from-to)745 - 752
Number of pages8
JournalFuture Medicinal Chemistry
Volume5
Issue number7
DOIs
Publication statusPublished - 2013

Cite this

Baell, Jonathan Bayldon ; Congreve, Miles ; Leeson, Paul ; Abad-Zapatero, Celerino. / Ask the experts: Past, present and future of the rule of five. In: Future Medicinal Chemistry. 2013 ; Vol. 5, No. 7. pp. 745 - 752.
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Ask the experts: Past, present and future of the rule of five. / Baell, Jonathan Bayldon; Congreve, Miles; Leeson, Paul; Abad-Zapatero, Celerino.

In: Future Medicinal Chemistry, Vol. 5, No. 7, 2013, p. 745 - 752.

Research output: Contribution to journalLetterOther

TY - JOUR

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AU - Baell, Jonathan Bayldon

AU - Congreve, Miles

AU - Leeson, Paul

AU - Abad-Zapatero, Celerino

PY - 2013

Y1 - 2013

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AB - Coined in 1997, by Christopher Lipinki et al., the rule of five (Ro5) comprises a set of parameters that determine drug-likeness for oral delivery. The parameters are as follows: no more than five hydrogen bond donors (nitrogen or oxygen atoms with one or more hydrogen atoms); no more than ten hydrogen bond acceptors (nitrogen or oxygen atoms); a molecular mass less than 500 Da; and an octanol water partition coefficient log P no greater than 5. Future Medicinal Chemistry invited a selection of leading researchers to express their views on Lipinski s Ro5, which has influenced drug design for over a decade. Their enlightening responses provide an insight into the current and future role of Ro5, and other rules of thumb, in the evolving world of medicinal chemistry.

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DO - 10.4155/FMC.13.61

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