Lipinski's Rule of Five
In 1997 Christopher A. Lipinskipublished a seminal paper identifying a series of features commonly found in orally active drugs. These features are referred to as Lipinski's rule of five and can be used as a rule of thumb to indicate whether a molecule is likely to be orally bioavailable (bioactive)(See also ADME). The "rule of five" is so called because most of the features start with the number five.
In general, an orally active drug has:
- not more than 5 hydrogen bonddonors (OH and NH groups)
- not more than 10 hydrogen bond acceptors (notably Nand O)
- a molecular weightunder 500
- a LogPunder 5
Lipinski's work has since been extended to include properties such as the number of rings and rotatable bonds.
References
- CA Lipinski, Adv. Drug Del. Rev. 1997, 23, 3
External links
- Interactive Rule of Five calculatorca:Regla del Cinc de Lipinski
fr:Lipinski's Rule of 5
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Categories: Medicinal chemistry| Pharmacology| Eponymous rules
This article is licensed under the GNU Free Documentation License. It uses material from the http://en.wikipedia.org/wiki/Lipinski%27s+Rule+of+Five Wikipedia article Lipinski's Rule of Five.
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