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Lipinski's Rule of Five
- Created 2012-03-13
Lipinski's rule of five
also known as the
Pfizer's rule of five
or simply the
Rule of five
(RO5) is a
rule of thumb
or determine if a
with a certain
has properties that would make it a likely orally active drug in humans. The rule was formulated by Christopher A. Lipinski in 1997, based on the observation that most medication drugs are relatively small and
The rule describes
important for a drug's
in the human body, including their
"). However, the rule does not predict if a compound is pharmacologically active.
The rule is important to keep in mind during
when a pharmacologically active
is optimized step-wise to increase the activity and selectivity of the compound as well as to insure drug-like physicochemical properties are maintained as described by Lipinski's rule. Candidate drugs that conform to the RO5 tend to have lower attrition rates during
s and hence have an increased chance of reaching the market.
from Wikipedia (last updated: 21 May), licensed under
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