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Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans.
Lipinski rule of 5 helps in distinguishing between drug like and non drug like molecules. It predicts high probability of success or failure due to drug likeness for molecules complying with 2 or more of the following rules; Molecular mass less than 500 Dalton; High lipophilicity (expressed as LogP less than 5) Less than 5 hydrogen bond donors
Lipinski's rule of five is a concept frequently used in drug discovery. This rule helps to predict if a biologically active molecule is likely to have the chemical and physical properties to be orally bioavailable.
To predict the properties of molecular drugs, Lipinski's “Rule of Five” rule is widely used. In 1997, Lipinski, a senior pharmaceutical chemist at Pfizer, determined the chemical properties of oral pharmaceutical small-molecule compounds by comparing candidate medicine molecules with ordinary organic compounds and summarized them as the ...
A general “rule of thumb” for valuation of drug-like properties, known as Lipinski's rule of 5 (Ro5), has been introduced for almost 2 decades, 2 which is a generally accepted method to predict drugs’ ADME (“absorption, distribution, metabolism, and excretion”) performance mainly for oral drugs.
In 1997 Christopher Lipinski and colleagues looked at the physicochemical characteristics of approved drugs and clinical candidates at that time, and proposed that the ' rule of 5 ' could...
Twenty five years ago, Christopher Lipinski and colleagues published arguably the most influential sentence in small-molecule drug discovery. Their cleverly crafted ‘rule of 5’ (Ro5)...