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Related Concept Videos

Midpoint Rule01:20

Midpoint Rule

Approximating areas under curved boundaries is a common problem in applied mathematics, particularly when an exact calculation is difficult or impractical. One effective numerical method for this purpose is the Midpoint Rule, which provides an estimate of the area under a curve by using rectangular approximations over a specified interval.Description of the Midpoint RuleThe Midpoint Rule begins by dividing the given interval into a number of equal subintervals. For each subinterval, the...
Five-Membered Heterocyclic Aromatic Compounds: Overview01:13

Five-Membered Heterocyclic Aromatic Compounds: Overview

Heterocyclic aromatic compounds are cyclic compounds that are aromatic and have one or more heteroatoms—atoms other than carbon, in the ring. Depending upon the number of atoms present in the ring, they can be either five or six-membered. Examples of five-membered heterocyclic aromatic compounds include pyrrole, furan, thiophene, and imidazole. Pyrrole consists of one nitrogen atom having one lone pair of electrons. Furan and thiophene have one oxygen and one sulfur heteroatom, respectively.
5-Number Summary01:04

5-Number Summary

In a dataset, the 5-number summary includes the minimum data value, the data value of the first quartile, the median data value or data value of the second quartile, the data value of the third quartile, and the maximum data value. These 5 data values can be visualized as a box and whisker plot.
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The Quotient Rule01:30

The Quotient Rule

The quotient rule is a fundamental differentiation technique in calculus used to differentiate functions expressed as a ratio of two differentiable functions. Given a function of the form:Where g(x) and h(x) are both differentiable and h(x) ≠ 0, the derivative of f(x) is given by:Example:The quotient rule is beneficial when differentiating rational functions, trigonometric ratios, and exponential functions. For example, given:applying the quotient rule,This rule is essential in solving problems...
Kirchoff's Rules: Application01:22

Kirchoff's Rules: Application

Kirchhoff's rules quantify the current flowing through a circuit and the voltage variations around the loop in a circuit. Applying Kirchhoff's rules generates a set of linear equations that allow us to find the unknown values in circuits. These may be currents, voltages, or resistances.
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Five-Factor Theory of Personality01:29

Five-Factor Theory of Personality

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The 5-Choice Serial Reaction Time Task: A Task of Attention and Impulse Control for Rodents
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The 5-Choice Serial Reaction Time Task: A Task of Attention and Impulse Control for Rodents

Published on: August 10, 2014

Overview on the Rule of Five.

Michael P Pollastri1

  • 1Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts, USA.

Current Protocols in Pharmacology
|February 2, 2012
PubMed
Summary
This summary is machine-generated.

Lipinski's Rule of Five provides medicinal chemists a quick way to assess drug candidates. This rule helps predict if molecules will have good solubility and permeability for oral bioavailability.

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Pharmacokinetics

Background:

  • The drug discovery paradigm shifted in the 1990s towards combinatorial chemistry and high-throughput screening.
  • This shift resulted in drug molecules with increased molecular weight and lipophilicity.
  • Physicochemical properties became critical for successful drug development.

Purpose of the Study:

  • To outline the basis of Lipinski's Rule of Five.
  • To explain how the Rule of Five has been applied in drug discovery.
  • To assess the impact of the Rule of Five on drug development.

Main Methods:

  • Analysis of compounds that successfully passed Phase I and entered Phase II clinical studies.
  • Correlation of computed physicochemical properties with aqueous solubility, permeability, and oral bioavailability.
  • Development of the
  • Rule of Five
  • as a predictive tool.

Main Results:

  • Lipinski's Rule of Five was established based on physicochemical properties of successful drug candidates.
  • The rule serves as a mnemonic for medicinal chemists to evaluate drug-likeness.
  • It aids in predicting the likelihood of good solubility and permeability profiles.

Conclusions:

  • The Rule of Five significantly impacts the drug discovery and optimization process.
  • It provides a rapid assessment of compound properties relevant to oral bioavailability.
  • This rule has become an essential tool in medicinal chemistry for guiding lead optimization.