INDEX pharmacokinetics, poor

An analysis of compounds in the World Drag Index has resulted in the rale-of-five, which states that poor oral absorption is expected for compounds with a molecular weight above 500, a calculated octanol/water partition coefficient >5, the number of hydrogen bond donors >5, and the number of hydrogen bond acceptors >10. Exceptions to this rale may be compounds with an active uptake mechanism. Such simple rales are now widely used in the design of combinatorial libraries. More detailed knowledge on relevant properties can be used to optimize oral absorption and pharmacokinetics, an approach which has been called property-based design. ... 

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