Revisiting the Rule of Five on the Basis of Pharmacokinetic Data from Rat
Lars Ridder, Hongwu Wang, Jacob de Vlieg, Markus Wagener · ChemMedChem · 2011
Physicochemical requirements for oral absorption: The Rule of Five (Ro5) and an alternative set of less stringent rules were evaluated with a large dataset of oral absorption in rat. A combined classification scheme is proposed in which the Ro5 (green area) is used to identify compounds with good oral absorption, whereas less stringent rules (yellow area) are used to differentiate the remaining compounds into medium and low absorption.