Figure 2.

Impact of hydrophobicity on developability assays and the profile of marketed oral drugs. (a) Percentages of GlaxoSmithKline compounds meeting developability criteria according to their property forecast indices (PFI and iPFI (intrinsic PFI based on LogP)), composite measures of hydrophobicity using the combination of chromatographically determined lipophilicities, and aromatic ring count. Some data, e.g., Cyp inhibition and passive permeability (P_app), display nonlinear behavior. Green, ≥67%; Yellow, 34–66%; Red, <33%. All data from Young et al,¹⁰¹ reproduced with permission. (b). Calculated PFI (from ref (101)) distribution of marketed oral drugs (from ref (100), updated with drugs launched up to 2014) shows 70% are in the lower risk zone (PFI < 7).