Table 2. Properties of 216 Oral Drugs Published since 1990.

^aFrom ref (5), updated with drugs launched up to 2014. Antivirals and anticancer kinase inhibitors contribute to increased cLogP and molecular weight versus earlier drugs (see Figure 1).

^bcLogP is the calculated 1-octanol−water partition coefficient from Biobyte (http://www.biobyte.com/bb/prod/clogp40.html).

^cCalculated property forecast index (from ref (6)) = Chrom LogD_pH7.4 + #Ar rings.

^dFraction of carbon sp3 atoms/total C atoms.

^eRule-of-5 failures (from ref (12)) in drugs published pre-1950, 1950−69 and 1970−89 (Figure 1) are 5.2%, 6.0% and 8.1%, respectively.