Table 2. Five Most Potent and Efficacious Compounds Identified, along with In Vitro/Physicochemical ADME Data.

^aIC₅₀: half-maximal inhibitory concentration value obtained from the CPE assay in eight-point dose response, measured in duplicate.

^bEfficacy: maximum inhibitory effect observed in CPE assay.

^cT_1/2: metabolic half-life measured in rat liver microsome fractions reported in minutes, with a minimum detectable half-life of 1 min.⁴⁷

^dParallel artificial membrane permeation assay (PAMPA) is reported as a metric of the passive permeability of the compounds (1 × 10^–6 cm/s).^48,49

^eSolubility—pION μSOL assay for kinetic aqueous solubility determination, pH 7.4.⁵⁰