Table 3. Notably Active Chemotype A Which Shows No Notable Cytotoxicity (IC50 ≤ 30 μM).
a
IC50: half-maximal inhibitory concentration values obtained from the CPE assay in eight-point dose response, measured in duplicate.
b
Values represent data obtained from five-point dose response, measured in duplicate.
c
Efficacy: maximum inhibitory effect observed in CPE assay.
d
T1/2: metabolic half-life measured in rat liver microsome fractions reported in minutes, the minimum detectable half-life of 1 min.47
e
Parallel artificial membrane permeation assay (PAMPA) is reported as a metric of the passive permeability of the compounds.48,49
f
Solubility—pION μSOL assay for kinetic aqueous solubility determination, pH 7.4.50