Table 2. SAR of Weakly Basic Amines.

^aIC₅₀ values are reported as the geometric mean of n ≥ 3 with the 95% CI in parentheses, except where otherwise noted.

^bExperimental pK_a.

^cExperimental logD using the shake-flask method at pH 7.4.³⁴

^dApparent intrinsic clearance (CL_int,app) obtained from human hepatocyte cells.³⁵

^ePermeability determined from an assay using low-efflux MDCKII cells.³⁶

^f6 is the more potent cis enantiomer; stereochemistry arbitrarily assigned.

^g7 is the more potent enantiomer; stereochemistry arbitrarily assigned.

^h8 is the more potent enantiomer; stereochemistry arbitrarily assigned.

ⁱCL_int,app obtained from human hepatocyte cells using the relay method for low-clearance compounds³⁷