Table 4. SAR of Truncated, Reversed Amides.


Biochemical inhibition of PLD1/2 was determined by immunoprecipitation on a plate (IPoP) of PLD1/2 from HEK cells.
Cellular assay performed with Calu-1 cell line.
Rat or human liver microsomes.
Efflux ratio determined by measuring Papp(B-A)/Papp(A-B).
cassette dosing used; [Clu] = Unbound clearance (Cl/fu).