<i>In vitro</i> Inhibition of Plasma LysoPLD Activity.

LysoPLD = lysophospholipase D. IC50 values of ONO-8430506 and other inhibitors for recombinant human ATX/ENPP2 when a synthetic fluorescent substrate (FS-3) or a biological substrate (16:0-LPC) was used are shown for (A). IC50 values of ONO-8430506 for recombinant ATX/ENPP2 protein enzyme activity and LysoPLD activity in plasma samples from various species when incubated in the presence of a biological substrate 16:0-LPC are shown for (B). When 16:0-LPC was used as a substrate, the enzyme activity was determined based on the amount of choline generated. The IC50 values means ± S.D. of three independent experiments.