GLPG-1690 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

HA130 is a selective ATX (autotaxin) inhibitor with IC50 of 28 nM.

Autotaxin-IN-13 ( ATX-i) is a highly potent, selective Autotaxin inhibitor with IC50 of 6 nM.Autotaxin showed sufficient oral bioavailability and low plasma clearance in vivo as well as a suitable half-life to allow for bid or food admix dosing.

PAT-505 (PAT 505, PAT505) is a potent, selective, noncompetitive, and orally active autotaxin inhibitor with IC50 of 2.0 nM against the lysoPLD activity of human ATX.

PAT-048 (PAT048) is a potent, selective, noncompetitive autotaxin inhibitor with IC50 of 1.1 nM against the lysoPLD activity of human ATX.

GWJ-A-23 (GWJ-23, GWJ23) is a potent, selective autotaxin inhibitor with Ki of 18 nM, an analog of the known ATX inhibitor S32826 and has improved aqueous solubility compared with the parent compound.

BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively.