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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; displays good potency in the LPA and rat whole blood assay (IC50=29 nM); shows substantial lowering of LPA in vivo, and excellent PK/Target Engagement relationship.




A potent and selective inhibitor of autotaxin with IC50 of 28 nM; shows no effect on chymotryptic, caspase, and tryptic activities of the proteasome, alkaline phosphatase and a broad-spectrum PEDs (IC50>10 uM); inhibits ATX-driven melanoma cell migration and decreases circulating LPA levels in mice.




GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM; inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma with IC50 of 418 nM, 542 nM, and 242 nM, respectively; shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.

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