GLPG1205 is a potent and selective GPR84 inhibitor (negative allosteric modulator) with IC50 of 54 nM (hGPR84).
GLPG1205 is fully selective over close homologs GPR43 (FFA2R) and GPR41 (FFA3R) and >100-fold selective over 123 other GPCRs on a Millipore GPCR Profiler panel.
GLPG1205 exhibits high potency in human and rat neutrophil assay with IC50 of 11 nM and 111 nM, respectively.
GLPG1205 (once-daily doses of 3 and 10 mg/kg) reduced disease activity index score and neutrophil infiltration in a mouse dextran sodium sulfate-induced chronic inflammatory bowel disease model, with efficacy similar to positive-control compound sulfasalazine.
