6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.

GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.

GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM).

DL-175 is a potent and selective biased GPR84 agonist with EC50 of 33 nM.DL-175 exhibits no significant activity in a panel of 168 other GPCRs.DL-175 display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells.DL-175 markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement.

PBI-4547 is an agonist of GPR40/120 and an antagonist of GPR84, also is a partial ligand and activator of PPAR.PBI-4547 dose-dependently inhibits GPR84/Gαi2 activation (reflected by an increase in BRET signal) with IC50 of 17 uM, activates GPR40 (EC50 of 102 µM for Gαq and 16 µM for Gαi2) and dose-dependently promoted β-arrestin-2 recruitment to GPR120 (EC50=148 uM).PBI-4547 prevents progression, improves glucose metabolism in a mouse model of NAFLD, restores hepatic glucose and FA metabolism.

PSB-1584 is a potent, selective agonist of GPR84 with EC50 of 5.0 nM, β-arrestin IC50 of 3.2 nM in human GPR84-expressing cells.

PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM.

PSB-17365 is a potent, selective, Gi-biased agonist of GPR84 with EC50 of 2.5 nM, β-arrestin IC50 of 104 nM in human GPR84-expressing cells.