| DC7925 |
GTPL-5846 (6-OAU)
Featured
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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. |
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| DC28800 |
GLPG1205 |
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. |
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| DC47628 |
GPR84 antagonist 1 |
GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84. |
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| DC49050 |
GPR84 antagonist 2
Featured
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GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). |
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| DC70360 |
DL-175 |
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. |
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| DC70679 |
PBI-4547 |
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. |
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| DC70713 |
PSB-1584 |
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. |
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| DC70714 |
PSB-16671
Featured
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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. |
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| DC70715 |
PSB-17365 |
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. |
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| DC73447 |
OX04528 |
OX04528 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 5.98 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells. |
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| DC73448 |
OX04529 |
OX04529 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 18.5 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells. |
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