. 2020 Sep 17;179(14):3529–3541. doi: 10.1111/bph.15248

TABLE 2.

Antagonist ligands with affinity at GPR84

Compound name	Potency (IC₅₀)	Model system (in vitro, ex vivo)	Comment	References
Orthosteric
PBI‐4050	Human: 0.4 mM (vs. sodium decanoate) ^b 0.21 mM (vs. embelin) ^b	‐Recombinant system ‐Human dermal fibroblasts ‐Human epithelial proximal tubule cells ‐Peritoneal mouse macrophages ‐Human podocytes ‐Human hepatic stellate cells ‐Human lung fibroblasts		Parker et al., 2017 Gagnon et al., 2018 Grouix et al., 2018 Li et al., 2018 Khalil et al., 2019 Nguyen et al., 2020
Allosteric
Compound 107	Human: 7.24–13.8 nM (vs. 2‐HTP) ^a 0.89–4.8 nM (vs. PSB‐16671) ^a Mouse: 125.9–316.2 nM (vs. 2‐HTP) ^a 67.61–144.5 nM (vs. PSB16671) ^a	‐Recombinant system ‐THP‐1 monocytes ‐RAW264.7 cells ‐Mouse bone marrow‐derived neutrophils ‐Human blood‐derived neutrophils	A tritium‐labelled form of an antagonist compound from the same series of 107 is available ([³H]G9543) ^c	Labéguère et al., 2014 Al Mahmud et al., 2017 Mancini et al., 2019 Labéguère et al., 2020
GLPG1205	Human: 54 nM (vs. DIM) ^a	‐Recombinant system ‐Human blood‐derived neutrophils ‐Rat blood‐derived neutrophils ‐Dog blood‐derived neutrophils ‐Human monocyte‐derived macrophages	From the same series as 107: in clinical trials in patients with idiopathic pulmonary fibrosis	Labéguère et al., 2014 Labéguère et al., 2020 Vermeire et al., 2017 Sundqvist et al., 2018

^{^a}

Potency values were generated using [³⁵S]GTPγS assay.

^{^b}

Potency values were generated using BRET activation biosensor assay.

^{^c}

Al Mahmud et al. (2017), Mancini et al. (2019), and Labéguère et al. (2020).