TABLE 1.
Compound name | Reported potency (EC50) | Model system (in vitro, ex vivo) | Comment | References |
---|---|---|---|---|
Orthosteric | ||||
Decanoic acid (C10) |
Human: 0.8–20.0 μM b 4.5–25.1 μM a 48 mM a |
‐Recombinant system ‐RAW264.7 cells ‐Mouse bone marrow‐derived macrophages ‐Mouse primary cultured microglia ‐3T3‐L1 adipocytes |
Wang et al., 2006 Nagasaki et al., 2012 Suzuki et al., 2013 Southern et al., 2013 Nikaido et al., 2015 Pillaiyar et al., 2017 Wei, Tokizane, Konishi, Yu, & Kiyama, 2017 Al Mahmud et al., 2017 Recio et al., 2018 Puengel et al., 2020 Lucy et al., 2019 |
|
Embelin |
Human: 89–200 nM b 0.63 μM a 0.4 μM c Mouse: 220 nM b |
‐Recombinant system ‐Human monocyte‐derived macrophages ‐Mouse peritoneal macrophages ‐Human blood‐derived neutrophils ‐Mouse blood‐derived neutrophils ‐Mouse primary cultured microglia ‐Human monocyte ‐Rat neutrophils |
Hakak, Unett, Gatlin, & Liaw, 2007 Southern et al., 2013 Al Mahmud et al., 2017 Wei et al., 2017 Pillaiyar et al., 2017 Gaidarov et al., 2018 Puengel et al., 2020 |
|
6‐OAU |
Human: 14–438 nM b 1.74–11 μM c 512 nM a |
‐Recombinant system ‐Mouse primary cultured microglia ‐Bone marrow‐derived macrophages ‐Human peripheral polymorphonuclear leukocyte ‐U937 cells differentiated into macrophage‐like cells ‐Human monocytes |
Suzuki et al., 2013 Liu et al., 2016 Zhang, Yang, Li, & Xie, 2016 Wei et al., 2017 Recio et al., 2018 Lucy et al., 2019 |
|
PSB‐1584 |
Human: 5 nM b 3.2 nM c |
‐Recombinant system | Tritium‐labelled form of this compound is available ([3H]PSB‐1584) d |
Pillaiyar et al., 2018 Köse et al., 2020 |
2‐HTP (Compound 1 or ZQ‐16) |
Human: 1–144 nM b 0.79–28.8 nM a 597 nM c Mouse: 30.2 nM a |
‐Recombinant system ‐THP‐1 monocytes ‐RAW264.7 cells ‐Mouse bone marrow‐derived neutrophils ‐Human blood‐derived neutrophils ‐Human monocytes ‐Human monocyte‐derived macrophages ‐Mouse bone marrow‐derived macrophages |
Zhang et al., 2016 Liu et al., 2016 Al Mahmud et al., 2017 Sundqvist et al., 2018 Mancini et al., 2019 Lucy et al., 2019 |
|
DL‐175 |
Human: 33 nM b |
‐Recombinant system ‐Mouse bone marrow‐derived macrophages ‐U937 cells differentiated into macrophage‐like cells ‐Human monocytes |
Displays bias agonism for Gi‐protein signalling pathway over arrestin recruitment compared with 6‐OAU | Lucy et al., 2019 |
Allosteric | ||||
DIM |
Human: 0.25–1.25 μM b 0.5–1 μM a 5.9 mM a Mouse: 4.26 μM a |
‐Recombinant system ‐RAW264.7 cells |
PSB‐15160 and PSB‐16671 are DIM analogues that display bias compared with DIM towards Gi‐mediated adenylyl cyclase inhibition over arrestin recruitment e |
Wang et al., 2006 Nikaido et al., 2015 Zhang et al., 2016 Al Mahmud et al., 2017 Pillaiyar et al., 2017 Mancini et al., 2019 |
Note: Note comments in the text about reported potency values and potential issues of receptor reserve.
Potency values were generated using [35S]GTPγS assay.
Potency values were generated using cAMP assay.
Potency values were generated using β‐arrestin recruitment assay.
Köse et al. (2020).