Some of the key agonists at the apelin receptor, their binding affinities, and whether they demonstrate bias compared with [Pyr1]apelin-13 (the predominant apelin isoform in the cardiovascular system (Maguire el al., 2009; Zhen et al., 2013) Endogenous agonists are denoted by “(E).”
Ligand | Action | Binding Affinity | Units | Bias | References |
---|---|---|---|---|---|
[Pyr1]Apelin-13 (E) | Full Agonist | 7.0–8.8 | pIC50 | — | Kawamata et al., 2001 |
Medhurst et al., 2003 | |||||
Apelin-13 (E) | Full Agonist | 8.8–9.5 | pIC50 | — | Fan et al., 2003 |
Hosoya et al., 2000 | |||||
Medhurst et al., 2003 | |||||
Apelin-17 (E) | Full Agonist | 7.9–9.0 | pIC50 | β-arrestin | El Messari et al., 2004 |
Medhurst et al., 2003 | |||||
Apelin-36 (E) | Full Agonist | 8.2–8.6 | pIC50 | — | Fan et al., 2003 |
Hosoya et al., 2000 | |||||
Kawamata et al., 2001 | |||||
Medhurst et al., 2003 | |||||
Elabela/Toddler-11 (E) | Full Agonist | 7.2 | pIC50 | Yang et al., 2016 | |
Elabela/Toddler-21 (E) | Full Agonist | 8.7 | pIC50 | β-arrestin | Yang et al., 2016 |
Elabela/Toddler-32 (E) | Full Agonist | 8.7 | pIC50 | β-arrestin | Yang et al., 2016 |
MM07 | Full Agonist | 9.5 | pEC50 | G protein | Brame et al., 2015 |
CMF-019 | Full Agonist | 8.6 | pIC50 | G protein | Read et al., 2016 |
ML233 | Full Agonist | — | — | — | Khan et al., 2011 |
E339-3D6 | Full Agonist | 6.4 | pKi | — | Iturrioz et al., 2010a |