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 |