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).”

LigandActionBinding AffinityUnitsBiasReferences
[Pyr1]Apelin-13 (E)Full Agonist7.0–8.8pIC50Kawamata et al., 2001
Medhurst et al., 2003
Apelin-13 (E)Full Agonist8.8–9.5pIC50Fan et al., 2003
Hosoya et al., 2000
Medhurst et al., 2003
Apelin-17 (E)Full Agonist7.9–9.0pIC50β-arrestinEl Messari et al., 2004
Medhurst et al., 2003
Apelin-36 (E)Full Agonist8.2–8.6pIC50Fan et al., 2003
Hosoya et al., 2000
Kawamata et al., 2001
Medhurst et al., 2003
Elabela/Toddler-11 (E)Full Agonist7.2pIC50Yang et al., 2016
Elabela/Toddler-21 (E)Full Agonist8.7pIC50β-arrestinYang et al., 2016
Elabela/Toddler-32 (E)Full Agonist8.7pIC50β-arrestinYang et al., 2016
MM07Full Agonist9.5pEC50G proteinBrame et al., 2015
CMF-019Full Agonist8.6pIC50G proteinRead et al., 2016
ML233Full AgonistKhan et al., 2011
E339-3D6Full Agonist6.4pKiIturrioz et al., 2010a