TABLE 3.

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