Target family: Apelin receptor (type: gpcr)
Target: apelin receptor

Ligand: ALX40-4C (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Cell-cell fusion and internalization of the CNS-based, HIV-1 co-receptor, APJ.
Published in: Virology

Ligand: compound 14a [PMID: 34795866] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.460000038146973 pEC50
Reference (Journal): Identification of 6-Hydroxypyrimidin-4(1<i>H</i>)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Published in: ACS Med Chem Lett

Ligand: compound 14a [PMID: 34795866] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.569999694824219 pEC50
Reference (Journal): Identification of 6-Hydroxypyrimidin-4(1<i>H</i>)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Published in: ACS Med Chem Lett

Ligand: CMF-019 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pEC50
Reference (Journal): Cardiac action of the first G protein biased small molecule apelin agonist.
Published in: Biochem Pharmacol

Ligand: BMS-986224 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pKd
Reference (Journal): In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.
Published in: Circ Heart Fail

Ligand: azelaprag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.489999771118164 pEC50
Reference (Journal): Cardiovascular response to small-molecule APJ activation.
Published in: JCI Insight

Ligand: azelaprag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.489999771118164 pEC50
Reference (Patent): Triazole agonists of the apj receptor

Ligand: apelin receptor early endogenous ligand (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.289999961853027 pKd
Reference (Journal): Apela Regulates Fluid Homeostasis by Binding to the APJ Receptor to Activate Gi Signaling.
Published in: J Biol Chem

Ligand: apelin-36 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Molecular properties of apelin: tissue distribution and receptor binding.
Published in: Biochim Biophys Acta

Ligand: apelin-36 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.
Published in: Biochemistry

Ligand: apelin-36 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Molecular and functional characteristics of APJ. Tissue distribution of mRNA and interaction with the endogenous ligand apelin.
Published in: J Biol Chem

Ligand: apelin-36 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
Published in: J Neurochem

Ligand: apelin-17 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
Published in: J Neurochem

Ligand: apelin-17 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Functional dissociation of apelin receptor signaling and endocytosis: implications for the effects of apelin on arterial blood pressure.
Published in: J Neurochem

Ligand: apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.
Published in: Biochemistry

Ligand: apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular and functional characteristics of APJ. Tissue distribution of mRNA and interaction with the endogenous ligand apelin.
Published in: J Biol Chem

Ligand: apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
Published in: J Neurochem

Ligand: [3H](Pyr1)[Met(0)11]-apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
Published in: J Neurochem

Ligand: [125I](Pyr1)apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): [(125)I]-(Pyr(1))Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man.
Published in: Br J Pharmacol

Ligand: [125I][Nle75,Tyr77]apelin-36 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 11.2 pKd
Reference (Journal): Molecular properties of apelin: tissue distribution and receptor binding.
Published in: Biochim Biophys Acta

Ligand: [125I][Glp65Nle75,Tyr77]apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.7 pKd
Reference (Journal): Molecular and functional characteristics of APJ. Tissue distribution of mRNA and interaction with the endogenous ligand apelin.
Published in: J Biol Chem

Ligand: [125I]apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.
Published in: Biochemistry

Ligand: [Pyr1]apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular properties of apelin: tissue distribution and receptor binding.
Published in: Biochim Biophys Acta

Ligand: [Pyr1]apelin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
Published in: J Neurochem

Ligand: MM54 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Discovery of a competitive apelin receptor (APJ) antagonist.
Published in: ChemMedChem

Ligand: MM07 (Peptide)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pEC50
Reference (Journal): Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist.
Published in: Hypertension

Ligand: ML233 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.429999828338623 pEC50
Reference (Journal): Functional Agonists of the Apelin (APJ) Receptor.
Published in: Probe Reports from the NIH Molecular Libraries Program

Ligand: ML221 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Published in: Bioorg Med Chem Lett

Ligand: Elabela/Toddler-32 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Webpage): ELABELA/Toddler, a critical regulator of cardiac development, is expressed in the human cardiovascular system and binds the apelin receptor.

Ligand: Elabela/Toddler-21 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Webpage): ELABELA/Toddler, a critical regulator of cardiac development, is expressed in the human cardiovascular system and binds the apelin receptor.

Ligand: Elabela/Toddler-11 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Webpage): ELABELA/Toddler, a critical regulator of cardiac development, is expressed in the human cardiovascular system and binds the apelin receptor.

Ligand: E339-3D6 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist.
Published in: FASEB J

Ligand: cyclourea apelin-12 (1-7) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pEC50
Reference (Journal): Evaluation of novel cyclic analogues of apelin.
Published in: Int J Mol Med

Ligand: cyclo apelin-12 (7-12) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): Evaluation of novel cyclic analogues of apelin.
Published in: Int J Mol Med

Ligand: cyclo apelin-12 (1-12) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Evaluation of novel cyclic analogues of apelin.
Published in: Int J Mol Med

Ligand: compound 40 [PMID: 34982553] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pKi
Reference (Journal): Size-Reduced Macrocyclic Analogues of [Pyr<sup>1</sup>]-apelin-13 Showing Negative Gα<sub>12</sub> Bias Still Produce Prolonged Cardiac Effects.
Published in: J Med Chem

Ligand: compound 39 [PMID: 34982553] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pKi
Reference (Journal): Size-Reduced Macrocyclic Analogues of [Pyr<sup>1</sup>]-apelin-13 Showing Negative Gα<sub>12</sub> Bias Still Produce Prolonged Cardiac Effects.
Published in: J Med Chem

Ligand: compound 21 [PMID: 34855405] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.220000267028809 pEC50
Reference (Journal): Identification of a Hydroxypyrimidinone Compound (<b>21</b>) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure.
Published in: J Med Chem

Ligand: compound 1 [PMID: 25241924] (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Published in: Bioorg Med Chem Lett

Ligand: compound 15a (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.029999732971191 pEC50
Reference (Journal): Biphenyl Acid Derivatives as APJ Receptor Agonists.
Published in: J Med Chem