Target family: Ghrelin receptor (type: gpcr)
Target: ghrelin receptor

Ligand: [des-octanoyl]ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland.
Published in: J Endocrinol Invest

Ligand: [125I][Tyr4]ghrelin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland.
Published in: J Endocrinol Invest

Ligand: [125I]Tyr-Ala-hexarelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): Growth hormone secretagogue binding sites in peripheral human tissues.
Published in: J Clin Endocrinol Metab

Ligand: [125I][His9]ghrelin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): [125I-His(9)]-ghrelin, a novel radioligand for localizing GHS orphan receptors in human and rat tissue: up-regulation of receptors with athersclerosis.
Published in: Br J Pharmacol

Ligand: [125I][His9]ghrelin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): [125I-His(9)]-ghrelin, a novel radioligand for localizing GHS orphan receptors in human and rat tissue: up-regulation of receptors with athersclerosis.
Published in: Br J Pharmacol

Ligand: SM-130,686 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.92 pIC50
Reference (Journal): Oxindole derivatives as orally active potent growth hormone secretagogues.
Published in: J Med Chem

Ligand: SM-130,686 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.51 pEC50
Reference (Journal): Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor.
Published in: Mol Pharmacol

Ligand: pralmorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: Japan only
Median affinity: 9.3 pKi
Reference (Journal): Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors.
Published in: Mol Endocrinol

Ligand: [35S]ibutamoren (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors.
Published in: Mol Endocrinol

Ligand: wFw-Isn-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Unique interaction pattern for a functionally biased ghrelin receptor agonist.
Published in: J Biol Chem

Ligand: Abbott 14c (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.15 pIC50
Reference (Journal): Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Published in: J Med Chem

Ligand: BIM 28163 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.09 pKi
Reference (Journal): Novel analogs of ghrelin: physiological and clinical implications.
Published in: Eur J Endocrinol

Ligand: [D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.35 pKd
Reference (Journal): High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.
Published in: Mol Endocrinol

Ligand: [des-octanoyl]ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Expression of ghrelin and biological activity of specific receptors for ghrelin and des-acyl ghrelin in human prostate neoplasms and related cell lines.
Published in: Eur J Endocrinol

Ligand: examorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.89 pKd
Reference (Journal): Growth hormone secretagogue binding sites in peripheral human tissues.
Published in: J Clin Endocrinol Metab

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.47 pEC50
Reference (Journal): Unique interaction pattern for a functionally biased ghrelin receptor agonist.
Published in: J Biol Chem

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland.
Published in: J Endocrinol Invest

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.
Published in: Mol Endocrinol

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.47 pEC50
Reference (Journal): High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.
Published in: Mol Endocrinol

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pEC50
Reference (Journal): LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor.
Published in: Cell Metab

Ligand: ghrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Ligand activation domain of human orphan growth hormone (GH) secretagogue receptor (GHS-R) conserved from Pufferfish to humans.
Published in: Mol Endocrinol

Ligand: GHRP-6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.34 pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: GHRP-6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.08 pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: GHRP-6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: GHRP-6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors.
Published in: Mol Endocrinol

Ligand: GHRP-6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors.
Published in: Mol Endocrinol

Ligand: GSK1614343 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Discovery process and characterization of novel carbohydrazide derivatives as potent and selective GHSR1a antagonists.
Published in: ChemMedChem

Ligand: GSK1614343 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKB
Reference (Journal): Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors.
Published in: Eur J Pharmacol

Ligand: HM01 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pKi
Reference (Journal): New ghrelin agonist, HM01 alleviates constipation and L-dopa-delayed gastric emptying in 6-hydroxydopamine rat model of Parkinson's disease.
Published in: Neurogastroenterol Motil

Ligand: ibutamoren (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterisation of a new oral GH secretagogue, NN703.
Published in: Eur J Endocrinol

Ligand: ibutamoren (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.34 pKi
Reference (Journal): Pharmacological characterisation of a new oral GH secretagogue, NN703.
Published in: Eur J Endocrinol

Ligand: ibutamoren (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: JMV3008 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.25 pIC50
Reference (Journal): Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.
Published in: J Med Chem

Ligand: L-692,429 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7 pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: L-692,429 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Published in: Mol Endocrinol

Ligand: L-692,429 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.22 pEC50
Reference (Journal): A nonpeptidyl growth hormone secretagogue.
Published in: Science

Ligand: liver enriched antimicrobial peptide 2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor.
Published in: Cell Metab

Ligand: YIL781 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.77 pKi
Reference (Journal): Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
Published in: Endocrinology

Ligand: macimorelin (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017), EMA (2019)
Primary target: yes
Median affinity: 7.809999942779541 pIC50
Reference (Journal): EP1572: a novel peptido-mimetic GH secretagogue with potent and selective GH-releasing activity in man.
Published in: J Endocrinol Invest

Ligand: PF-05190457 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.850000381469727 pKi
Reference (Journal): Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.
Published in: Br J Pharmacol

Ligand: PF-05190457 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pKi
Reference (Journal): Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.
Published in: Br J Pharmacol

Ligand: PF-05190457 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.109999656677246 pKi
Reference (Journal): Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.
Published in: Br J Pharmacol

Ligand: PF-6870961 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pKi
Reference (Journal): Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor.
Published in: J Pharmacol Exp Ther

Ligand: PF-6870961 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pKi
Reference (Journal): Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor.
Published in: J Pharmacol Exp Ther