Target family: Melanocortin receptors (type: gpcr)
Target: MC<sub>3</sub> receptor

Ligand: [125I]SHU9119 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Molecular determinants of melanocortin 4 receptor ligand binding and MC4/MC3 receptor selectivity.
Published in: J Pharmacol Exp Ther

Ligand: [125I]NDP-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Co-operative regulation of ligand binding to melanocortin receptor subtypes: evidence for interacting binding sites.
Published in: Eur J Pharmacol

Ligand: SHU9119 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
Published in: Eur J Pharmacol

Ligand: SHU9119 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
Published in: J Med Chem

Ligand: SHU9119 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
Published in: Eur J Pharmacol

Ligand: SHU9119 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
Published in: Neuropeptides

Ligand: setmelanotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
Published in: Peptides

Ligand: PG-901 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.
Published in: J Med Chem

Ligand: PG-106 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5.
Published in: Peptides

Ligand: MT-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
Published in: Eur J Pharmacol

Ligand: HS024 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKd
Reference (Journal): Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo.
Published in: Endocrinology

Ligand: HS014 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKd
Reference (Journal): Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
Published in: Neuropeptides

Ligand: γ-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKd
Reference (Journal): Conformation of the core sequence in melanocortin peptides directs selectivity for the melanocortin MC3 and MC4 receptors.
Published in: J Biol Chem

Ligand: [D-Trp8]γ-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
Published in: J Med Chem

Ligand: bremelanotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.28000020980835 pKi
Reference (Journal): Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
Published in: J Med Chem

Ligand: AP1189 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pKd
Reference (Patent): Phenyl pyrrole aminoguanidine derivatives

Ligand: α-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Conformation of the core sequence in melanocortin peptides directs selectivity for the melanocortin MC3 and MC4 receptors.
Published in: J Biol Chem