Target family: Melanocortin receptors (type: gpcr)
Target: MC<sub>1</sub> receptor

Ligand: [125I]NDP-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 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: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 pKd
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: ASIP [90-132 (L89Y)] (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Functional properties of an agouti signaling protein variant and characteristics of its cognate radioligand.
Published in: Am J Physiol Regul Integr Comp Physiol

Ligand: bremelanotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 8.1899995803833 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: HS014 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7 pKd
Reference (Journal): Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
Published in: Neuropeptides

Ligand: HS024 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 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: MS05 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): New highly specific agonistic peptides for human melanocortin MC(1) receptor.
Published in: Peptides

Ligand: MT-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
Published in: Eur J Pharmacol

Ligand: MT-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Design of potent linear &alpha;-melanotropin 4-10 analogues modified in positions 5 and 10.
Published in: J Med Chem

Ligand: setmelanotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 8.40999984741211 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: SHU9119 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
Published in: Neuropeptides

Ligand: ACTH (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Characterisation of melanocortin receptor subtypes by radioligand binding analysis.
Published in: Eur J Pharmacol

Ligand: afamelanotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2014), FDA (2019)
Median affinity: 10 pIC50
Reference (Journal): The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
Published in: Eur J Pharmacol

Ligand: afamelanotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2014), FDA (2019)
Median affinity: 10 pIC50
Reference (Journal): Proopiomelanocortin processing in the pituitary, central nervous system, and peripheral tissues.
Published in: Endocr Rev

Ligand: agouti (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor.
Published in: Nature

Ligand: agouti (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): Melanocortin receptor binding determinants in the agouti protein.
Published in: Biochemistry

Ligand: α-MSH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
Published in: Eur J Pharmacol

Ligand: ASIP [90-132 (L89Y)] (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Effects of recombinant agouti-signaling protein on melanocortin action.
Published in: Mol Endocrinol