Target family: Melanin-concentrating hormone receptors (type: gpcr)
Target: MCH<sub>1</sub> receptor

Ligand: S36539 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: 4-arylphthalazin-1(2H)-3,4-Di-F (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): 4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1).
Published in: Bioorg Med Chem Lett

Ligand: 7-fluorochromone-2-carboxamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Published in: J Med Chem

Ligand: Ac-hMCH-(6-16)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.
Published in: Biochemistry

Ligand: ATC0065 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists.
Published in: J Pharmacol Exp Ther

Ligand: ATC0175 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists.
Published in: J Pharmacol Exp Ther

Ligand: [Ava9,10,Ava14,15]-Ac-hMCH6-16-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.
Published in: Biochemistry

Ligand: AZ13483342 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: AZ13483342 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Webpage): AZ13483342.

Ligand: C3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: compound 17 [PMID: 17125263] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): 6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.
Published in: J Med Chem

Ligand: compound 2 [PMID: 11375253] (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: compound 4b [PMID: 19683441] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.319999694824219 pIC50
Reference (Journal): Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound (R)-10h [PMID: 22490048] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities.
Published in: J Med Chem

Ligand: GW803430 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: MCH (salmon) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: MCH (salmon) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: MCH (salmon) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1.
Published in: Nature

Ligand: MCH6-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: MCH6-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: melanin-concentrating hormone (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1.
Published in: Nature

Ligand: melanin-concentrating hormone (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: melanin-concentrating hormone (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: MQ1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): The MCH(1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times.
Published in: Br J Pharmacol

Ligand: MQ1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities.
Published in: J Med Chem

Ligand: p-guanidinobenzoyl-MCH-(7-17) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): S38151 [p-guanidinobenzoyl-[Des-Gly(10)]-MCH(7-17)] is a potent and selective antagonist at the MCH(1) receptor and has anti-feeding properties in vivo.
Published in: Peptides

Ligand: [Phe13,Tyr19]MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Melanin-concentrating hormone receptor is a target of leptin action in the mouse brain.
Published in: Endocrinology

Ligand: [Phe13,Tyr19]MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1.
Published in: Nature

Ligand: [Phe13,Tyr19]MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: [Phe13,Tyr19]MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.
Published in: Proc Natl Acad Sci USA

Ligand: pyrrolidine MCHR1 antagonist 1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition.
Published in: Bioorg Med Chem Lett

Ligand: S36057 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: S36057 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: S36077 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: S36077 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study.
Published in: J Pharmacol Exp Ther

Ligand: S36540 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: S36541 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: S38151 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): S38151 [p-guanidinobenzoyl-[Des-Gly(10)]-MCH(7-17)] is a potent and selective antagonist at the MCH(1) receptor and has anti-feeding properties in vivo.
Published in: Peptides

Ligand: SB-568849 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
Published in: Bioorg Med Chem Lett

Ligand: SNAP-7941 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist.
Published in: Nat Med

Ligand: SNAP-7941 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pA2
Reference (Journal): Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist.
Published in: Nat Med

Ligand: [125I](3-iodo-Tyr13)-MCH (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: [125I]MCH (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1.
Published in: Nature

Ligand: [125I][Phe13,Tyr19]MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Melanin-concentrating hormone binding sites in human SVK14 keratinocytes.
Published in: Biochem Biophys Res Commun

Ligand: [125I]S36057 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor.
Published in: Br J Pharmacol

Ligand: [3H]MCH (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Melanin-concentrating hormone binding sites in human SVK14 keratinocytes.
Published in: Biochem Biophys Res Commun

Ligand: [3H]SNAP-7941 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist.
Published in: Nat Med

Ligand: T-226296 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.
Published in: Eur J Pharmacol

Ligand: tetralin_urea analogue (7o) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: TPI 1361-17 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): The pharmacological properties of a novel MCH1 receptor antagonist isolated from combinatorial libraries.
Published in: Eur J Pharmacol

Ligand: variant MCH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1.
Published in: Nature