Target family: Melatonin receptors (type: gpcr)
Target: MT<sub>1</sub> receptor

Ligand: 2-iodo-melatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of a retinal melatonin receptor.
Published in: J Pharmacol Exp Ther

Ligand: 2-iodo-melatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 2-methoxy-α,β-didehydro-agomelatine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.5 pKi
Reference (Journal): Synthesis of new N-(arylcyclopropyl)acetamides and N-(arylvinyl)acetamides as conformationally-restricted ligands for melatonin receptors.
Published in: Bioorg Med Chem Lett

Ligand: 2-[125I]melatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 2-[125I]melatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 4P-PDOT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 4P-PDOT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 4P-PDOT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms.
Published in: FASEB J

Ligand: 5-HEAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): A new melatonin receptor ligand with mt1-agonist and MT2-antagonist properties.
Published in: J Pineal Res

Ligand: 6-Cl-MLT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 6-Cl-MLT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 6-Cl-MLT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of a retinal melatonin receptor.
Published in: J Pharmacol Exp Ther

Ligand: 6-Cl-MLT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): GR196429: a nonindolic agonist at high-affinity melatonin receptors.
Published in: J Pharmacol Exp Ther

Ligand: 6-hydroxymelatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): GR196429: a nonindolic agonist at high-affinity melatonin receptors.
Published in: J Pharmacol Exp Ther

Ligand: 6-hydroxymelatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 6-hydroxymelatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors.
Published in: Br J Pharmacol

Ligand: 6-hydroxymelatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of a retinal melatonin receptor.
Published in: J Pharmacol Exp Ther

Ligand: AAE-M-PBP-amine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKi
Reference (Journal): MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides.
Published in: ChemMedChem

Ligand: agomelatine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): GR196429: a nonindolic agonist at high-affinity melatonin receptors.
Published in: J Pharmacol Exp Ther

Ligand: agomelatine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: AZD7325 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pIC50
Reference (Webpage): AZD7325.

Ligand: CBOBNEA (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.
Published in: Bioorg Med Chem

Ligand: difluoroagomelatine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.5 pKi
Reference (Journal): Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).
Published in: Eur J Med Chem

Ligand: EFPPEA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.199999809265137 pKi
Reference (Journal): Synthesis of a novel series of tricyclic dihydrofuran derivatives: discovery of 8,9-dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as melatonin receptor (MT1/MT2) ligands.
Published in: J Med Chem

Ligand: GR 128107 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: GR 128107 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): The putative melatonin receptor antagonist GR128107 is a partial agonist on Xenopus laevis melanophores.
Published in: Br J Pharmacol

Ligand: GR 196429 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): GR196429: a nonindolic agonist at high-affinity melatonin receptors.
Published in: J Pharmacol Exp Ther

Ligand: GR 196429 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors.
Published in: Br J Pharmacol

Ligand: ICOA-13 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 4.96999979019165 pKi
Reference (Journal): Design and validation of the first cell-impermeant melatonin receptor agonist.
Published in: Br J Pharmacol

Ligand: IIK7 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.
Published in: J Med Chem

Ligand: K185 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.
Published in: J Med Chem

Ligand: luzindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: luzindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Luzindole (N-0774): a novel melatonin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: luzindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors.
Published in: Br J Pharmacol

Ligand: luzindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: LY 156735 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.1 pKi
Reference (Journal): A single blind, placebo controlled, across groups dose escalation study of the safety, tolerability, pharmacokinetics and pharmacodynamics of the melatonin analog beta-methyl-6-chloromelatonin.
Published in: Life Sci

Ligand: melatonin (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: melatonin (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: melatonin (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of a retinal melatonin receptor.
Published in: J Pharmacol Exp Ther

Ligand: ramelteon (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2005)
Primary target: yes
Median affinity: 10.899999618530273 pKi
Reference (Journal): Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist.
Published in: Neuropharmacology

Ligand: S20928 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S22153 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S24014 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S24773 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S26131 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S26284 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New selective ligands of human cloned melatonin MT1 and MT2 receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]SD6 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.899999618530273 pKd
Reference (Journal): New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors.
Published in: Int J Mol Sci

Ligand: [125I]SD6 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.960000038146973 pKd
Reference (Journal): New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors.
Published in: Int J Mol Sci

Ligand: [125I]SD6 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.960000038146973 pKd
Reference (Journal): Alternative Radioligands for Investigating the Molecular Pharmacology of Melatonin Receptors.
Published in: J Pharmacol Exp Ther

Ligand: [3H]melatonin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors.
Published in: Br J Pharmacol

Ligand: tasimelteon (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2014), EMA (2015)
Primary target: yes
Median affinity: 9.5 pKi
Reference (Journal): Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials.
Published in: Lancet

Ligand: tasimelteon (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2014), EMA (2015)
Primary target: yes
Median affinity: 9.5 pKi
Reference (Webpage): Tasimelteon Advisory Committee Meeting Briefing Materials.

Ligand: UCM1341 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.109999656677246 pKi
Reference (Journal): Identification of Bivalent Ligands with Melatonin Receptor Agonist and Fatty Acid Amide Hydrolase (FAAH) Inhibitory Activity That Exhibit Ocular Hypotensive Effect in the Rabbit.
Published in: J Med Chem

Ligand: UCM 549 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.
Published in: J Med Chem

Ligand: UCM 549 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists.
Published in: ChemMedChem

Ligand: UCM 724 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pKi
Reference (Journal): Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists.
Published in: ChemMedChem

Ligand: UCM 793 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.
Published in: J Med Chem

Ligand: UCSF3384 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pEC50
Reference (Journal): Virtual discovery of melatonin receptor ligands to modulate circadian rhythms.
Published in: Nature

Ligand: UCSF4226 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.829999923706055 pEC50
Reference (Journal): Virtual discovery of melatonin receptor ligands to modulate circadian rhythms.
Published in: Nature

Ligand: UCSF7447 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pEC50
Reference (Journal): Virtual discovery of melatonin receptor ligands to modulate circadian rhythms.
Published in: Nature