Target family: Trace amine receptor (type: gpcr)
Target: TA<sub>1</sub> receptor

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.5 pEC50
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: RO5256390 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): TAAR1 agonists attenuate extended-access cocaine self-administration and yohimbine-induced reinstatement of cocaine-seeking.
Published in: Br J Pharmacol

Ligand: [3H]tyramine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKd
Reference (Journal): Trace amines: identification of a family of mammalian G protein-coupled receptors.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists.
Published in: PLoS ONE

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amines: identification of a family of mammalian G protein-coupled receptors.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.
Published in: Mol Pharmacol

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia.
Published in: Genes Brain Behav

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1.
Published in: J Pharmacol Exp Ther

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.
Published in: Mol Pharmacol

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.
Published in: Mol Pharmacol

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pIC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 5.4 pIC50
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Published in: Proc Natl Acad Sci USA

Ligand: EPPTB (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).
Published in: Bioorg Med Chem Lett

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.
Published in: Mol Pharmacol

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia.
Published in: Genes Brain Behav

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.
Published in: Bioorg Med Chem

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.
Published in: Mol Pharmacol

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amines: identification of a family of mammalian G protein-coupled receptors.
Published in: Proc Natl Acad Sci USA

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists.
Published in: PLoS ONE

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.
Published in: Mol Pharmacol

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia.
Published in: Genes Brain Behav

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1.
Published in: J Pharmacol Exp Ther

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.
Published in: Mol Pharmacol

Ligand: β-phenylethylamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.
Published in: Bioorg Med Chem

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor agonists: synthesis and evaluation of thyronamines and related analogues.
Published in: J Med Chem

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor agonists: synthesis and evaluation of thyronamines and related analogues.
Published in: J Med Chem

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1.
Published in: J Med Chem

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone.
Published in: Nat Med

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1.
Published in: J Med Chem

Ligand: 3-iodothyronamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone.
Published in: Nat Med

Ligand: 2-phenyl-propylamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1.
Published in: J Pharmacol Exp Ther

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amines: identification of a family of mammalian G protein-coupled receptors.
Published in: Proc Natl Acad Sci USA

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists.
Published in: PLoS ONE

Ligand: ractopamine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pEC50
Reference (Journal): Ractopamine, a livestock feed additive, is a full agonist at trace amine-associated receptor 1.
Published in: J Pharmacol Exp Ther

Ligand: ralmitaront (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.230000019073486 pEC50
Reference (Patent): 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pEC50
Reference (Journal): Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.
Published in: Bioorg Med Chem

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.
Published in: Mol Pharmacol

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia.
Published in: Genes Brain Behav

Ligand: R(-)amphetamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pEC50
Reference (Journal): Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.
Published in: Mol Pharmacol

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: RO5166017 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pEC50
Reference (Journal): TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Published in: Proc Natl Acad Sci USA

Ligand: ulotaront (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.849999904632568 pIC50
Reference (Journal): SEP-363856, a Novel Psychotropic Agent with a Unique, Non-D<sub>2</sub> Receptor Mechanism of Action.
Published in: J Pharmacol Exp Ther

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.
Published in: J Pharmacol Exp Ther

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1.
Published in: J Pharmacol Exp Ther

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pEC50
Reference (Journal): Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.
Published in: Mol Pharmacol

Ligand: tyramine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.
Published in: Biochem J

Ligand: octopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia.
Published in: Genes Brain Behav