Target family: Dopamine receptors (type: gpcr)
Target: D<sub>1</sub> receptor

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: A68930 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.82 pEC50
Reference (Journal): Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors.
Published in: Pharmacol Biochem Behav

Ligand: A77636 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.739999771118164 pKi
Reference (Journal): Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors.
Published in: Neuropharmacology

Ligand: (+)-ADTN (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: (+)-ADTN (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 6.2 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 6.2 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: cabergoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996)
Median affinity: 6.7 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.1 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 6.9 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: dihydrexidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Dihydrexidine, a novel selective high potency full dopamine D-1 receptor agonist.
Published in: Eur J Pharmacol

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: ecopipam (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes.
Published in: Pharmacol Biochem Behav

Ligand: fenoldopam (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: flupentixol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: flupentixol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: fluphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 7.7 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: no
Median affinity:  pKi
Reference (Journal): Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
Published in: J Psychopharmacol (Oxford)

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6.7 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity: 7.2 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: LY3154885 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.929999828338623 pEC50
Reference (Journal): Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Published in: J Med Chem

Ligand: mesoridazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1970)
Primary target: no
Median affinity: 6.989999771118164 pKi
Reference (Journal): Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
Published in: Bioorg Med Chem Lett

Ligand: mevidalen (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.210000038146973 pEC50
Reference (Journal): Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Published in: J Med Chem

Ligand: mevidalen (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 8.640000343322754 pEC50
Reference (Journal): Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Published in: J Med Chem

Ligand: noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.3 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: N-propylnorapomorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity:  pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: periciazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2009)
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Affinity of neuroleptics for D1 receptor of human brain striatum.
Published in: J Psychiatry Neurosci

Ligand: prochlorperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: no
Median affinity: 7.110000133514404 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: rotigotine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2006), FDA (2007)
Median affinity: 5.6 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SCH-23390 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SCH-23390 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: SKF-38393 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.
Published in: J Biol Chem

Ligand: SKF-38393 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SKF-75670 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Dopamine receptor agonists: selectivity and dopamine D1 receptor efficacy.
Published in: Eur J Pharmacol

Ligand: SKF-76783 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SKF-81297 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Dopamine receptor agonists: selectivity and dopamine D1 receptor efficacy.
Published in: Eur J Pharmacol

Ligand: (+)-SKF-82526 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: (-)-SKF-82526 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SKF-82958 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The full D1 dopamine receptor agonist SKF-82958 induces neuropeptide mRNA in the normosensitive striatum of rats: regulation of D1/D2 interactions by muscarinic receptors.
Published in: J Pharmacol Exp Ther

Ligand: SKF-83566 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: SKF-83959 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pEC50
Reference (Journal): Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor.
Published in: ACS Chem Neurosci

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: [125I]SCH23982 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pKd
Reference (Journal): Molecular cloning and expression of the gene for a human D1 dopamine receptor.
Published in: Nature

Ligand: [3H]SCH-23390 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pKd
Reference (Journal): Cloning and expression of human and rat D1 dopamine receptors.
Published in: Nature

Ligand: tavapadon (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pKi
Reference (Journal): Novel Strategies To Activate the Dopamine D<sub>1</sub> Receptor: Recent Advances in Orthosteric Agonism and Positive Allosteric Modulation.
Published in: J Med Chem

Ligand: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 7 pKi
Reference (Journal): Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
Published in: Nature

Ligand: UCM-1306 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pEC50
Reference (Journal): 2-(Fluoromethoxy)-4'-(<i>S</i>-methanesulfonimidoyl)-1,1'-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D<sub>1</sub> Receptor for Parkinson's Disease.
Published in: J Med Chem