Target family: Dopamine receptors (type: gpcr)
Target: D<sub>2</sub> receptor

Ligand: 7-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: 7-trans-OH-PIPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.
Published in: J Med Chem

Ligand: alizapride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  -

Ligand: amisulpride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.
Published in: Mol Pharmacol

Ligand: amisulpride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: amisulpride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 7.800000190734863 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Lack of discrimination by agonists for D2 and D3 dopamine receptors.
Published in: Neuropsychopharmacology

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity: 7.6 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Primary target: yes
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: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Primary target: yes
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

Ligand: aripiprazole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Median affinity: 9.7 pKi
Reference (Journal): Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology.
Published in: Mol Pharmacol

Ligand: aripiprazole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors.
Published in: Eur J Med Chem

Ligand: aripiprazole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: yes
Median affinity: 7.420000076293945 pEC50
Reference (Journal): Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy.
Published in: Proc Natl Acad Sci USA

Ligand: asenapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009), EMA (2010)
Primary target: yes
Median affinity: 8.920000076293945 pKi
Reference (Journal): Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
Published in: J Psychopharmacol (Oxford)

Ligand: benperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2006)
Primary target: no
Median affinity: 10.569999694824219 pKi
Reference (Journal): Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.
Published in: Mol Psychiatry

Ligand: benzquinamide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 5.400000095367432 pKi
Reference (Journal): Identifying mechanism-of-action targets for drugs and probes.
Published in: Proc Natl Acad Sci USA

Ligand: blonanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 9.850000381469727 pKi
Reference (Journal): Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.
Published in: Bioorg Med Chem Lett

Ligand: brexpiprazole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2018)
Primary target: no
Median affinity: 9.520000457763672 pKi
Reference (Journal): Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator.
Published in: J Pharmacol Exp Ther

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
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: 7.3 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
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: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of the human dopamine D3 receptor expressed in transfected cell lines.
Published in: Eur J Pharmacol

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Lack of discrimination by agonists for D2 and D3 dopamine receptors.
Published in: Neuropsychopharmacology

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
Published in: J Pharmacol Exp Ther

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: cabergoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
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: cariprazine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2017)
Primary target: no
Median affinity: 8.239999771118164 pKi
Reference (Journal): Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
Published in: Bioorg Med Chem Lett

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: chlorprothixene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.529999732971191 pKi
Reference (Journal): Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.
Published in: Bioorg Med Chem Lett

Ligand: cinnarizine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1989)
Primary target: no
Median affinity: 7.880000114440918 pKi
Reference (Journal): Possible pharmacokinetic and pharmacodynamic factors affecting parkinsonism inducement by cinnarizine and flunarizine.
Published in: Biochem Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
Published in: J Psychopharmacol (Oxford)

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 6.2 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of the human dopamine D3 receptor expressed in transfected cell lines.
Published in: Eur J Pharmacol

Ligand: compound 3 [PMID: 23134120] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.929999828338623 pKi
Reference (Journal): Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Published in: J Med Chem

Ligand: domperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: domperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.5 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: domperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

Ligand: dopamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity:  pKi
Reference (Journal): Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology.
Published in: Mol 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): Lack of discrimination by agonists for D2 and D3 dopamine receptors.
Published in: Neuropsychopharmacology

Ligand: EGIS-11150 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Egis-11150: a candidate antipsychotic compound with procognitive efficacy in rodents.
Published in: Neuropharmacology

Ligand: eticlopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Characterization of the human dopamine D3 receptor expressed in transfected cell lines.
Published in: Eur J Pharmacol

Ligand: eticlopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
Published in: J Pharmacol Exp Ther

Ligand: flunarizine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Interaction of flunarizine with dopamine D2 and D1 receptors.
Published in: Eur J Pharmacol

Ligand: flunarizine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Possible pharmacokinetic and pharmacodynamic factors affecting parkinsonism inducement by cinnarizine and flunarizine.
Published in: Biochem Pharmacol

Ligand: flupentixol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.819999694824219 pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: fluphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 8.84000015258789 pKi
Reference (Journal): Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.
Published in: Bioorg Med Chem

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of the human dopamine D3 receptor expressed in transfected cell lines.
Published in: Eur J Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes.
Published in: Pharmacol Biochem Behav

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.
Published in: Eur J Pharmacol

Ligand: HS665 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.349999904632568 pKi
Reference (Journal): Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Published in: J Med Chem

Ligand: iloperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Primary target: no
Median affinity: 6.960000038146973 pIC50
Reference (Journal): 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
Published in: J Med Chem

Ligand: trans-flupenthixol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: L-741,626 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
Published in: Bioorg Med Chem Lett

Ligand: L-741,626 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Published in: J Med Chem

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
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: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Primary target: yes
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
Published in: Neuropsychopharmacology

Ligand: LP-12 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.650000095367432 pKi
Reference (Journal): Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Published in: J Med Chem

Ligand: LP-211 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pKi
Reference (Journal): Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
Published in: J Med Chem

Ligand: LP-44 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.140000343322754 pKi
Reference (Journal): Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Published in: J Med Chem

Ligand: lumateperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.489999771118164 pKi
Reference (Journal): Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Published in: J Med Chem

Ligand: lumateperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.489999771118164 pKi
Reference (Journal): Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission.
Published in: Psychopharmacology (Berl.)

Ligand: lurasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2010), EMA (2014)
Primary target: no
Median affinity: 8.770000457763672 pKi
Reference (Journal): Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity.
Published in: J Pharmacol Exp Ther

Ligand: mesoridazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1970)
Primary target: no
Median affinity: 8.65999984741211 pKi
Reference (Journal): Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
Published in: Bioorg Med Chem Lett

Ligand: metoclopramide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 7.539999961853027 pKi
Reference (Journal): Prediction of catalepsies induced by amiodarone, aprindine and procaine: similarity in conformation of diethylaminoethyl side chain.
Published in: J Pharmacol Exp Ther

Ligand: metopimazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  -

Ligand: ML321 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists.
Published in: Probe Reports from the NIH Molecular Libraries Program

Ligand: ML321 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
Published in: J Med Chem

Ligand: MLS1547 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.229999542236328 pKi
Reference (Journal): Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.
Published in: Mol Pharmacol

Ligand: nafadotride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology.
Published in: Mol Pharmacol

Ligand: nafadotride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents.
Published in: J Pharmacol Exp Ther

Ligand: (-)-N-porphynorapomorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

Ligand: (-)-N-porphynorapomorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Primary target: yes
Median affinity: 8.680000305175781 pKi
Reference (Journal): Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
Published in: Neuropsychopharmacology

Ligand: PD 128907 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907.
Published in: J Pharmacol Exp Ther

Ligand: PD 128907 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

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: perospirone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 9.220000267028809 pKi
Reference (Journal): Brain receptors for antipsychotic drugs and dopamine: direct binding assays.
Published in: Proc Natl Acad Sci USA

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: yes
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Antipsychotic drugs, dopamine receptors, and schizophrenia.
Published in: Clinical Neuroscience Research

Ligand: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Median affinity: 7.6 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: pipotiazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1980)
Primary target: yes
Median affinity: 9.699999809265137 pKi
Reference (Journal): Localization and function of the D3 dopamine receptor.
Published in: Arzneimittelforschung

Ligand: piribedil (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: pramipexole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA and EMA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.
Published in: Eur J Pharmacol

Ligand: pramipexole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA and EMA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): A functional test identifies dopamine agonists selective for D<sub>3</sub>versus D<sub>2</sub>receptors.
Published in: Neuroreport

Ligand: prochlorperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 8.4399995803833 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: promazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 6.519999980926514 pKi
Reference (Journal): Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.
Published in: J Pharmacol Exp Ther

Ligand: quetiapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 7.199999809265137 pKi
Reference (Journal): Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
Published in: Neuropsychopharmacology

Ligand: quinelorane (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: quinelorane (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin secretion and catalepsy.
Published in: J Pharmacol Exp Ther

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
Published in: Eur J Pharmacol

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine.
Published in: Nature

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Lack of discrimination by agonists for D2 and D3 dopamine receptors.
Published in: Neuropsychopharmacology

Ligand: quinpirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor.
Published in: Mol Pharmacol