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

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 7.960000038146973 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: ziprasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2001)
Primary target: yes
Median affinity: 8.550000190734863 pKi
Reference (Journal): Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
Published in: Neuropsychopharmacology

Ligand: vilazodone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2011)
Primary target: no
Median affinity: 6.179999828338623 pIC50
Reference (Journal): Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Published in: J Med Chem

Ligand: UNC9994 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 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: UNC9994 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKi
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: UNC9975 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.59000015258789 pKi
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: UNC9975 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 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: UNC0006 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.920000076293945 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: UNC0006 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
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: (+)-UH232 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: (+)-UH232 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: (+)-UH232 (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: trifluoperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
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: trifluoperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
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: terguride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Median affinity: 9.1 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: terguride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.9 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: [3H]spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues.
Published in: Br J Pharmacol

Ligand: [3H]spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): Concentration of receptor and ligand revisited in a modified receptor binding protocol for high-affinity radioligands: [3H]Spiperone binding to D2 and D3 dopamine receptors.
Published in: J Neurosci Methods

Ligand: [3H]spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): Cloning and expression of a rat D2 dopamine receptor cDNA.
Published in: Nature

Ligand: [3H]raclopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain.
Published in: Biochem Pharmacol

Ligand: [3H]nemonapride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.9 pKd
Reference (Journal): Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole.
Published in: J Neurochem

Ligand: [3H]N-methylspiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.7 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: sumanirole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease.
Published in: J Pharmacol Exp Ther

Ligand: sulpiride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Lack of discrimination by agonists for D2 and D3 dopamine receptors.
Published in: Neuropsychopharmacology

Ligand: (-)-sulpiride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
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: (-)-sulpiride (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: (-)-sulpiride (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: (+)-sulpiride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
Published in: Nature

Ligand: (+)-sulpiride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.22 pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: (-)-stepholidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.940000057220459 pKi
Reference (Journal): (-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling.
Published in: Psychopharmacology (Berl.)

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

Ligand: sertindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.
Published in: Eur J Pharmacol

Ligand: sertindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
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: (+)-SCH-23390 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Expression and pharmacological characterization of the human D3 dopamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: SB269652 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.380000114440918 pKB
Reference (Journal): A new mechanism of allostery in a G protein-coupled receptor dimer.
Published in: Nat Chem Biol

Ligand: (+)-S-14297 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 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: R-VK4-40 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pKi
Reference (Journal): The highly selective dopamine D<sub>3</sub>R antagonist, R-VK4-40 attenuates oxycodone reward and augments analgesia in rodents.
Published in: Neuropharmacology

Ligand: roxindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 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: roxindole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.6 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: rotigotine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2006), FDA (2007)
Primary target: yes
Median affinity: 10.220000267028809 pKi
Reference (Journal): Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.
Published in: J Med Chem

Ligand: ropinirole (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (2006)
Primary target: yes
Median affinity: 8.140000343322754 pKi
Reference (Journal): Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Published in: J Med Chem

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: yes
Median affinity: 9.359999656677246 pKi
Reference (Journal): Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
Published in: Neuropsychopharmacology

Ligand: raclopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: raclopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 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: raclopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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