Target family: 5-Hydroxytryptamine receptors (type: gpcr)
Target: 5-HT<sub>6</sub> receptor

Ligand: 1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 2-bromo-LSD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: 5-benzyloxytryptamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: 5-benzyloxytryptamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: 5-benzyloxytryptamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 5-MeO-DMT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: α-ergocryptine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: amoxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: amoxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity: 7.3 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: amoxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: aripiprazole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: no
Median affinity: 6.800000190734863 pKi
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: BRL-15572 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 7.5 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 7.5 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: bufotenine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: capeserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties.
Published in: J Pharmacol Exp Ther

Ligand: cerlapirdine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.890000343322754 pKi
Reference (Journal): SAM-531, N,N-dimethyl-3-{[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]oxy} propan-1-amine, a novel serotonin-6 receptor antagonist with preclinical pro-cognitive efficacy.
Published in: Alzheimers Dement

Ligand: CGS-12066 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 8.4 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity:  pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 6.9 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 6.8 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: dihydroergocristine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: dimethyltryptamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: DM-1451 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: donitriptan (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine.
Published in: J Pharmacol Exp Ther

Ligand: duloxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2004)
Median affinity: 6.4 pKi
Reference (Journal): Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.
Published in: Neuropsychopharmacology

Ligand: E6801 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
Published in: J Med Chem

Ligand: EMD-386088 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.130000114440918 pIC50
Reference (Journal): 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: EMDT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Published in: J Med Chem

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: fluoxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1987)
Median affinity: 5.8 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: fluperlapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: fluperlapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: fluperlapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: fluphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity:  pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: fluphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 7.8 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ICI 169369 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: idalopirdine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.079999923706055 pKi
Reference (Journal): Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
Published in: J Med Chem

Ligand: iloperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Median affinity: 7.4 pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: iloperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Median affinity: 7.2 pKi
Reference (Journal): Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Published in: Neuropsychopharmacology

Ligand: m-chlorophenylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: intepirdine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.770000457763672 pKi
Reference (Journal): Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
Published in: J Med Chem

Ligand: lergotrile (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity:  pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity:  pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: LY 165,163 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: Lysergide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: Lysergide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: Lysergide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: MPDT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Published in: J Med Chem

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity: 8 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity:  pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity:  pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity: 8 pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: OPC 4392 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 7.5 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.8 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.1 pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Median affinity: 7.2 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity: 5.6 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: Ro 04-6790 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
Published in: Br J Pharmacol

Ligand: Ro 04-6790 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: Ro 04-6790 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: Ro 04-6790 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
Published in: Br J Pharmacol

Ligand: Ro 63-0563 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
Published in: Br J Pharmacol

Ligand: Ro 63-0563 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: Ro 63-0563 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
Published in: Br J Pharmacol

Ligand: Ro 63-0563 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: RU 24969 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: S 16924 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol.
Published in: J Pharmacol Exp Ther

Ligand: SB258585 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.529999732971191 pKi
Reference (Journal): Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue.
Published in: Br J Pharmacol

Ligand: SB 271046 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKi
Reference (Journal): 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Published in: J Med Chem

Ligand: SB357134 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Published in: Bioorg Med Chem Lett

Ligand: SB399885 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models.
Published in: Eur J Pharmacol

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity: 5.6 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity: 5.2 pKi
Reference (Journal): Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
Published in: J Neurochem

Ligand: [11C]GSK215083 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKi
Reference (Journal): Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor.
Published in: J Nucl Med

Ligand: [125I]SB258585 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models.
Published in: Eur J Pharmacol

Ligand: [3H]5-CT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: [3H]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Published in: Mol Pharmacol

Ligand: [3H]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: [3H]Ro 63-0563 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKd
Reference (Journal): The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Published in: Mol Pharmacol

Ligand: TFMPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: TFMPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 8.2 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 7.2 pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: tiospirone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
Published in: J Neurochem

Ligand: tiospirone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther

Ligand: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Published in: Mol Pharmacol

Ligand: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Published in: Neuropharmacology

Ligand: vortioxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: no
Median affinity: 6.480000019073486 pKi
Reference (Journal): Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Published in: J Med Chem

Ligand: WAY-181187 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466.
Published in: Neuropsychopharmacology

Ligand: WAY-208466 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.319999694824219 pKi
Reference (Journal): Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Published in: Bioorg Med Chem

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Published in: Br J Pharmacol

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Median affinity: 8.3 pKi
Reference (Journal): Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
Published in: Psychopharmacology (Berl.)

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Median affinity: 8.9 pKi
Reference (Journal): Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
Published in: J Pharmacol Exp Ther