Target family: 5-Hydroxytryptamine receptors (type: gpcr)
Target: 5-HT<sub>7</sub> receptor

Ligand: 1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 2-bromo-LSD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 2-bromo-LSD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: 2-MPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.
Published in: Biochem Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: 5-MeO-DMT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 6.4 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
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): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: amoxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity: 7.4 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: aripiprazole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: AS-19 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.220000267028809 pKi
Reference (Journal): Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor.
Published in: Bioorg Med Chem

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: bufotenine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: buspirone (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Median affinity: 6.4 pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: buspirone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1986)
Median affinity: 6.4 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: (+)-butaclamol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: capeserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.5 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: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.6 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: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.6 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: 5.3 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1993)
Median affinity: 5.8 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
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): 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): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 7.4 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
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 characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

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): 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): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: cyamemazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.
Published in: Biochem Pharmacol

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 6.9 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: dihydroergocryptine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: dihydroergocryptine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity: 6.8 pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity: 8 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: dipropyl-5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: DM-1451 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: DR-4004 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor.
Published in: J Med Chem

Ligand: DR-4004 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
Published in: J Med Chem

Ligand: E55888 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice.
Published in: Pain

Ligand: EGIS-11150 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pKi
Reference (Journal): Egis-11150: a candidate antipsychotic compound with procognitive efficacy in rodents.
Published in: Neuropharmacology

Ligand: EMDT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 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: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity: 7.3 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: fluperlapine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.3 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: 7.5 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: 7.9 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: 8.1 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: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity: 6.3 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
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: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: iloperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Median affinity: 7 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: iloperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Median affinity: 7.7 pKi
Reference (Journal): Iloperidone binding to human and rat dopamine and 5-HT receptors.
Published in: Eur J Pharmacol

Ligand: m-chlorophenylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: JNJ-18038683 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.199999809265137 pKi
Reference (Journal): Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder.
Published in: J Pharmacol Exp Ther

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6.4 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: LP-12 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.890000343322754 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: 9.239999771118164 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: yes
Median affinity: 9.65999984741211 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: (+)-LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: lurasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2010), EMA (2014)
Primary target: yes
Median affinity: 9.3100004196167 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: LY344864 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.
Published in: Life Sci

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: mesulergine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 7.9 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 7.9 pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: MPDT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 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: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity: 6.5 pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: Antagonist
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: oleamide (Metabolite)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors.
Published in: Biochem Pharmacol

Ligand: OPC 4392 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 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:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.6 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: 7.2 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: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 9.300000190734863 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: pirenperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

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

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKd
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: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: RU 24969 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: SB 207710 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SB 258719 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Published in: Br J Pharmacol

Ligand: SB269970 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.
Published in: Br J Pharmacol

Ligand: SB656104 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Published in: Bioorg Med Chem Lett

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity:  pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity:  pKi
Reference (Journal): Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Published in: Br J Pharmacol

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity:  pKi
Reference (Journal): Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Published in: Proc Natl Acad Sci USA

Ligand: sumatriptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1992)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: [125I]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.
Published in: Neuron

Ligand: [3H]5-CT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.
Published in: Br J Pharmacol

Ligand: [3H]5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: [3H]5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.
Published in: FEBS Lett

Ligand: [3H]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.
Published in: Neuropsychopharmacology

Ligand: [3H]LSD (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.
Published in: FEBS Lett

Ligand: [3H]SB269970 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.92 pKd
Reference (Journal): [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.
Published in: Br J Pharmacol

Ligand: TFMPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: TFMPP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Published in: Mol Pharmacol

Ligand: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1962)
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: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1962)
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: tiospirone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 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: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
Published in: J Biol Chem

Ligand: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: vortioxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: yes
Median affinity: 6.349999904632568 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: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Published in: Br J Pharmacol

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity: 5.6 pKi
Reference (Journal): Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
Published in: J Biol Chem

Ligand: ziprasidone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (2001)
Median affinity: 8.4 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: 8.4 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: 8.8 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