Target family: 5-Hydroxytryptamine receptors (type: gpcr)
Target: 5-HT<sub>4</sub> receptor

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKd
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.
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 four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
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 human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
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 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
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 and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: BIMU 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: BIMU 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: BIMU 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: BIMU 1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: BIMU 8 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: BIMU 8 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: BIMU 8 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: capeserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 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: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1993)
Median affinity: 7.5 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: cisapride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: DAU 6285 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: DAU 6285 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: donecopride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.180000305175781 pKi
Reference (Journal): Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatment.
Published in: Proc Natl Acad Sci USA

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.
Published in: Br J Pharmacol

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: GR 125487 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: GR 125487 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: GR 125487 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.6 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: metoclopramide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 6 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: ML 10302 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.
Published in: J Med Chem

Ligand: ML 10302 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: ML 10302 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: ML 10302 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: ML 10302 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
Published in: Br J Pharmacol

Ligand: ML 10375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: ML 10375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: ML 10375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
Published in: Br J Pharmacol

Ligand: ML 10375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: ML 10375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: mosapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: PF-04995274 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pKi
Reference (Journal): Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
Published in: J Med Chem

Ligand: piboserod (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: piboserod (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: piboserod (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and pharmacological activity of metabolites of the 5-HT(4) receptor antagonist SB-207266.
Published in: Bioorg Med Chem

Ligand: prucalopride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2018)
Median affinity:  pKi
Reference (Journal): The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Published in: Eur J Pharmacol

Ligand: prucalopride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2018)
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: relenopride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pKi
Reference (Journal): Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation.
Published in: Neurogastroenterol Motil

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: renzapride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: RO 116 1148 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists.
Published in: J Biol Chem

Ligand: RS 100235 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: RS 100235 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.
Published in: Br J Pharmacol

Ligand: RS 116 0086 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists.
Published in: J Biol Chem

Ligand: RS 39604 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: RS 39604 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.
Published in: Br J Pharmacol

Ligand: RS 39604 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: RS 57639 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: RS 67333 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: RS 67333 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: RS67506 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pEC50
Reference (Journal): Peripheral 5-HT4 receptors.
Published in: FASEB J

Ligand: SB 203186 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SB 204070 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: SB 204070 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: SB 204070 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Published in: Br J Pharmacol

Ligand: SB 204070 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: SB 204070 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: SB 207710 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SC 53116 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: SDZ 205557 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: SDZ 205557 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): 5-Hydroxytryptamine2B receptor mediates contraction in the mesenteric artery of mineralocorticoid hypertensive rats.
Published in: Hypertension

Ligand: [11C]SB207145 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Journal): Mass dose effects and in vivo affinity in brain PET receptor studies--a study of cerebral 5-HT4 receptor binding with [11C]SB207145.
Published in: Nucl Med Biol

Ligand: [123I]SB 207710 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.069999694824219 pKd
Reference (Journal): [<sup>125</sup>I]-SB 207710, A potent, slective radioligand for 5-HT<sub>4</sub> receptors.
Published in: Br J Pharmacol

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
Published in: Br J Pharmacol

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: [3H]GR 113808 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: [3H]RS 57639 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKd
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: [3H]RS 57639 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: TD-8954 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.
Published in: Bioorg Med Chem Lett

Ligand: tegaserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002)
Median affinity:  pKi
Reference (Journal): Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
Published in: J Neurochem

Ligand: tegaserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (2002)
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Published in: J Neurochem

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6.8 pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7.1 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: velusetrag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.699999809265137 pKi
Reference (Journal): Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation.
Published in: Bioorg Med Chem Lett

Ligand: velusetrag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.699999809265137 pKi
Reference (Journal): The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: vilazodone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2011)
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Published in: J Med Chem

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.
Published in: Neuropharmacology

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
Published in: FEBS Lett

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.
Published in: Neuroreport

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Published in: Eur J Pharmacol

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants.
Published in: EMBO J

Ligand: zacopride (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
Published in: J Neurochem