Target family: 5-HT<sub>3</sub> receptors (type: lgic)
Target: 5-HT<sub>3</sub>A

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro.
Published in: Eur J Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Different efficacy of specific agonists at 5-HT3 receptor splice variants: the role of the extra six amino acid segment.
Published in: Br J Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b)) expressed in Xenopus laevis oocytes.
Published in: Br J Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors.
Published in: Eur J Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors.
Published in: Eur J Pharmacol

Ligand: granisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2012)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: granisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2012)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: ginkgolide B (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3.14 pIC50
Reference (Journal): Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.
Published in: Mol Pharmacol

Ligand: ethanol (Metabolite)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Mutations of L293 in transmembrane two of the mouse 5-hydroxytryptamine3A receptor alter gating and alcohol modulatory actions.
Published in: Br J Pharmacol

Ligand: ethanol (Metabolite)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Alcohols potentiate the function of 5-HT3 receptor-channels on NCB-20 neuroblastoma cells by favouring and stabilizing the open channel state.
Published in: J Physiol (Lond.)

Ligand: ethanol (Metabolite)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): The interaction of trichloroethanol with murine recombinant 5-HT3 receptors.
Published in: Br J Pharmacol

Ligand: ethanol (Metabolite)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity.
Published in: Brain Res Mol Brain Res

Ligand: diltiazem (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1982)
Median affinity: 4.68 pIC50
Reference (Journal): Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.
Published in: Mol Pharmacol

Ligand: diltiazem (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1982)
Median affinity:  pIC50
Reference (Journal): Diltiazem causes open channel block of recombinant 5-HT3 receptors.
Published in: J Physiol (Lond.)

Ligand: diltiazem (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1982)
Median affinity:  pIC50
Reference (Journal): A role for the Val291 residue within the transmembrane domain 2 in diltiazem- and TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester]-mediated 5-hydroxytryptamine type 3A receptor regulations.
Published in: Biol Pharm Bull

Ligand: CSTI-300 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.649999618530273 pKi
Reference (Journal): CSTI-300 (SMP-100); a Novel 5-HT<sub>3</sub> Receptor Partial Agonist with Potential to Treat Patients with Irritable Bowel Syndrome or Carcinoid Syndrome.
Published in: J Pharmacol Exp Ther

Ligand: cocaine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: cocaine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: cilansetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome.
Published in: J Pharmacol Sci

Ligand: Ca2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): An electrophysiological investigation of the properties of a murine recombinant 5-HT3 receptor stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: Ca2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): Ion permeation properties of a cloned human 5-HT3 receptor transiently expressed in HEK 293 cells.
Published in: Amino Acids

Ligand: Ca2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): The role of the agonist binding site in Ca(2+) inhibition of the recombinant 5-HT(3A) receptor.
Published in: Eur J Pharmacol

Ligand: Ca2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): Role of aspartate 298 in mouse 5-HT3A receptor gating and modulation by extracellular Ca2+.
Published in: J Physiol (Lond.)

Ligand: Ca2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A).
Published in: J Physiol (Lond.)

Ligand: bilobalide (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3.33 pIC50
Reference (Journal): Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.
Published in: Mol Pharmacol

Ligand: AZD0328 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pKi
Reference (Journal): Discovery and development of α7 nicotinic acetylcholine receptor modulators.
Published in: J Med Chem

Ligand: azasetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.5 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: alosetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002)
Primary target: yes
Median affinity: 9.5 pKi
Reference (Journal): Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome.
Published in: J Pharmacol Sci

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro.
Published in: Eur J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Probing the role of a conserved M1 proline residue in 5-hydroxytryptamine(3) receptor gating.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The pharmacological and functional characteristics of the serotonin 5-HT(3A) receptor are specifically modified by a 5-HT(3B) receptor subunit.
Published in: J Biol Chem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): General anesthetic-induced channel gating enhancement of 5-hydroxytryptamine type 3 receptors depends on receptor subunit composition.
Published in: J Pharmacol Exp Ther

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: 5-hydroxyindole (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Allosteric potentiation of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells by 5-hydroxyindole and analogues.
Published in: Neuropharmacology

Ligand: 5-hydroxyindole (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): The 5-HT3B subunit confers spontaneous channel opening and altered ligand properties of the 5-HT3 receptor.
Published in: J Biol Chem

Ligand: 5-hydroxyindole (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Diltiazem causes open channel block of recombinant 5-HT3 receptors.
Published in: J Physiol (Lond.)

Ligand: 5-hydroxyindole (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells.
Published in: Br J Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro.
Published in: Eur J Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Allosteric interactions among agonists and antagonists at 5-hydroxytryptamine3 receptors.
Published in: J Neurochem

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Allosteric interactions among agonists and antagonists at 5-hydroxytryptamine3 receptors.
Published in: J Neurochem

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4.5 pEC50
Reference (Journal): Pharmacological characterization of the apparent splice variants of the murine 5-HT3 R-A subunit expressed in Xenopus laevis oocytes.
Published in: Neuropharmacology

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.1 pEC50
Reference (Journal): Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol