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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1899
Target Type SINGLE PROTEIN
Preferred Name Serotonin 3a (5-HT3a) receptor
Synonyms 5-HT-3 | 5-HT3-A | 5-HT3A | 5-HT3R | 5-hydroxytryptamine receptor 3 | 5-hydroxytryptamine receptor 3A | 5HT3R | HTR3 | HTR3A | Serotonin receptor 3A | Serotonin-gated ion channel receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • ion channel > ligand-gated ion channel > 5ht3 receptor

Target Components

Component Description Relationship Accession
5-hydroxytryptamine receptor 3A SINGLE PROTEIN P46098

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111332 Serotonin 3 (5-HT3) receptor PROTEIN COMPLEX
CHEMBL2096904 Serotonin (5-HT) receptor PROTEIN FAMILY
CHEMBL2094132 Serotonin 3 (5-HT3) receptor PROTEIN COMPLEX GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL46 ONDANSETRON Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed
CHEMBL289469 GRANISETRON Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed
CHEMBL1720 PALONOSETRON HYDROCHLORIDE Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed FDA
CHEMBL1200885 ALOSETRON HYDROCHLORIDE Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed
CHEMBL1200940 METOCLOPRAMIDE HYDROCHLORIDE HYDRATE Serotonin 3a (5-HT3a) receptor antagonist 4 ISBN
CHEMBL1201111 ONDANSETRON HYDROCHLORIDE Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed
CHEMBL1237080 GRANISETRON HYDROCHLORIDE Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed
CHEMBL2107387 VORTIOXETINE HYDROBROMIDE Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed PubMed
CHEMBL2368924 Dolasetron Mesylate Serotonin 3a (5-HT3a) receptor antagonist 4 DailyMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000166736
Ensembl ENSG00000166736
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005892 (acetylcholine-gated channel complex)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030054 (cell junction)
GO:0030424 (axon)
GO:0043025 (neuronal cell body)
GO:0045202 (synapse)
GO:0045211 (postsynaptic membrane)
GO:1904602 (serotonin-activated cation-selective channel complex)
GO Molecular Function GO:0004889 (acetylcholine-activated cation-selective channel activity)
GO:0005230 (extracellular ligand-gated ion channel activity)
GO:0005232 (serotonin-activated cation-selective channel activity)
GO:0005249 (voltage-gated potassium channel activity)
GO:0005515 (protein binding)
GO:0015276 (ligand-gated ion channel activity)
GO:0015464 (acetylcholine receptor activity)
GO:0022850 (serotonin-gated cation channel activity)
GO:0042166 (acetylcholine binding)
GO:0051378 (serotonin binding)
GO Biological Process GO:0006810 (transport)
GO:0006811 (ion transport)
GO:0007165 (signal transduction)
GO:0007271 (synaptic transmission, cholinergic)
GO:0034220 (ion transmembrane transport)
GO:0042220 (response to cocaine)
GO:0045471 (response to ethanol)
GO:0071363 (cellular response to growth factor stimulus)
GO:0071805 (potassium ion transmembrane transport)
GO:0098655 (cation transmembrane transport)
Wikipedia HTR3A

Target Cross References - Protein

canSAR P46098
Human Protein Atlas ENSG00000166736
IntAct P46098
Guide to Pharmacology 373
Open Targets ENSG00000166736
PharmGKB PA29555
Pharos P46098 (Tclin)
Reactome R-HSA-975298 (Ligand-gated ion channel transport.)
UniProt B4DSY6 G5E986 O60854 P46098 Q7KZM7 Q99918 Q9BSZ9

Target Cross References - Domain

InterPro IPR006029 (Neurotrans-gated_channel_TM.)
IPR006201 (Neur_channel.)
IPR006202 (Neur_chan_lig-bd.)
IPR008132 (5HT3_rcpt.)
IPR008133 (5HT3_rcpt_A.)
IPR018000 (Neurotransmitter_ion_chnl_CS.)
IPR027361 (Acetylcholine_rcpt_TM.)
Pfam PF02931 (Neur_chan_LBD)
PF02932 (Neur_chan_memb)
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