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Target Report Card

Target Name and Classification

Target ID CHEMBL228
Target Type SINGLE PROTEIN
Preferred Name Serotonin transporter
Synonyms 5HT transporter | 5HTT | HTT | SERT | SERT | SLC6A4 | Sodium-dependent serotonin transporter | Solute carrier family 6 member 4
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transporter > electrochemical transporter > slc superfamily of solute carriers > slc06 neurotransmitter transporter family

Target Components

Component Description Relationship Accession
Sodium-dependent serotonin transporter SINGLE PROTEIN P31645

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2095201 Monoamine transporters; serotonin & dopamine SELECTIVITY GROUP
CHEMBL2111346 Serotonin and norepinephrine transporters (SERT/NET) SELECTIVITY GROUP
CHEMBL2363064 Monoamine transporter PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1113 AMOXAPINE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1118 DESVENLAFAXINE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1409 FLUVOXAMINE MALEATE Serotonin transporter inhibitor 4 FDA
CHEMBL1692 IMIPRAMINE HYDROCHLORIDE Serotonin transporter inhibitor 4 PubMed
CHEMBL1708 PAROXETINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1709 SERTRALINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed FDA
CHEMBL1200322 ESCITALOPRAM OXALATE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1200328 DULOXETINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed PubMed
CHEMBL1200332 PROTRIPTYLINE HYDROCHLORIDE Serotonin transporter inhibitor 4 PubMed
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1200595 CHLORPHENTERMINE HYDROCHLORIDE Serotonin transporter substrate 4 PubMed PubMed
CHEMBL1200609 PAROXETINE MESYLATE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1200631 IMIPRAMINE PAMOATE Serotonin transporter inhibitor 4 PubMed
CHEMBL1200710 CLOMIPRAMINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed PubMed PubMed
CHEMBL1200781 CITALOPRAM HYDROBROMIDE Serotonin transporter inhibitor 4 FDA
CHEMBL1200798 TRAZODONE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed FDA
CHEMBL1200964 AMITRIPTYLINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1201066 VENLAFAXINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed PubMed PubMed
CHEMBL1201156 NORTRIPTYLINE HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed FDA
CHEMBL1201728 DESVENLAFAXINE SUCCINATE Serotonin transporter inhibitor 4 DailyMed
CHEMBL1615374 VILAZODONE HYDROCHLORIDE Serotonin transporter inhibitor 4 FDA PubMed
CHEMBL2096626 MILNACIPRAN HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL2105732 LEVOMILNACIPRAN HYDROCHLORIDE Serotonin transporter inhibitor 4 DailyMed
CHEMBL2107387 VORTIOXETINE HYDROBROMIDE Serotonin transporter inhibitor 4 DailyMed PubMed
CHEMBL3039565 DESVENLAFAXINE FUMARATE Serotonin transporter inhibitor 4 FDA
CHEMBL3545044 ITI-007 Serotonin transporter inhibitor 3 Other PubMed PubMed
CHEMBL1631540 GSK163090 Serotonin transporter antagonist 2 PubMed
CHEMBL2103829 FAXELADOL Serotonin transporter inhibitor 2 PubMed
CHEMBL2104986 TEDATIOXETINE Serotonin transporter inhibitor 2 Other Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000108576
Ensembl ENSG00000108576
GO Cellular Component GO:0005768 (endosome)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0010008 (endosome membrane)
GO:0012505 (endomembrane system)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0043005 (neuron projection)
GO:0045121 (membrane raft)
GO:0098793 (presynapse)
GO Molecular Function GO:0005328 (neurotransmitter:sodium symporter activity)
GO:0005335 (serotonin:sodium symporter activity)
GO:0005515 (protein binding)
GO:0008504 (monoamine transmembrane transporter activity)
GO:0015222 (serotonin transmembrane transporter activity)
GO:0015293 (symporter activity)
GO:0017022 (myosin binding)
GO:0017075 (syntaxin-1 binding)
GO:0017137 (Rab GTPase binding)
GO:0019811 (cocaine binding)
GO:0042803 (protein homodimerization activity)
GO:0046872 (metal ion binding)
GO:0050998 (nitric-oxide synthase binding)
GO:0051015 (actin filament binding)
GO Biological Process GO:0001666 (response to hypoxia)
GO:0006810 (transport)
GO:0006836 (neurotransmitter transport)
GO:0006837 (serotonin transport)
GO:0007268 (chemical synaptic transmission)
GO:0007420 (brain development)
GO:0007584 (response to nutrient)
GO:0007613 (memory)
GO:0007623 (circadian rhythm)
GO:0009636 (response to toxic substance)
GO:0010033 (response to organic substance)
GO:0010628 (positive regulation of gene expression)
GO:0015844 (monoamine transport)
GO:0021794 (thalamus development)
GO:0021941 (negative regulation of cerebellar granule cell precursor proliferation)
GO:0032227 (negative regulation of synaptic transmission, dopaminergic)
GO:0032355 (response to estradiol)
GO:0035176 (social behavior)
GO:0042310 (vasoconstriction)
GO:0042493 (response to drug)
GO:0042713 (sperm ejaculation)
GO:0045665 (negative regulation of neuron differentiation)
GO:0045787 (positive regulation of cell cycle)
GO:0046621 (negative regulation of organ growth)
GO:0048854 (brain morphogenesis)
GO:0051259 (protein oligomerization)
GO:0051260 (protein homooligomerization)
GO:0051610 (serotonin uptake)
GO:0055085 (transmembrane transport)
GO:0071300 (cellular response to retinoic acid)
GO:0071310 (cellular response to organic substance)
GO:0071321 (cellular response to cGMP)
Wikipedia Serotonin_transporter

Target Cross References - Protein

canSAR P31645
Human Protein Atlas ENSG00000108576
IntAct P31645
Guide to Pharmacology 928
MICAD NBK23298 (Serotonin transporter (SERT); 5-HT)
NBK23385 (Serotonin transporter)
NBK23720 (Serotonin transporter (SERT))
Open Targets ENSG00000108576
PharmGKB PA312
Reactome R-HSA-380615 (Serotonin clearance from the synaptic cleft.)
UniProt P31645 Q5EE02

Target Cross References - Domain

InterPro IPR000175 (Na/ntran_symport.)
IPR013086 (Na/ntran_symport_serotonin_N.)
Pfam PF00209 (SNF)
PF03491 (5HT_transport_N)

Target Cross References - Structure

PDBe 5I6X 5I6Z 5I71 5I73 5I74 5I75
CREDO 5I6X 5I6Z 5I71 5I73 5I74 5I75
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