General Information of the Protein
Protein ID
PT06607
Protein Name
Solute carrier family 22 member 3
Secondarily
Protein Name
Extraneuronal monoamine transporter
Organic cation transporter 3
Gene Name
SLC22A3
Secondarily
Gene Name
EMTH
OCT3
Sequence
MPSFDEALQRVGEFGRFQRRVFLLLCLTGVTFAFLFVGVVFLGTQPDHYWCRGPSAAALAERCGWSPEEEWNRTAPASRGPEPPERRGRCQRYLLEAANDSASATSALSCADPLAAFPNRSAPLVPCRGGWRYAQAHSTIVSEFDLVCVNAWMLDLTQAILNLGFLTGAFTLGYAADRYGRIVIYLLSCLGVGVTGVVVAFAPNFPVFVIFRFLQGVFGKGTWMTCYVIVTEIVGSKQRRIVGIVIQMFFTLGIIILPGIAYFIPNWQGIQLAITLPSFLFLLYYWVVPESPRWLITRKKGDKALQILRRIAKCNGKYLSSNYSEITVTDEEVSNPSFLDLVRTPQMRKCTLILMFAWFTSAVVYQGLVMRLGIIGGNLYIDFFISGVVELPGALLILLTIERLGRRLPFAASNIVAGVACLVTAFLPEGIAWLRTTVATLGRLGITMAFEIVYLVNSELYPTTLRNFGVSLCSGLCDFGGIIAPFLLFRLAAVWLELPLIIFGILASICGGLVMLLPETKGIALPETVDDVEKLGSPHSCKCGRNKKTPVSRSHL
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC22 family of organic cation and anion transporters
Function
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:10196521, PubMed:10966924, PubMed:12538837, PubMed:17460754, PubMed:20858707). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:10966924). Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter (PubMed:12538837). Implicated in monoamine neurotransmitters uptake such as dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, histamine, serotonin and tyramine, thereby supporting a role in homeostatic regulation of aminergic neurotransmission in the brain (PubMed:10196521, PubMed:16581093, PubMed:20858707). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency (PubMed:17460754). May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow (PubMed:10966924). May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Mediates the transport of polyamine spermidine and putrescine (By similarity). Mediates the bidirectional transport of polyamine agmatine (PubMed:12538837). Also transports guanidine (PubMed:10966924). May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
O75751

Secondarily ID:
Q5SYN6
Q9UP02
    Show/Hide
Ensembl ID
ENSG00000146477
HGNC ID
HGNC:10967
Subcellular Location
Cell membrane
Apical cell membrane
Basolateral cell membrane
Mitochondrion membrane
Endomembrane system
Nucleus membrane
Nucleus outer membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0458165
N-(2-chloroethyl)-N-methyl-9H-fluoren-9-amine
   Show/Hide
C16H16ClN
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0306009
(2E)-1-ethyl-2-[(1-ethyl-2-quinolin-1-iumyl)methylidene]quinoline;chloride
   Show/Hide
C23H23N2+
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0042374
(11beta)-11,21-dihydroxypregn-4-ene-3,20-dione
   Show/Hide
C21H30O4
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0046285
(1E)-2-[6-[[amino-[(E)-[amino-(4-chloroanilino)methylene]amino]methylene]amino]hexyl]-1-[amino-(4-chloroanilino)methylene]guanidine;hydrochloride
   Show/Hide
C22H30Cl2N10
 1
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
CP0493666
2-(4-iodophenyl)guanidine
   Show/Hide
C7H8IN3
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0436865
2-(4-tert-butylphenyl)guanidine
   Show/Hide
C11H17N3
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0047815
1N-amino(immino)methyl-4-chloroaniline
   Show/Hide
C7H8ClN3
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0006292
(1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-triene-5,14-diol
   Show/Hide
C18H24O2
 1
1
IC50 = 2880 nM
   TI
   LI
   LO
   TS
CP0038813
(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
   Show/Hide
C21H30O2
 1
1
IC50 = 4280 nM
   TI
   LI
   LO
   TS
CP0398506
METIPRENALINE
   Show/Hide
C12H19NO3
 1
1
IC50 = 4380 nM
   TI
   LI
   LO
   TS
CP0112201
1N-amino(immino)methyl-4-methylaniline
   Show/Hide
C8H11N3
 1
1
IC50 = 4600 nM
   TI
   LI
   LO
   TS
CP0134614
2-(4-bromophenyl)guanidine
   Show/Hide
C7H8BrN3
 1
1
IC50 = 4800 nM
   TI
   LI
   LO
   TS
CP0041351
2,2&#39;-THIOBIS(4,6-DICHLOROPHENOL)
   Show/Hide
C12H6Cl4O2S
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0134865
Benzyl-(2-chloro-ethyl)-(1-methyl-2-phenoxy-ethyl)-amine
   Show/Hide
C18H22ClNO
 1
1
IC50 = 6130 nM
   TI
   LI
   LO
   TS
CP0051682
1N-amino(immino)methyl-3-chloroaniline
   Show/Hide
C7H8ClN3
 1
1
IC50 = 7600 nM
   TI
   LI
   LO
   TS
CP0014442
4-[5-(4-amidinophenoxy)pentoxy]benzamidine;2-hydroxyethanesulfonic acid
   Show/Hide
C19H24N4O2
 1
1
IC50 = 9500 nM
   TI
   LI
   LO
   TS
CP0076561
3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N'-sulfamoylpropanimidamide
   Show/Hide
C8H15N7O2S3
 1
1
IC50 = 10700 nM
   TI
   LI
   LO
   TS
CP0040814
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone
   Show/Hide
C19H21N5O4
 1
1
IC50 = 12600 nM
   TI
   LI
   LO
   TS
CP0000082
CAS_68647
   Show/Hide
C18H19N3O
 1
1
IC50 = 17400 nM
   TI
   LI
   LO
   TS
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
   Show/Hide
C29H31N7O
 1
1
IC50 = 25500 nM
   TI
   LI
   LO
   TS
CP0194487
2-(4-fluorophenyl)guanidine
   Show/Hide
C7H8FN3
 1
1
IC50 = 27800 nM
   TI
   LI
   LO
   TS
CP0002490
1,4-bis[2-(2-hydroxyethylamino)ethylamino]-5,8-bis(oxidanyl)anthracene-9,10-dione;hydrochloride
   Show/Hide
C22H28N4O6
 1
1
IC50 = 60500 nM
   TI
   LI
   LO
   TS
CP0076378
(4S)-4,11-DIETHYL-4-HYDROXY-3,14-DIOXO-3,4,12,14-TETRAHYDRO-1H-PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLIN-9-YL 1,4'-BIPIPERIDINE-1'-CARBOXYLATE
   Show/Hide
C33H38N4O6
 1
1
IC50 = 74600 nM
   TI
   LI
   LO
   TS
CP0222047
1-phenylguanidine
   Show/Hide
C7H9N3
 1
1
IC50 = 99800 nM
   TI
   LI
   LO
   TS
CP0261931
(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium-7-one
   Show/Hide
C21H26NO4+
 1
1
Km = 22500 nM
   TI
   LI
   LO
   TS
CP0402053
N-phenyl-N-piperidin-4-ylpropanamide
   Show/Hide
C14H20N2O
 1
1
Km = 49100 nM
   TI
   LI
   LO
   TS
CP0072630
(-)-(5R)-4,5-Epoxy-3-hydroxy-9alpha-methylmorphinan-6-one
   Show/Hide
C17H19NO3
 1
1
Km = 755000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Organic cation transporter 3 (OCT3) )
Target Type Literature-reported Target