General Information of the Protein
Protein ID
PT04591
Protein Name
Solute carrier family 22 member 2
Secondarily
Protein Name
Organic cation transporter 2
Gene Name
SLC22A2
Secondarily
Gene Name
2-Oct
Sequence
MPTTVDDVLEHGGEFHFFQKQMFFLLALLSATFAPIYVGIVFLGFTPDHRCRSPGVAELSLRCGWSPAEELNYTVPGPGPAGEASPRQCRRYEVDWNQSTFDCVDPLASLDTNRSRLPLGPCRDGWVYETPGSSIVTEFNLVCANSWMLDLFQSSVNVGFFIGSMSIGYIADRFGRKLCLLTTVLINAAAGVLMAISPTYTWMLIFRLIQGLVSKAGWLIGYILITEFVGRRYRRTVGIFYQVAYTVGLLVLAGVAYALPHWRWLQFTVSLPNFFFLLYYWCIPESPRWLISQNKNAEAMRIIKHIAKKNGKSLPASLQRLRLEEETGKKLNPSFLDLVRTPQIRKHTMILMYNWFTSSVLYQGLIMHMGLAGDNIYLDFFYSALVEFPAAFMIILTIDRIGRRYPWAASNMVAGAACLASVFIPGDLQWLKIIISCLGRMGITMAYEIVCLVNAELYPTFIRNLGVHICSSMCDIGGIITPFLVYRLTNIWLELPLMVFGVLGLVAGGLVLLLPETKGKALPETIEEAENMQRPRKNKEKMIYLQVQKLDIPLN
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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:9260930, PubMed:9687576). Functions as a Na(+)-independent, bidirectional uniporter (PubMed:9687576, PubMed:21128598). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:9260930, PubMed:9687576, PubMed:15212162). However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (PubMed:15783073). Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters (PubMed:9687576, PubMed:16581093, PubMed:17460754). Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system (PubMed:17460754). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) (PubMed:9260930, PubMed:12089365, PubMed:15212162, PubMed:17072098, PubMed:24961373). Mediates the uptake and efflux of quaternary ammonium compound choline (PubMed:9260930). Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine (PubMed:12538837, PubMed:21128598). Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:12395288, PubMed:16394027). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable).
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Uniprot ID
Primary ID:
O15244

Secondarily ID:
Q5T7Q6
Q6PIQ8
Q8NG62
Q9NQB9
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Ensembl ID
ENSG00000112499
HGNC ID
HGNC:10966
Subcellular Location
Basolateral cell membrane
Basal cell membrane
Apical cell 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: CL000088 , Flp-In-293
Compound ID Compound Name Compound Formula
CP0036757
3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
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C19H24N2
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0001598
1,2,3,4-tetrahydro-9-acridinamine
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C13H14N2
 1
1
IC50 = 680 nM
   TI
   LI
   LO
   TS
CP0000082
CAS_68647
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C18H19N3O
 1
1
IC50 = 890 nM
   TI
   LI
   LO
   TS
CP0066121
N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine
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C18H23NO
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0069487
2-({6-[bis(2-hydroxyethyl)amino]-4,8-bis(piperidin-1-yl)pyrimido[5,4-d][1,3]diazin-2-yl}(2-hydroxyethyl)amino)ethan-1-ol
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C24H40N8O4
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0049757
4-(diisopropylamino)-2-phenyl-2-pyridin-2-ylbutanamide
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C21H29N3O
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0035927
(Cimetidine) N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine,cyanide
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C10H16N6S
 1
1
IC50 = 23000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04368 Solute carrier family 22 member 2 Rattus norvegicus, Rat