General Information of the Protein
Protein ID
PT03795
Protein Name
Solute carrier family 22 member 1
Secondarily
Protein Name
Organic cation transporter 1
Gene Name
SLC22A1
Secondarily
Gene Name
1-Oct
Sequence
MPTVDDILEQVGESGWFQKQAFLILCLLSAAFAPICVGIVFLGFTPDHHCQSPGVAELSQRCGWSPAEELNYTVPGLGPAGEAFLGQCRRYEVDWNQSALSCVDPLASLATNRSHLPLGPCQDGWVYDTPGSSIVTEFNLVCADSWKLDLFQSCLNAGFLFGSLGVGYFADRFGRKLCLLGTVLVNAVSGVLMAFSPNYMSMLLFRLLQGLVSKGNWMAGYTLITEFVGSGSRRTVAIMYQMAFTVGLVALTGLAYALPHWRWLQLAVSLPTFLFLLYYWCVPESPRWLLSQKRNTEAIKIMDHIAQKNGKLPPADLKMLSLEEDVTEKLSPSFADLFRTPRLRKRTFILMYLWFTDSVLYQGLILHMGATSGNLYLDFLYSALVEIPGAFIALITIDRVGRIYPMAMSNLLAGAACLVMIFISPDLHWLNIIIMCVGRMGITIAIQMICLVNAELYPTFVRNLGVMVCSSLCDIGGIITPFIVFRLREVWQALPLILFAVLGLLAAGVTLLLPETKGVALPETMKDAENLGRKAKPKENTIYLKVQTSEPSGT
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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:9187257, PubMed:11388889, PubMed:9655880, PubMed:11408531, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:12439218, PubMed:12719534). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily 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 (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:9260930, PubMed:24961373, PubMed:35469921, PubMed:12439218). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). 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). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:9260930, PubMed:11408531, PubMed:15389554, PubMed:35469921).
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Uniprot ID
Primary ID:
O15245

Secondarily ID:
A6NFF3
A8K1H2
C9JSU6
O15395
Q9NQD4
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Ensembl ID
ENSG00000175003
HGNC ID
HGNC:10963
Subcellular Location
Basolateral cell membrane
Apical cell membrane
Lateral cell membrane
Basal cell membrane
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 = 37000 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 = 81000 nM
   TI
   LI
   LO
   TS
CP0001598
1,2,3,4-tetrahydro-9-acridinamine
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C13H14N2
 1
1
IC50 = 83000 nM
   TI
   LI
   LO
   TS
CP0000082
CAS_68647
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C18H19N3O
 1
1
IC50 > 100000 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 > 100000 nM
   TI
   LI
   LO
   TS
CP0049757
4-(diisopropylamino)-2-phenyl-2-pyridin-2-ylbutanamide
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C21H29N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0066121
N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine
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C18H23NO
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS