General Information of the Protein
Protein ID
PT06157
Protein Name
Solute carrier family 22 member 1
Secondarily
Protein Name
Organic cation transporter 1
Gene Name
SLC22A1
Secondarily
Gene Name
1-Oct
Sequence
MPTVDDVLEQVGEFGWFQKQAFLLLCLISASLAPIYVGIVFLGFTPGHYCQNPGVAELSQRCGWSQAEELNYTVPGLGPSDEASFLSQCMRYEVDWNQSTLDCVDPLSSLVANRSQLPLGPCEHGWVYDTPGSSIVTEFNLVCGDAWKVDLFQSCVNLGFFLGSLVVGYIADRFGRKLCLLVTTLVTSVSGVLTAVAPDYTSMLLFRLLQGMVSKGSWVSGYTLITEFVGSGYRRTTAILYQMAFTVGLVGLAGVAYAIPDWRWLQLAVSLPTFLFLLYYWFVPESPRWLLSQKRTTRAVRIMEQIAQKNGKVPPADLKMLCLEEDASEKRSPSFADLFRTPNLRKHTVILMYLWFSCAVLYQGLIMHVGATGANLYLDFFYSSLVEFPAAFIILVTIDRIGRIYPIAASNLVTGAACLLMIFIPHELHWLNVTLACLGRMGATIVLQMVCLVNAELYPTFIRNLGMMVCSALCDLGGIFTPFMVFRLMEVWQALPLILFGVLGLTAGAMTLLLPETKGVALPETIEEAENLGRRKSKAKENTIYLQVQTGKSSST
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Organism
Rattus norvegicus, Rat
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:7990927, PubMed:8955087, PubMed:10570053, PubMed:10997918, PubMed:10864577, PubMed:11502595, PubMed:11408531, PubMed:12395288, PubMed:16142924, PubMed:15640376, PubMed:16272756, PubMed:15662044, PubMed:16581093, PubMed:17567940). Functions as a pH- and Na(+)-independent, bidirectional transporter (PubMed:8955087, PubMed:16142924). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (PubMed:8955087, PubMed:9405386, PubMed:16142924, PubMed:17567940). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed in the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds from the blood by hepatic and renal clearance (PubMed:7990927, PubMed:9703985, PubMed:10997918). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal excretion and elimination of organic cations from the systemic circulation (By similarity). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, neurotransmitters dopamine, serotonin, noradrenaline, adrenaline and histamine, and quaternary ammonium compound such as choline (PubMed:8955087, PubMed:9776363, PubMed:10570053, PubMed:11502595, PubMed:11408531, PubMed:11758759, PubMed:15662044, PubMed:16581093, PubMed:17567940). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (By similarity). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (By similarity). Contributes to the influx and efflux of fatty acid carriers carnitines and acylcarnitines across the basolateral membrane of hepatocytes, from the liver to the systemic circulation and inversely and may be involved in regulating the systemic availability of hepatic acylcarnitines (By similarity). 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 (By similarity). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (By similarity). May contribute to the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Also mediates 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:8955087, PubMed:10864577, PubMed:11408531, PubMed:12395288).
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Uniprot ID
Primary ID:
Q63089

Secondarily ID:
O35882
Q6AYW1
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Ensembl ID
ENSG00000175003
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0416744
1-propan-2-yl-2-[(1-propan-2-ylquinolin-1-ium-4-yl)methylidene]quinoline
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C25H27N2+
 1
1
Ki = 110 nM
   TI
   LI
   LO
   TS
CP0306009
(2E)-1-ethyl-2-[(1-ethyl-2-quinolin-1-iumyl)methylidene]quinoline;chloride
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C23H23N2+
 1
1
Ki = 500 nM
   TI
   LI
   LO
   TS
CP0869435
Cyanine-863
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C24H26ClN3
 1
1
Ki = 670 nM
   TI
   LI
   LO
   TS
CP0041905
2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2)
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C9H9Cl2N3
 1
1
Ki = 1400 nM
   TI
   LI
   LO
   TS
CP0078400
QUININE
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C20H24N2O2
 1
1
Ki = 4300 nM
   TI
   LI
   LO
   TS
CP0034615
(6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol
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C20H24N2O2
 1
1
Ki = 6000 nM
   TI
   LI
   LO
   TS
CP0398506
METIPRENALINE
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C12H19NO3
 1
1
Ki = 25000 nM
   TI
   LI
   LO
   TS
CP0042374
(11beta)-11,21-dihydroxypregn-4-ene-3,20-dione
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C21H30O4
 1
1
Ki = 72000 nM
   TI
   LI
   LO
   TS
CP0186826
CAS_39484
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C12H12N+
 1
1
Km = 13000 nM
   TI
   LI
   LO
   TS