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TargetDrug transporters

Solute carrier family 22 member 1

SLC and ABC transporters governing uptake and efflux — distinct from the monoamine transporters.

Measurements
15
Compounds
5
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

S22A1_HUMANSLC22A1Homo sapiens

Solute carrier family 22 member 1

Electrogenic voltage-dependent uniporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics11388889,11408531,12439218,12719534,15389554,16263091,16272756,16581093,19536068,21128598,23680637,24961373,34040533,9187257,9260930,9655880. 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 circulation16263091. Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline12439218,24961373,35469921,9260930. Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover21128598. Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism24961373. Also transport choline, albeit with low affinity40972734. 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 epithelium15817714. Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficiency17460754. Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha)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)11408531,15389554,35469921,9260930
Mediates the uptake of 1-methyl-4-phenylpyridinium (MPP(+))
Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))
Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))
Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))

Quoted from UniProt’s FUNCTION annotation for O15245 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
SPNS30.8920.0650.0000.888
CERS20.8670.4650.0000.762
SLC28A10.8660.0000.0000.860
SLC47A10.8600.0450.0000.855
SLC28A20.8170.0000.0000.815
ABCG20.8100.0940.0000.798
SLC47A20.8020.0450.0000.795
SLCO1B10.7950.0000.0000.769
SLCO1B30.7430.0000.0000.727
ABCB10.7230.0700.0000.704

Where it sits in the cell

UniProt, curated Basolateral cell membrane · Apical cell membrane · Lateral cell membrane · Basal cell membrane · Cell membrane

Expression by cell type

Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Hepatocytes1,217.8 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • liver595.7 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

0596 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of SLC22A1 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 7

  • pituitary gland0.3 nTPM
  • cerebral cortex0.1 nTPM
  • cerebellum0.1 nTPM
  • hippocampal formation0.1 nTPM
  • amygdala0.1 nTPM
  • basal ganglia0.1 nTPM
  • retina0.1 nTPM

Peripheral and autonomic · 14

  • liver595.7 nTPM
  • spleen1.4 nTPM
  • skeletal muscle0.9 nTPM
  • kidney0.8 nTPM
  • thyroid gland0.7 nTPM
  • lung0.4 nTPM
  • pancreas0.4 nTPM
  • stomach 10.3 nTPM
  • salivary gland0.3 nTPM
  • small intestine0.2 nTPM
  • colon0.2 nTPM
  • adrenal gland0.2 nTPM
  • heart muscle0.1 nTPM
  • urinary bladder0.1 nTPM

Transcript is not protein. These are RNA levels for SLC22A1, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 4

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Solute carrier family 22 member 1Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4009597
Solute carrier family 22 member 1Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323354
Solute carrier family 22 member 1Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323354
Solute carrier family 22 member 1Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL994103

Other measurements 11

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Solute carrier family 22 member 1Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL993349
Solute carrier family 22 member 1Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL993349
Solute carrier family 22 member 1Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL993349
Solute carrier family 22 member 1Drug transportersRatio— no normalized value— value does not convert to pXHomo sapiensCHEMBL4009602
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323334
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323334
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323335
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323335
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323336
Solute carrier family 22 member 1Drug transportersFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323336
Solute carrier family 22 member 1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4323337