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TargetDrug transporters

ATP-binding cassette sub-family C member 4

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

Measurements
7
Compounds
4
Binding constants
1
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

MRP4_HUMANABCC4Homo sapiens

ATP-binding cassette sub-family C member 4

ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds and xenobiotics from cells11856762,12523936,15364914,38886124,40138312. Transports a range of endogenous molecules that have a key role in cellular communication and signaling, including cyclic nucleotides such as cyclic AMP (cAMP) and cyclic GMP (cGMP), bile acids, steroid conjugates, urate, and prostaglandins11856762,12523936,12835412,12883481,15364914,15454390,16282361,17959747,18300232,26721430,38886124,40138312. Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC417959747. Mediates the cotransport of bile acids with reduced glutathione (GSH)12523936,12883481,16282361. Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotic molecules11856762,12105214,15454390,17344354,18300232. Confers resistance to anticancer agents such as methotrexate11106685

Quoted from UniProt’s FUNCTION annotation for O15439 (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
MRPS70.9480.0000.0000.948
SLC22A110.8280.0700.0000.820
SLC22A70.8150.0700.0000.807
SLC22A80.8060.0700.0000.797
PDZK10.8050.4450.0000.657
SNX270.7990.6300.0000.479
SLC9A3R10.7710.5220.0000.527
SLC22A120.7680.0700.0000.757
SLC22A60.7340.0700.0000.721
FABP60.7330.0000.0000.730

Where it sits in the cell

  • Plasma membrane
  • Golgi apparatusadditional
  • Vesiclesadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Basolateral cell membrane · Apical cell membrane

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Renal collecting duct intercalated cells1,141 nCPM
  • Microglia943.8 nCPM
  • Megakaryocyte-Erythroid progenitors529.2 nCPM
  • Platelets443.6 nCPM
  • Mast cells410.3 nCPM
  • Megakaryocyte progenitors381.3 nCPM
  • Hematopoietic stem cells355.2 nCPM
  • Proximal tubule cells323.3 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.

  • prostate38.7 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.

017 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 ABCC4 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 · 10

  • cerebral cortex2.9 nTPM
  • spinal cord2.4 nTPM
  • midbrain1.9 nTPM
  • hypothalamus1.7 nTPM
  • hippocampal formation1.4 nTPM
  • amygdala1.4 nTPM
  • pituitary gland1.2 nTPM
  • basal ganglia1.1 nTPM
  • retina0.8 nTPM
  • cerebellum0.1 nTPM

Peripheral and autonomic · 16

  • kidney16.8 nTPM
  • urinary bladder14.4 nTPM
  • colon8.3 nTPM
  • lung7.2 nTPM
  • thyroid gland7.2 nTPM
  • smooth muscle5.9 nTPM
  • small intestine5.0 nTPM
  • stomach 14.7 nTPM
  • skeletal muscle4.7 nTPM
  • duodenum4.6 nTPM
  • spleen3.9 nTPM
  • pancreas3.1 nTPM
  • heart muscle1.9 nTPM
  • salivary gland1.4 nTPM
  • liver1.2 nTPM
  • adrenal gland1.2 nTPM

Transcript is not protein. These are RNA levels for ABCC4, 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.

Equilibrium binding constants 1

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
ATP-binding cassette sub-family C member 4Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3535467

Functional readouts 4

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

TargetClassTypeValue (nM)pXOrganismAssay
ATP-binding cassette sub-family C member 4Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4028924
ATP-binding cassette sub-family C member 4Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4028924
ATP-binding cassette sub-family C member 4Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4028924
ATP-binding cassette sub-family C member 4Drug transportersIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4028924

Other measurements 2

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
ATP-binding cassette sub-family C member 4Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL3533485
ATP-binding cassette sub-family C member 4Drug transportersInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL3533495