ATP-binding cassette sub-family C member 2
SLC and ABC transporters governing uptake and efflux — distinct from the monoamine transporters.
- Measurements
- 10
- Compounds
- 6
- 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.
ATP-binding cassette sub-family C member 2
ATP-dependent transporter of the ATP-binding cassette (ABC) family that hydrolyzes ATP to enable active transport of endogenous and xenobiotic substrates conjugated with glucuronate, glutathione or sulfate. Operates at apical membranes of polarized cells such as hepatocytes, renal and intestinal epithelial cells, where it mediates hepatobiliary and renal excretion of conjugated substrates preventing them from being recycled back into the bloodstream10220572,10421658,11500505,16332456,29175180,30959153,31704245. Involved in canalicular bile production. Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin, enabling bilirubin detoxification10421658. Mediates the efflux of steroid glucuronates and may regulate their hepatobiliary and renal metabolic clearance. Displays low affinity but high transport velocity toward androgen conjugates such as testosterone and dihydrotestosterone glucuronates as well as toward estrogen conjugates including estradiol, estrone and estriol glucuronates29175180,30959153,31704245. May control the hepatobiliary and renal efflux of inflammatory leukotriene C4 (LTC4) and related cysteinyl leukotrienes11500505. Transports sulfated bile salt such as taurolithocholate sulfate16332456. It is functionally inactive toward androgen sulfates39993711. Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors10220572,11500505,12441801. Can confer resistance to several anticancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine, by decreasing accumulation of these drugs in cells10220572,11500505
Quoted from UniProt’s FUNCTION annotation for Q92887 (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.
| Partner | Combined | Experiment | Database | Text mining |
|---|---|---|---|---|
| ABCG2 | 0.979 | 0.100 | 0.800 | 0.889 |
| SLC22A8 | 0.913 | 0.070 | 0.000 | 0.902 |
| UGT1A6 | 0.844 | 0.000 | 0.000 | 0.821 |
| SLCO1B1 | 0.842 | 0.000 | 0.000 | 0.827 |
| SLCO1B3 | 0.817 | 0.000 | 0.000 | 0.801 |
| RDX | 0.811 | 0.292 | 0.000 | 0.733 |
| CRY1 | 0.807 | 0.189 | 0.000 | 0.769 |
| PDZK1 | 0.798 | 0.480 | 0.000 | 0.589 |
| UGT2B7 | 0.798 | 0.000 | 0.000 | 0.774 |
| SLC10A1 | 0.792 | 0.000 | 0.000 | 0.769 |
Where it sits in the cell
UniProt, curated Apical 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.
- Hepatocytes583.5 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.
- liver113.8 nTPM
- intestine37.9 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.
Brain
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: retina 3.6, midbrain 0.1, spinal cord 0.1, pituitary gland 0.1.
Body
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 ABCC2 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
- retina3.6 nTPM
- cerebellum0.4 nTPM
- cerebral cortex0.1 nTPM
- hippocampal formation0.1 nTPM
- amygdala0.1 nTPM
- hypothalamus0.1 nTPM
- basal ganglia0.1 nTPM
- midbrain0.1 nTPM
- spinal cord0.1 nTPM
- pituitary gland0.1 nTPM
Peripheral and autonomic · 16
- liver113.8 nTPM
- small intestine37.9 nTPM
- duodenum36.8 nTPM
- kidney17.3 nTPM
- urinary bladder1.2 nTPM
- spleen1.2 nTPM
- pancreas1.0 nTPM
- skeletal muscle1.0 nTPM
- stomach 10.6 nTPM
- lung0.5 nTPM
- colon0.5 nTPM
- adrenal gland0.4 nTPM
- thyroid gland0.4 nTPM
- salivary gland0.4 nTPM
- heart muscle0.2 nTPM
- smooth muscle0.2 nTPM
Transcript is not protein. These are RNA levels for ABCC2, 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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 2 | Drug transporters | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4028922 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4028922 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4028922 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4028922 |
Other measurements 6
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1006005 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1006005 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1006005 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3533493 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3535468 |
| ATP-binding cassette sub-family C member 2 | Drug transporters | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3535469 |