Broad substrate specificity ATP-binding cassette transporter ABCG2
SLC and ABC transporters governing uptake and efflux — distinct from the monoamine transporters.
- Measurements
- 5
- Compounds
- 1
- 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.
Broad substrate specificity ATP-binding cassette transporter ABCG2
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells11306452,12958161,19506252,20705604,28554189,30405239,31003562. Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme20705604,23189181. Also mediates the efflux of sphingosine-1-P from cells20110355. Acts as a urate exporter functioning in both renal and extrarenal urate excretion19506252,20368174,22132962,31003562,36749388. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates12682043,28554189,30405239. Mediates the secretion of the vitamins riboflavin and biotin into milk (By similarity). Involved in the excretion of the riboflavin-derived compound lumichrome into the intestinal lumen and in its secretion into milk39337371. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux11306452,12477054,15670731,18056989,31254042. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity). In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
Quoted from UniProt’s FUNCTION annotation for Q9UNQ0 (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 |
|---|---|---|---|---|
| ABCC2 | 0.979 | 0.100 | 0.800 | 0.889 |
| ABCC1 | 0.971 | 0.100 | 0.000 | 0.968 |
| SLCO1B1 | 0.886 | 0.000 | 0.000 | 0.886 |
| SLC2A9 | 0.881 | 0.045 | 0.000 | 0.873 |
| SLC22A12 | 0.869 | 0.094 | 0.000 | 0.860 |
| BSG | 0.841 | 0.000 | 0.000 | 0.839 |
| MRPS7 | 0.813 | 0.000 | 0.000 | 0.813 |
| SLC22A1 | 0.810 | 0.094 | 0.000 | 0.798 |
| SLC22A8 | 0.808 | 0.094 | 0.000 | 0.796 |
| ALB | 0.807 | 0.000 | 0.000 | 0.806 |
Where it sits in the cell
- Plasma membrane
- Nucleoplasmadditional
Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.
UniProt, curated Cell membrane · Apical cell membrane · Mitochondrion membrane
Expression by cell type
Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Breast lactating cells316.5 nCPM
- Hofbauer cells298.9 nCPM
- Enterocytes267.3 nCPM
- Vascular endothelial cells142 nCPM
- Extravillous trophoblasts116.4 nCPM
- Colonocytes104.6 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.
- intestine83.2 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Functional readouts 1
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Drug transporters | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4478426 |
Other measurements 4
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 |
|---|---|---|---|---|---|---|
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Drug transporters | GI50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4478434 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Drug transporters | GI50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4478435 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Drug transporters | GI50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4478436 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Drug transporters | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4478441 |