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TargetDrug transporters

ATP-dependent translocase ABCB1

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

Measurements
25
Compounds
8
Binding constants
16
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

MDR1_HUMANABCB1Homo sapiens

ATP-dependent translocase ABCB1

Translocates drugs and phospholipids across the membrane2897240,35970996,8898203,9038218,35507548. Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins8898203. Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells2897240,35970996,9038218

Quoted from UniProt’s FUNCTION annotation for P08183 (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
CYP3A50.9200.0500.0000.913
IGKV2D-290.9070.9070.0000.000
CYP3A40.8860.0500.0000.876
SLCO1B10.8830.0000.0000.877
CYP2C190.8580.0690.0000.850
SLCO1B30.8440.0000.0000.836
NR1I20.8420.0000.0000.832
ABCF2-20.8120.0710.0000.803
ABCF20.8120.0710.0000.803
PPIG0.8090.0680.0000.802

Where it sits in the cell

  • Plasma membrane

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 · Cytoplasm

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.

  • Adrenal cortex cells747.9 nCPM
  • Hematopoietic stem cells640 nCPM
  • Enterocytes630.7 nCPM
  • Vascular endothelial cells507.4 nCPM
  • Colonocytes256 nCPM
  • NK-cells216.6 nCPM
  • Thymocytes162.6 nCPM
  • Innate lymphoid cells147.7 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.

  • adrenal gland96.1 nTPM
  • intestine66.6 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 16

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

TargetClassTypeValue (nM)pXOrganismAssay
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076230
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076230
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076230
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076230
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076229
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076229
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076229
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076229
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076224
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076224
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076224
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076224
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076225
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076225
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076225
ATP-dependent translocase ABCB1Drug transportersKi— no normalized value— value does not convert to pXMus musculusCHEMBL2076225

Other measurements 9

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-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076240
ATP-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2075640
ATP-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076203
ATP-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076203
ATP-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2076203
ATP-dependent translocase ABCB1Drug transportersActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2075633
ATP-dependent translocase ABCB1Drug transportersRatio— no normalized value— value does not convert to pXHomo sapiensCHEMBL827620
ATP-dependent translocase ABCB1Drug transportersTransport— no normalized value— value does not convert to pXHomo sapiensCHEMBL825762
ATP-dependent translocase ABCB1Drug transportersRatio— no normalized value— value does not convert to pXHomo sapiensCHEMBL884551