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TargetOther named receptors

Glucagon receptor

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
5
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

GLR_HUMANGCGRHomo sapiens

Glucagon receptor

G protein-coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase32193322,38346960. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system

Quoted from UniProt’s FUNCTION annotation for P47871 (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
GCG0.9990.9000.9000.999
GNAS0.9950.9250.9000.385
GNAQ0.9690.2230.9000.639
GNB10.9610.9240.5000.072
GNAI10.9150.9100.0000.080
GNG20.9070.8230.5000.000
IGHV3-160.8000.8000.0000.000
INS0.7950.0000.0000.791
GIP0.7920.1560.4000.621
VIP0.7870.1050.4000.636

Where it sits in the cell

  • Golgi apparatus

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

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Distal convoluted tubule cells55.3 nCPM
  • Renal collecting duct intercalated cells38.6 nCPM
  • Renal connecting tubule cells28.7 nCPM
  • Loop of henle epithelial cells25.2 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.

  • liver167.2 nTPM
  • kidney49.3 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

cerebral cortex — no resolved target expressed herecerebellum — 0.1 nTPM, from GCGRhippocampal formation — no resolved target expressed hereamygdala — no resolved target expressed herehypothalamus — 0.1 nTPM, from GCGRthalamus — no resolved target expressed herebasal ganglia — no resolved target expressed heremedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: retina 0.7, pituitary gland 0.2, midbrain 0.1, spinal cord 0.1.

0167 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 GCGR 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 · 6

  • retina0.7 nTPM
  • pituitary gland0.2 nTPM
  • cerebellum0.1 nTPM
  • hypothalamus0.1 nTPM
  • midbrain0.1 nTPM
  • spinal cord0.1 nTPM

Peripheral and autonomic · 12

  • liver167.2 nTPM
  • kidney49.3 nTPM
  • adrenal gland2.4 nTPM
  • pancreas1.4 nTPM
  • colon0.8 nTPM
  • small intestine0.6 nTPM
  • thyroid gland0.2 nTPM
  • urinary bladder0.2 nTPM
  • stomach 10.1 nTPM
  • duodenum0.1 nTPM
  • spleen0.1 nTPM
  • salivary gland0.1 nTPM

Transcript is not protein. These are RNA levels for GCGR, 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 5

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

TargetClassTypeValue (nM)pXOrganismAssay
Glucagon receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291802
Glucagon receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291802
Glucagon receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291802
Glucagon receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291802
Glucagon receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291802