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PsychedeliaDokholyan Laboratory
TargetNuclear receptors

Glucocorticoid receptor

Steroid and other ligand-activated transcription factors.

Measurements
30
Compounds
12
Binding constants
7
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

GCR_HUMANNR3C1Homo sapiens

Glucocorticoid receptor

Receptor for glucocorticoids (GC)27120390,37478846. Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors28139699. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling9590696. Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay25775514. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
Has transcriptional activation and repression activity11435610,15769988,15866175,17635946,19141540,19248771,20484466,21664385,23820903. Mediates glucocorticoid-induced apoptosis23303127. Promotes accurate chromosome segregation during mitosis25847991. May act as a tumor suppressor25847991. May play a negative role in adipogenesis through the regulation of lipolytic and antilipogenic gene expression (By similarity)
Acts as a dominant negative inhibitor of isoform Alpha20484466,7769088,8621628. Has intrinsic transcriptional activity independent of isoform Alpha when both isoforms are coexpressed19248771,26711253. Loses this transcription modulator function on its own20484466. Has no hormone-binding activity8621628. May play a role in controlling glucose metabolism by maintaining insulin sensitivity (By similarity). Reduces hepatic gluconeogenesis through down-regulation of PEPCK in an isoform Alpha-dependent manner26711253. Directly regulates STAT1 expression in isoform Alpha-independent manner26711253
Has lower transcriptional activation activity than isoform Alpha. Exerts a dominant negative effect on isoform Alpha trans-repression mechanism20484466
Increases activity of isoform Alpha
More effective than isoform Alpha in transcriptional activation, but not repression activity
Has transcriptional activation activity
Has transcriptional activation activity
Has transcriptional activation activity
Has highest transcriptional activation activity of all isoforms created by alternative initiation15866175,23820903. Has transcriptional repression activity23303127. Mediates glucocorticoid-induced apoptosis23303127,23820903
Has transcriptional activation activity
Has transcriptional activation activity
Has lowest transcriptional activation activity of all isoforms created by alternative initiation15866175,23820903. Has transcriptional repression activity23303127

Quoted from UniProt’s FUNCTION annotation for P04150 (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
FKBP50.9990.3760.5000.998
HSP90AA10.9990.9940.5000.996
NCOA20.9980.9880.0000.892
HSP90AB10.9980.5480.5000.994
PTGES30.9970.9710.8000.591
NCOA10.9970.9890.0000.800
FKBP40.9960.6430.8000.954
NCOR10.9950.9780.5000.622
STIP10.9930.9730.5000.586
HSPA40.9920.6590.0000.979

Where it sits in the cell

  • Nucleoplasm
  • Cytosol
  • Mitochondriaadditional

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

UniProt, curated Cytoplasm · Nucleus · Mitochondrion · Cytoplasm, cytoskeleton, spindle · Cytoplasm, cytoskeleton, microtubule organizing center, centrosome · Chromosome · Nucleus, nucleoplasm

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.

  • Corticotrophs1,168.5 nCPM
  • Neutrophils1,012.2 nCPM
  • pDCs861.8 nCPM
  • Myonuclei691.5 nCPM

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 — 17.4 nTPM, from NR3C1cerebellum — 21.8 nTPM, from NR3C1hippocampal formation — 10.6 nTPM, from NR3C1amygdala — 10.4 nTPM, from NR3C1hypothalamus — 11.4 nTPM, from NR3C1thalamus — no resolved target expressed herebasal ganglia — 10.9 nTPM, from NR3C1medulla 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: pituitary gland 15.4, spinal cord 13.9, midbrain 11.4, retina 8.8.

Body

heart — 22.7 nTPM, from NR3C1smooth muscle — 22.2 nTPM, from NR3C1lung — 30.1 nTPM, from NR3C1liver — 37.2 nTPM, from NR3C1kidney — 17.9 nTPM, from NR3C1stomach — 15.1 nTPM, from NR3C1duodenum — 18.1 nTPM, from NR3C1small intestine — 17.0 nTPM, from NR3C1colon — 13.1 nTPM, from NR3C1adrenal gland — 11.1 nTPM, from NR3C1thyroid gland — 24.0 nTPM, from NR3C1pancreas — 13.9 nTPM, from NR3C1urinary bladder — 17.0 nTPM, from NR3C1skeletal muscle — 42.1 nTPM, from NR3C1spleen — 23.1 nTPM, from NR3C1salivary gland — 15.2 nTPM, from NR3C1
042 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 NR3C1 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

  • cerebellum21.8 nTPM
  • cerebral cortex17.4 nTPM
  • pituitary gland15.4 nTPM
  • spinal cord13.9 nTPM
  • hypothalamus11.4 nTPM
  • midbrain11.4 nTPM
  • basal ganglia10.9 nTPM
  • hippocampal formation10.6 nTPM
  • amygdala10.4 nTPM
  • retina8.8 nTPM

Peripheral and autonomic · 16

  • skeletal muscle42.1 nTPM
  • liver37.2 nTPM
  • lung30.1 nTPM
  • thyroid gland24.0 nTPM
  • spleen23.1 nTPM
  • heart muscle22.7 nTPM
  • smooth muscle22.2 nTPM
  • duodenum18.1 nTPM
  • kidney17.9 nTPM
  • small intestine17.0 nTPM
  • urinary bladder17.0 nTPM
  • salivary gland15.2 nTPM
  • stomach 115.1 nTPM
  • pancreas13.9 nTPM
  • colon13.1 nTPM
  • adrenal gland11.1 nTPM

Transcript is not protein. These are RNA levels for NR3C1, 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 7

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

TargetClassTypeValue (nM)pXOrganismAssay
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150

Functional readouts 23

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

TargetClassTypeValue (nM)pXOrganismAssay
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291848
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291848
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291848
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291849
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909150
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291850
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291849
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291849
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291849
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291849
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291848
Glucocorticoid receptorNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291848
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