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PsychedeliaDokholyan Laboratory
TargetNuclear receptors

Nuclear receptor subfamily 1 group I member 2

Steroid and other ligand-activated transcription factors.

Measurements
18
Compounds
7
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

NR1I2_HUMANNR1I2Homo sapiens

Nuclear receptor subfamily 1 group I member 2

Nuclear receptor that acts as a transcription factor regulating genes involved in the metabolism and excretion of xenobiotics, drugs, and endogenous compounds. Activated by a broad range of endogenous steroids (e.g. pregnenolone, progesterone) and xenobiotics, including the antibiotic rifampicin and certain plant-derived metabolites. Upon ligand binding, translocates to the nucleus, forms a heterodimer with the retinoid X receptor/RXR, and binds to response elements in target promoters, leading to transcriptional activation. Target genes include cytochrome P450 enzymes such as CYP3A4 and ATP-binding cassette transporters including ABCB1/MDR1

Quoted from UniProt’s FUNCTION annotation for O75469 (reviewed).

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
RXRA0.9990.9700.0000.982
NCOA10.9980.9890.0000.883
CYP3A40.9620.0710.0000.955
NR0B20.9520.2940.0000.933
PPARGC1A0.8910.6830.0000.664
XPR10.8890.0000.0000.889
EPRS10.8820.0000.0000.882
NCOR20.8800.6520.5000.368
CYP3A70.8760.0710.0000.865
CYP2B60.8720.0560.0000.863

Where it sits in the cell

  • Nucleoplasm

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

UniProt, curated Nucleus · 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.

  • Enterocytes61.1 nCPM
  • Hepatocytes39.7 nCPM
  • Colonocytes26.8 nCPM
  • Enteric transient amplifying cells16.1 nCPM
  • Enteric stem cells13.6 nCPM
  • Paneth cells11.6 nCPM
  • Goblet cells9.4 nCPM
  • Gastric progenitor cells7.7 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.

  • liver44.3 nTPM
  • intestine29.4 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 — no resolved target expressed herehippocampal formation — no resolved target expressed hereamygdala — no resolved target expressed herehypothalamus — 0.3 nTPM, from NR1I2thalamus — no resolved target expressed herebasal ganglia — 0.1 nTPM, from NR1I2medulla 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 0.1.

Body

heart — no resolved target expressed heresmooth muscle — 0.5 nTPM, from NR1I2lung — no resolved target expressed hereliver — 44.3 nTPM, from NR1I2kidney — 0.1 nTPM, from NR1I2stomach — 1.6 nTPM, from NR1I2duodenum — 26.5 nTPM, from NR1I2small intestine — 29.4 nTPM, from NR1I2colon — 11.5 nTPM, from NR1I2adrenal gland — 0.1 nTPM, from NR1I2thyroid gland — no resolved target expressed herepancreas — 0.1 nTPM, from NR1I2urinary bladder — no resolved target expressed hereskeletal muscle — no resolved target expressed herespleen — 0.1 nTPM, from NR1I2salivary gland — no resolved target expressed here
044 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 NR1I2 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 · 3

  • hypothalamus0.3 nTPM
  • basal ganglia0.1 nTPM
  • retina0.1 nTPM

Peripheral and autonomic · 10

  • liver44.3 nTPM
  • small intestine29.4 nTPM
  • duodenum26.5 nTPM
  • colon11.5 nTPM
  • stomach 11.6 nTPM
  • smooth muscle0.5 nTPM
  • kidney0.1 nTPM
  • adrenal gland0.1 nTPM
  • pancreas0.1 nTPM
  • spleen0.1 nTPM

Transcript is not protein. These are RNA levels for NR1I2, 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 14

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

TargetClassTypeValue (nM)pXOrganismAssay
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEC5012,6004.90Homo sapiensCHEMBL3531878
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291845
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291845
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291845
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291845
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291844
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291844
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291844
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291844
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291844
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291846
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL3531531
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL3531532
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291845

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.

TargetClassTypeValue (nM)pXOrganismAssay
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL3531880
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL3531873
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsActivity— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3531877
Nuclear receptor subfamily 1 group I member 2Nuclear receptorsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL3531879
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