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PsychedeliaDokholyan Laboratory
TargetNuclear receptors

Estrogen receptor beta

Steroid and other ligand-activated transcription factors.

Measurements
19
Compounds
9
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

ESR2_HUMANESR2Homo sapiens

Estrogen receptor beta

Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1/ER-alpha, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner20074560
Lacks ligand binding ability and has no or only very low ERE binding activity resulting in the loss of ligand-dependent transactivation ability

Quoted from UniProt’s FUNCTION annotation for Q92731 (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
NCOA10.9990.9840.8000.946
ESR10.9980.8300.9000.934
NCOA30.9970.8500.9000.816
SRC0.9950.6290.9000.889
NCOA20.9930.7790.8000.872
SP10.9880.5230.9000.786
MED10.9880.6910.9000.666
CAV10.9710.0490.5000.945
NCOR10.9700.1190.9000.693
JUN0.9670.0570.9000.686

Where it sits in the cell

  • Nucleoplasm
  • Vesiclesadditional

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

UniProt, curated Nucleus

Expression by cell type

Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Epicardial cells909.7 nCPM
  • Cardiomyocytes389.3 nCPM
  • Rod photoreceptor cells291 nCPM
  • Adrenal cortex cells212.8 nCPM
  • Myonuclei183.5 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 gland6.5 nTPM
  • ovary6.2 nTPM
  • testis5.6 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 — 0.2 nTPM, from ESR2cerebellum — 0.8 nTPM, from ESR2hippocampal formation — 0.2 nTPM, from ESR2amygdala — 0.2 nTPM, from ESR2hypothalamus — 0.5 nTPM, from ESR2thalamus — no resolved target expressed herebasal ganglia — 0.3 nTPM, from ESR2medulla 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 1.8, pituitary gland 1.0, midbrain 0.2, spinal cord 0.2.

Body

heart — 0.7 nTPM, from ESR2smooth muscle — 0.3 nTPM, from ESR2lung — 0.7 nTPM, from ESR2liver — 0.8 nTPM, from ESR2kidney — 1.3 nTPM, from ESR2stomach — 0.9 nTPM, from ESR2duodenum — 0.8 nTPM, from ESR2small intestine — 1.2 nTPM, from ESR2colon — 0.8 nTPM, from ESR2adrenal gland — 6.5 nTPM, from ESR2thyroid gland — 0.7 nTPM, from ESR2pancreas — 2.3 nTPM, from ESR2urinary bladder — 1.1 nTPM, from ESR2skeletal muscle — 1.5 nTPM, from ESR2spleen — 1.8 nTPM, from ESR2salivary gland — 0.9 nTPM, from ESR2
07 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 ESR2 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

  • retina1.8 nTPM
  • pituitary gland1.0 nTPM
  • cerebellum0.8 nTPM
  • hypothalamus0.5 nTPM
  • basal ganglia0.3 nTPM
  • cerebral cortex0.2 nTPM
  • hippocampal formation0.2 nTPM
  • amygdala0.2 nTPM
  • midbrain0.2 nTPM
  • spinal cord0.2 nTPM

Peripheral and autonomic · 16

  • adrenal gland6.5 nTPM
  • pancreas2.3 nTPM
  • spleen1.8 nTPM
  • skeletal muscle1.5 nTPM
  • kidney1.3 nTPM
  • small intestine1.2 nTPM
  • urinary bladder1.1 nTPM
  • stomach 10.9 nTPM
  • salivary gland0.9 nTPM
  • liver0.8 nTPM
  • duodenum0.8 nTPM
  • colon0.8 nTPM
  • heart muscle0.7 nTPM
  • lung0.7 nTPM
  • thyroid gland0.7 nTPM
  • smooth muscle0.3 nTPM

Transcript is not protein. These are RNA levels for ESR2, 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
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146

Functional readouts 12

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

TargetClassTypeValue (nM)pXOrganismAssay
Estrogen receptor betaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291793
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291793
Estrogen receptor betaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291793
Estrogen receptor betaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291793
Estrogen receptor betaNuclear receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291793
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
Estrogen receptor betaNuclear receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909146
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