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PsychedeliaDokholyan Laboratory
TargetEnzymes

Histone-lysine N-methyltransferase EHMT2

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
20
Compounds
17
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

EHMT2_HUMANEHMT2Homo sapiens

Histone-lysine N-methyltransferase EHMT2

Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones11316813,20084102. Also mediates monomethylation of 'Lys-56' of histone H3 (H3K56me1) in G1 phase, leading to promote interaction between histone H3 and PCNA and regulating DNA replication22387026. Also weakly methylates 'Lys-27' of histone H3 (H3K27me)11316813. Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently. Probably targeted to histone H3 by different DNA-binding proteins like E2F6, MGA, MAX and/or DP1. Also able to mono- and dimethylate histone H1-4 at 'Lys-26' (H1.4K26me1 and H1.4K26me2, respectively)19144645. In addition to the histone methyltransferase activity, also methylates non-histone proteins: mediates dimethylation of 'Lys-373' of p53/TP5320118233. Also methylates CDYL, WIZ, ACIN1, DNMT1, HDAC1, ERCC6, KLF12 and itself18438403

Quoted from UniProt’s FUNCTION annotation for Q96KQ7 (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
EHMT10.9990.8360.9000.979
CBX30.9990.9790.5000.965
HDAC10.9990.6620.5000.996
H3-3B0.9980.9300.5000.962
DNMT10.9980.6300.0000.995
H3C130.9980.9390.5000.945
H3C120.9980.9250.5000.962
UHRF10.9970.7220.0000.990
H3-40.9960.9390.0000.945
H3-50.9950.9170.0000.945

Where it sits in the cell

  • Nucleoplasm
  • Nuclear speckles

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

UniProt, curated Nucleus · Chromosome

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.

  • Oligodendrocytes36 nCPM
  • Astrocytes32.9 nCPM
  • Brain inhibitory neurons31.6 nCPM
  • Late spermatids31 nCPM
  • Oligodendrocyte progenitor cells30 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 — 26.1 nTPM, from EHMT2cerebellum — 24.2 nTPM, from EHMT2hippocampal formation — 16.8 nTPM, from EHMT2amygdala — 17.9 nTPM, from EHMT2hypothalamus — 16.7 nTPM, from EHMT2thalamus — no resolved target expressed herebasal ganglia — 27.4 nTPM, from EHMT2medulla 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: midbrain 14.2, spinal cord 12.1, pituitary gland 11.8, retina 0.4.

Body

heart — 5.4 nTPM, from EHMT2smooth muscle — 0.2 nTPM, from EHMT2lung — 6.8 nTPM, from EHMT2liver — 4.3 nTPM, from EHMT2kidney — 8.1 nTPM, from EHMT2stomach — 8.9 nTPM, from EHMT2duodenum — 0.5 nTPM, from EHMT2small intestine — 9.8 nTPM, from EHMT2colon — 11.9 nTPM, from EHMT2adrenal gland — 8.8 nTPM, from EHMT2thyroid gland — 9.7 nTPM, from EHMT2pancreas — 7.3 nTPM, from EHMT2urinary bladder — 13.5 nTPM, from EHMT2skeletal muscle — 5.2 nTPM, from EHMT2spleen — 10.7 nTPM, from EHMT2salivary gland — 8.9 nTPM, from EHMT2
027 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 EHMT2 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

  • basal ganglia27.4 nTPM
  • cerebral cortex26.1 nTPM
  • cerebellum24.2 nTPM
  • amygdala17.9 nTPM
  • hippocampal formation16.8 nTPM
  • hypothalamus16.7 nTPM
  • midbrain14.2 nTPM
  • spinal cord12.1 nTPM
  • pituitary gland11.8 nTPM
  • retina0.4 nTPM

Peripheral and autonomic · 16

  • urinary bladder13.5 nTPM
  • colon11.9 nTPM
  • spleen10.7 nTPM
  • small intestine9.8 nTPM
  • thyroid gland9.7 nTPM
  • stomach 18.9 nTPM
  • salivary gland8.9 nTPM
  • adrenal gland8.8 nTPM
  • kidney8.1 nTPM
  • pancreas7.3 nTPM
  • lung6.8 nTPM
  • heart muscle5.4 nTPM
  • skeletal muscle5.2 nTPM
  • liver4.3 nTPM
  • duodenum0.5 nTPM
  • smooth muscle0.2 nTPM

Transcript is not protein. These are RNA levels for EHMT2, 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 20

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

TargetClassTypeValue (nM)pXOrganismAssay
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
Histone-lysine N-methyltransferase EHMT2EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1738442
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