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PsychedeliaDokholyan Laboratory
TargetEnzymes

Cytochrome P450 2E1

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

Measurements
20
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

CP2E1_HUMANCYP2E1Homo sapiens

Cytochrome P450 2E1

A cytochrome P450 monooxygenase involved in the metabolism of fatty acids10553002,18577768. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase)10553002,18577768. Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates fatty acids specifically at the omega-1 position displaying the highest catalytic activity for saturated fatty acids10553002,18577768. May be involved in the oxidative metabolism of xenobiotics (Probable)

Quoted from UniProt’s FUNCTION annotation for P05181 (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
CYP3A40.9910.0760.9090.863
ADH1B0.9880.0000.9000.877
CYP1A20.9820.0000.9130.748
UGT1A60.9810.0000.9090.796
GSTP10.9790.0450.9000.784
GSTM10.9760.0450.9000.770
EPHX10.9710.0710.9000.699
UGT1A10.9700.0000.9090.673
UGT1A40.9700.0000.9090.680
UGT1A70.9690.0000.9090.669

Where it sits in the cell

  • Endoplasmic reticulum
  • Mitochondria

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

UniProt, curated Endoplasmic reticulum membrane · Microsome membrane · Mitochondrion inner membrane

Expression by cell type

Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Hepatocytes7,806.9 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.

  • liver9,697 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 — 8.6 nTPM, from CYP2E1cerebellum — 12.8 nTPM, from CYP2E1hippocampal formation — 5.0 nTPM, from CYP2E1amygdala — 3.9 nTPM, from CYP2E1hypothalamus — 4.9 nTPM, from CYP2E1thalamus — no resolved target expressed herebasal ganglia — 5.2 nTPM, from CYP2E1medulla 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 10.7, spinal cord 4.3, pituitary gland 3.9, midbrain 3.8.

Body

heart — 2.1 nTPM, from CYP2E1smooth muscle — 2.0 nTPM, from CYP2E1lung — 2.4 nTPM, from CYP2E1liver — 9697.0 nTPM, from CYP2E1kidney — 8.5 nTPM, from CYP2E1stomach — 6.4 nTPM, from CYP2E1duodenum — 1.3 nTPM, from CYP2E1small intestine — 2.0 nTPM, from CYP2E1colon — 4.8 nTPM, from CYP2E1adrenal gland — 2.8 nTPM, from CYP2E1thyroid gland — 3.8 nTPM, from CYP2E1pancreas — 11.8 nTPM, from CYP2E1urinary bladder — 3.4 nTPM, from CYP2E1skeletal muscle — 2.7 nTPM, from CYP2E1spleen — 6.4 nTPM, from CYP2E1salivary gland — 3.4 nTPM, from CYP2E1
09697 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 CYP2E1 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

  • cerebellum12.8 nTPM
  • retina10.7 nTPM
  • cerebral cortex8.6 nTPM
  • basal ganglia5.2 nTPM
  • hippocampal formation5.0 nTPM
  • hypothalamus4.9 nTPM
  • spinal cord4.3 nTPM
  • amygdala3.9 nTPM
  • pituitary gland3.9 nTPM
  • midbrain3.8 nTPM

Peripheral and autonomic · 16

  • liver9697.0 nTPM
  • pancreas11.8 nTPM
  • kidney8.5 nTPM
  • stomach 16.4 nTPM
  • spleen6.4 nTPM
  • colon4.8 nTPM
  • thyroid gland3.8 nTPM
  • urinary bladder3.4 nTPM
  • salivary gland3.4 nTPM
  • adrenal gland2.8 nTPM
  • skeletal muscle2.7 nTPM
  • lung2.4 nTPM
  • heart muscle2.1 nTPM
  • smooth muscle2.0 nTPM
  • small intestine2.0 nTPM
  • duodenum1.3 nTPM

Transcript is not protein. These are RNA levels for CYP2E1, 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
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137

Functional readouts 7

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137
Cytochrome P450 2E1EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909137

Other measurements 6

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
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538696
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538696
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538695
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538695
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538701
Cytochrome P450 2E1EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538697
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