Cytochrome P450 2C8
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 9
- Compounds
- 1
- Binding constants
- 2
- 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.
Cytochrome P450 2C8
A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins11093772,14559847,15766564,19965576,7574697. 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)11093772,14559847,15766564,19965576,7574697. Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond15766564,19965576,7574697. Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form11093772. Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1)14559847. Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol)26427316
Quoted from UniProt’s FUNCTION annotation for P10632 (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.
| Partner | Combined | Experiment | Database | Text mining |
|---|---|---|---|---|
| CYP3A4 | 0.973 | 0.076 | 0.906 | 0.544 |
| EPHX2 | 0.973 | 0.068 | 0.906 | 0.700 |
| CYP3A7 | 0.969 | 0.076 | 0.906 | 0.552 |
| CYP4A11 | 0.966 | 0.084 | 0.907 | 0.474 |
| ENSP00000480571 | 0.961 | 0.000 | 0.900 | 0.529 |
| PPIG | 0.957 | 0.000 | 0.000 | 0.956 |
| CYP3A5 | 0.956 | 0.076 | 0.906 | 0.378 |
| CYP1A1 | 0.955 | 0.000 | 0.908 | 0.467 |
| CYP4F2 | 0.951 | 0.086 | 0.905 | 0.305 |
| CYP2E1 | 0.951 | 0.000 | 0.908 | 0.363 |
Where it sits in the cell
- Vesicles
- Plasma membraneadditional
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
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.
- Hepatocytes2,460.9 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.
- liver2,014.2 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
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: retina 2.9, pituitary gland 2.5, midbrain 1.0, spinal cord 1.0.
Body
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 CYP2C8 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
- retina2.9 nTPM
- pituitary gland2.5 nTPM
- hypothalamus2.4 nTPM
- basal ganglia2.1 nTPM
- cerebral cortex1.7 nTPM
- hippocampal formation1.3 nTPM
- amygdala1.3 nTPM
- midbrain1.0 nTPM
- spinal cord1.0 nTPM
- cerebellum0.9 nTPM
Peripheral and autonomic · 15
- liver2014.2 nTPM
- stomach 15.5 nTPM
- adrenal gland1.7 nTPM
- pancreas1.6 nTPM
- kidney1.3 nTPM
- small intestine1.0 nTPM
- spleen0.9 nTPM
- thyroid gland0.8 nTPM
- lung0.4 nTPM
- colon0.4 nTPM
- heart muscle0.2 nTPM
- urinary bladder0.2 nTPM
- skeletal muscle0.2 nTPM
- salivary gland0.2 nTPM
- duodenum0.1 nTPM
Transcript is not protein. These are RNA levels for CYP2C8, 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 2
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Cytochrome P450 2C8 | Enzymes | Kd | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624358 |
| Cytochrome P450 2C8 | Enzymes | Kd | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624356 |
Other measurements 7
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Cytochrome P450 2C8 | Enzymes | Drug metabolism | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624337 |
| Cytochrome P450 2C8 | Enzymes | Ratio | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624343 |
| Cytochrome P450 2C8 | Enzymes | Drug metabolism | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624348 |
| Cytochrome P450 2C8 | Enzymes | Drug metabolism | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624351 |
| Cytochrome P450 2C8 | Enzymes | Drug metabolism | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624327 |
| Cytochrome P450 2C8 | Enzymes | FC | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624363 |
| Cytochrome P450 2C8 | Enzymes | Drug metabolism | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5624332 |