Skip to content
PsychedeliaDokholyan Laboratory
TargetEnzymes

Cytochrome P450 2B6

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

Measurements
6
Compounds
4
Binding constants
4
Median pX
5.59

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

CP2B6_HUMANCYP2B6Homo sapiens

Cytochrome P450 2B6

A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids12865317,21289075. 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). Catalyzes the epoxidation of double bonds of arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling21289075. Hydroxylates steroid hormones, including testosterone at C-16 and estrogens at C-212865317,21289075. Plays a role in the oxidative metabolism of xenobiotics, including plant lipids and drugs11695850,22909231. Acts as a 1,4-cineole 2-exo-monooxygenase11695850
Allele 2B6*9: Has low affinity for anandamide and can only produce 11,12 EpETrE-EAs

Quoted from UniProt’s FUNCTION annotation for P20813 (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
CYP3A50.9700.0760.9080.574
CYP3A70.9670.0760.9080.520
CYP4A110.9660.0710.9090.491
PPIG0.9640.0000.0000.964
CYP1A20.9630.0000.9110.504
AOX10.9630.0000.9110.597
CYP3A40.9600.0760.9080.411
ENSP000004805710.9600.0000.9000.534
CYP1A10.9590.0000.9110.497
SULT2A10.9550.0000.9000.541

Where it sits in the cell

  • Nuclear membrane
  • Nucleoplasmadditional
  • Cytosoladditional

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.

  • Hepatocytes1,059.9 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.

  • liver549.6 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 — 0.1 nTPM, from CYP2B6cerebellum — no resolved target expressed herehippocampal formation — no resolved target expressed hereamygdala — no resolved target expressed herehypothalamus — no resolved target expressed herethalamus — no resolved target expressed herebasal ganglia — no resolved target expressed heremedulla 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 0.6.

Body

heart — no resolved target expressed heresmooth muscle — 0.5 nTPM, from CYP2B6lung — 5.6 nTPM, from CYP2B6liver — 549.6 nTPM, from CYP2B6kidney — 14.4 nTPM, from CYP2B6stomach — 0.5 nTPM, from CYP2B6duodenum — 7.4 nTPM, from CYP2B6small intestine — 7.1 nTPM, from CYP2B6colon — 4.7 nTPM, from CYP2B6adrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — no resolved target expressed hereurinary bladder — no resolved target expressed hereskeletal muscle — 0.2 nTPM, from CYP2B6spleen — no resolved target expressed heresalivary gland — no resolved target expressed here
0550 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 CYP2B6 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 · 2

  • retina0.6 nTPM
  • cerebral cortex0.1 nTPM

Peripheral and autonomic · 9

  • liver549.6 nTPM
  • kidney14.4 nTPM
  • duodenum7.4 nTPM
  • small intestine7.1 nTPM
  • lung5.6 nTPM
  • colon4.7 nTPM
  • smooth muscle0.5 nTPM
  • stomach 10.5 nTPM
  • skeletal muscle0.2 nTPM

Transcript is not protein. These are RNA levels for CYP2B6, 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.

III · Ranking

Compounds by strongest binding constant

One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.

  1. 01Cannabidivarin5.89
  2. 02Cannabinol5.59

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 4

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 2B6EnzymesKi1,3005.89Homo sapiensCHEMBL5096654
Cytochrome P450 2B6EnzymesKi2,5505.59Homo sapiensCHEMBL5096670
Cytochrome P450 2B6EnzymesKi39,0004.41Homo sapiensCHEMBL5096669
Cytochrome P450 2B6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687729

Functional readouts 1

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 2B6EnzymesIC507,4005.13Homo sapiensCHEMBL5096653

Other measurements 1

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 2B6EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743267
← All targets