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PsychedeliaDokholyan Laboratory
TargetEnzymes

Cytochrome P450 2D6

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

Measurements
114
Compounds
36
Binding constants
17
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

CP2D6_HUMANCYP2D6Homo sapiens

Cytochrome P450 2D6

A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids18698000,19965576,20972997,21289075,21576599. 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)18698000,19965576,20972997,21289075,21576599. Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA)19965576,20972997. Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling18698000,21289075. Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis21576599. Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid10681376. Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

Quoted from UniProt’s FUNCTION annotation for P10635 (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
UGT1A60.9840.0000.9070.833
UGT1A40.9810.0000.9070.795
UGT1A100.9790.0000.9070.776
UGT1A70.9790.0000.9070.776
UGT2B70.9790.0000.9070.776
UGT1A80.9790.0000.9070.776
UGT1A10.9790.0000.9070.776
UGT1A30.9730.0000.9070.706
UGT2B150.9700.0000.9070.676
UGT1A90.9690.0000.9070.673

Where it sits in the cell

  • Golgi apparatus

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

  • Enterocytes212.7 nCPM
  • Hepatocytes109.4 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.

  • liver386.2 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

cerebral cortex — 0.2 nTPM, from CYP2D6cerebellum — 0.5 nTPM, from CYP2D6hippocampal formation — 0.1 nTPM, from CYP2D6amygdala — 0.1 nTPM, from CYP2D6hypothalamus — 0.3 nTPM, from CYP2D6thalamus — no resolved target expressed herebasal ganglia — 0.4 nTPM, from CYP2D6medulla 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: pituitary gland 0.4, midbrain 0.1, spinal cord 0.1.

Body

heart — 0.1 nTPM, from CYP2D6smooth muscle — no resolved target expressed herelung — 0.1 nTPM, from CYP2D6liver — 386.2 nTPM, from CYP2D6kidney — 0.3 nTPM, from CYP2D6stomach — 0.1 nTPM, from CYP2D6duodenum — 3.5 nTPM, from CYP2D6small intestine — 15.2 nTPM, from CYP2D6colon — 0.5 nTPM, from CYP2D6adrenal gland — 0.2 nTPM, from CYP2D6thyroid gland — 0.4 nTPM, from CYP2D6pancreas — 0.8 nTPM, from CYP2D6urinary bladder — 0.1 nTPM, from CYP2D6skeletal muscle — no resolved target expressed herespleen — 0.3 nTPM, from CYP2D6salivary gland — 0.2 nTPM, from CYP2D6
0386 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 CYP2D6 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 · 9

  • cerebellum0.5 nTPM
  • basal ganglia0.4 nTPM
  • pituitary gland0.4 nTPM
  • hypothalamus0.3 nTPM
  • cerebral cortex0.2 nTPM
  • hippocampal formation0.1 nTPM
  • amygdala0.1 nTPM
  • midbrain0.1 nTPM
  • spinal cord0.1 nTPM

Peripheral and autonomic · 14

  • liver386.2 nTPM
  • small intestine15.2 nTPM
  • duodenum3.5 nTPM
  • pancreas0.8 nTPM
  • colon0.5 nTPM
  • thyroid gland0.4 nTPM
  • kidney0.3 nTPM
  • spleen0.3 nTPM
  • adrenal gland0.2 nTPM
  • salivary gland0.2 nTPM
  • heart muscle0.1 nTPM
  • lung0.1 nTPM
  • stomach 10.1 nTPM
  • urinary bladder0.1 nTPM

Transcript is not protein. These are RNA levels for CYP2D6, 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 17

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL729206
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743414
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4834799
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4834799
Cytochrome P450 2D6EnzymesKd— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624354
Cytochrome P450 2D6EnzymesKd— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624359
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687733
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096656
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743415
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL729206

Functional readouts 55

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 2D6EnzymesPotency25.107.60Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesIC5043.007.37Homo sapiensCHEMBL5117646
Cytochrome P450 2D6EnzymesIC5052.007.28Homo sapiensCHEMBL5332454
Cytochrome P450 2D6EnzymesIC502426.62Homo sapiensCHEMBL5609488
Cytochrome P450 2D6EnzymesPotency1,9955.70Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency2,5125.60Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency3,9815.40Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency3,9815.40Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency3,9815.40Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency10,0005.00Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency12,5894.90Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency25,1194.60Homo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL663531
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL860702
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5140379
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5356179
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909136
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096655
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL3888374
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5730217
Cytochrome P450 2D6EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1227846
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614110
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321
Cytochrome P450 2D6EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741321

Other measurements 42

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 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538992
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL3538991
Cytochrome P450 2D6EnzymesCL— no normalized value— value does not convert to pXHomo sapiensCHEMBL3539096
Cytochrome P450 2D6EnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4612560
Cytochrome P450 2D6EnzymesFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4479112
Cytochrome P450 2D6EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743272
Cytochrome P450 2D6EnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL3535053
Cytochrome P450 2D6EnzymesFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL4479111
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL883679
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL883679
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL883679
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873574
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873574
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873574
Cytochrome P450 2D6EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624329
Cytochrome P450 2D6EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624334
Cytochrome P450 2D6EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624339
Cytochrome P450 2D6EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624341
Cytochrome P450 2D6EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624346
Cytochrome P450 2D6EnzymesFC— no normalized value— value does not convert to pXHomo sapiensCHEMBL5624362
Cytochrome P450 2D6Enzymeskon— no normalized value— value does not convert to pXHomo sapiensCHEMBL5730217
Cytochrome P450 2D6Enzymesk_off— no normalized value— value does not convert to pXHomo sapiensCHEMBL5730217
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL883673
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL883673
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL883673
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872252
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872252
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872252
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872251
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872251
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL872251
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873573
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873573
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873573
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL873567
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL873567
Cytochrome P450 2D6EnzymesKm— no normalized value— value does not convert to pXHomo sapiensCHEMBL873567
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873575
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873575
Cytochrome P450 2D6EnzymesVmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL873575
Cytochrome P450 2D6EnzymesKinact— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743414
Cytochrome P450 2D6EnzymesKinact— no normalized value— value does not convert to pXHomo sapiensCHEMBL1743415
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