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PsychedeliaDokholyan Laboratory
TargetEnzymes

Cytochrome P450 1A1

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

Measurements
5
Compounds
3
Binding constants
4
Median pX
6.30

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

CP1A1_HUMANCYP1A1Homo sapiens

Cytochrome P450 1A1

A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins10681376,11555828,12865317,14559847,15041462,15805301,18577768,19965576,20972997. 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)10681376,11555828,12865317,14559847,15041462,15805301,18577768,19965576,20972997. Catalyzes the hydroxylation of carbon-hydrogen bonds. Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C15-alpha and C16-alpha positions11555828,12865317,14559847,15805301. Displays different regioselectivities for polyunsaturated fatty acids (PUFA) hydroxylation15041462,18577768. Catalyzes the epoxidation of double bonds of certain PUFA15041462,19965576,20972997. Converts arachidonic acid toward epoxyeicosatrienoic acid (EET) regioisomers, 8,9-, 11,12-, and 14,15-EET, that function as lipid mediators in the vascular system20972997. Displays an absolute stereoselectivity in the epoxidation of eicosapentaenoic acid (EPA) producing the 17(R),18(S) enantiomer15041462. May play an important role in all-trans retinoic acid biosynthesis in extrahepatic tissues. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid10681376. May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent)21068195

Quoted from UniProt’s FUNCTION annotation for P04798 (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
GSTM10.9910.0450.9000.918
CYP3A40.9870.0760.9090.810
UGT1A60.9860.0000.9090.845
UGT1A70.9850.0000.9090.838
COMT0.9850.0000.9000.853
UGT1A40.9850.0000.9090.839
UGT1A100.9850.0000.9090.838
UGT1A10.9850.0000.9090.839
EPHX10.9850.0690.9000.852
UGT1A80.9850.0000.9090.838

Where it sits in the cell

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

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Epididymal clear cells51 nCPM
  • Urothelial cells41.7 nCPM
  • Hepatocytes13.6 nCPM
  • Vascular endothelial cells13.6 nCPM
  • Endometrial glandular cells10.3 nCPM
  • Endometrial secretory cells8.8 nCPM
  • Gastric progenitor cells6.4 nCPM
  • Salivary duct cells5.2 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.

  • liver61.8 nTPM
  • urinary bladder59.6 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 — 0.7 nTPM, from CYP1A1cerebellum — 0.1 nTPM, from CYP1A1hippocampal formation — 0.4 nTPM, from CYP1A1amygdala — 0.4 nTPM, from CYP1A1hypothalamus — 0.5 nTPM, from CYP1A1thalamus — no resolved target expressed herebasal ganglia — 0.3 nTPM, from CYP1A1medulla 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 0.6, midbrain 0.3, spinal cord 0.3, retina 0.2.

Body

heart — 10.8 nTPM, from CYP1A1smooth muscle — no resolved target expressed herelung — 9.9 nTPM, from CYP1A1liver — 61.8 nTPM, from CYP1A1kidney — 1.4 nTPM, from CYP1A1stomach — 1.6 nTPM, from CYP1A1duodenum — 0.6 nTPM, from CYP1A1small intestine — 18.6 nTPM, from CYP1A1colon — 2.1 nTPM, from CYP1A1adrenal gland — 0.6 nTPM, from CYP1A1thyroid gland — 2.0 nTPM, from CYP1A1pancreas — 0.6 nTPM, from CYP1A1urinary bladder — 59.6 nTPM, from CYP1A1skeletal muscle — 4.0 nTPM, from CYP1A1spleen — 0.1 nTPM, from CYP1A1salivary gland — 1.6 nTPM, from CYP1A1
062 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 CYP1A1 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

  • cerebral cortex0.7 nTPM
  • pituitary gland0.6 nTPM
  • hypothalamus0.5 nTPM
  • hippocampal formation0.4 nTPM
  • amygdala0.4 nTPM
  • basal ganglia0.3 nTPM
  • midbrain0.3 nTPM
  • spinal cord0.3 nTPM
  • retina0.2 nTPM
  • cerebellum0.1 nTPM

Peripheral and autonomic · 15

  • liver61.8 nTPM
  • urinary bladder59.6 nTPM
  • small intestine18.6 nTPM
  • heart muscle10.8 nTPM
  • lung9.9 nTPM
  • skeletal muscle4.0 nTPM
  • colon2.1 nTPM
  • thyroid gland2.0 nTPM
  • stomach 11.6 nTPM
  • salivary gland1.6 nTPM
  • kidney1.4 nTPM
  • duodenum0.6 nTPM
  • adrenal gland0.6 nTPM
  • pancreas0.6 nTPM
  • spleen0.1 nTPM

Transcript is not protein. These are RNA levels for CYP1A1, 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. 01Cannabidiol6.80
  2. 02Cannabidivarin5.80

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 1A1EnzymesKi1606.80Homo sapiensCHEMBL4687717
Cytochrome P450 1A1EnzymesKi1,6005.80Homo sapiensCHEMBL5096652
Cytochrome P450 1A1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4035356
Cytochrome P450 1A1EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4035356

Functional readouts 1

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 1A1EnzymesIC5060.007.22Homo sapiensCHEMBL5096651
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