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PsychedeliaDokholyan Laboratory
TargetEnzymes

Cytochrome P450 1A2

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

Measurements
39
Compounds
25
Binding constants
9
Median pX
5.57

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

CP1A2_HUMANCYP1A2Homo sapiens

Cytochrome P450 1A2

A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins10681376,11555828,12865317,19965576,9435160. 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)10681376,11555828,12865317,19965576,9435160. Catalyzes the hydroxylation of carbon-hydrogen bonds11555828,12865317. Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E211555828,12865317. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis21576599. May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid10681376. Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer19965576. Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA9435160. May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent)21068195. Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin14725854. Metabolizes caffeine via N3-demethylation (Probable)

Quoted from UniProt’s FUNCTION annotation for P05177 (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
GAPDH0.9890.0730.0000.988
CYP2E10.9820.0000.9130.748
CYP7A10.9730.0000.9000.526
NAT20.9730.0000.9000.715
CYP4A110.9720.0580.9110.520
CYP2A60.9690.0000.9110.511
CYP3A40.9680.0760.9090.442
UGT1A80.9640.0000.6810.865
CYP2B60.9630.0000.9110.504
EPHX10.9610.0690.9000.611

Where it sits in the cell

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.

  • Hepatocytes756.3 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.

  • liver478.4 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 CYP1A2cerebellum — 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 0.4.

Body

heart — 0.1 nTPM, from CYP1A2smooth muscle — 0.1 nTPM, from CYP1A2lung — 0.4 nTPM, from CYP1A2liver — 478.4 nTPM, from CYP1A2kidney — 0.2 nTPM, from CYP1A2stomach — 0.2 nTPM, from CYP1A2duodenum — 0.1 nTPM, from CYP1A2small intestine — 0.2 nTPM, from CYP1A2colon — 0.1 nTPM, from CYP1A2adrenal gland — 0.3 nTPM, from CYP1A2thyroid gland — 2.0 nTPM, from CYP1A2pancreas — no resolved target expressed hereurinary bladder — 0.1 nTPM, from CYP1A2skeletal muscle — 0.3 nTPM, from CYP1A2spleen — 0.3 nTPM, from CYP1A2salivary gland — 0.3 nTPM, from CYP1A2
0478 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 CYP1A2 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

  • retina0.4 nTPM
  • cerebral cortex0.2 nTPM

Peripheral and autonomic · 15

  • liver478.4 nTPM
  • thyroid gland2.0 nTPM
  • lung0.4 nTPM
  • adrenal gland0.3 nTPM
  • skeletal muscle0.3 nTPM
  • spleen0.3 nTPM
  • salivary gland0.3 nTPM
  • kidney0.2 nTPM
  • stomach 10.2 nTPM
  • small intestine0.2 nTPM
  • heart muscle0.1 nTPM
  • smooth muscle0.1 nTPM
  • duodenum0.1 nTPM
  • colon0.1 nTPM
  • urinary bladder0.1 nTPM

Transcript is not protein. These are RNA levels for CYP1A2, 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. 01Cannabidiol5.57

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 9

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 1A2EnzymesKi2,6905.57Homo sapiensCHEMBL4687718
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4035357
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132

Functional readouts 30

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

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909132
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1227228
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
Cytochrome P450 1A2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1741322
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