CYP2J2

Summary

CYP2J2 (cytochrome P450 family 2 subfamily J member 2, HGNC:2634) is a protein-coding gene on chromosome 1p32.1, encoding Cytochrome P450 2J2 (P51589). A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) in the cardiovascular system.

This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and is thought to be the predominant enzyme responsible for epoxidation of endogenous arachidonic acid in cardiac tissue. Multiple transcript variants have been found for this gene.

Source: NCBI Gene 1573 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 76 total
• Druggable target: yes — 25 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000775

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2634
Approved symbol	CYP2J2
Name	cytochrome P450 family 2 subfamily J member 2
Location	1p32.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000134716
Ensembl biotype	protein_coding
OMIM	601258
Entrez	1573

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 5 protein_coding, 3 nonsense_mediated_decay, 1 retained_intron

ENST00000371204, ENST00000466095, ENST00000468257, ENST00000469406, ENST00000492633, ENST00000905907, ENST00000905908, ENST00000905909, ENST00000905910

RefSeq mRNA: 1 — MANE Select: NM_000775 NM_000775

CCDS: CCDS613

Canonical transcript exons

ENST00000371204 — 9 exons

Exon	Start	End
ENSE00001454618	59926537	59926773
ENSE00001912764	59893308	59893829
ENSE00003478386	59912162	59912311
ENSE00003480243	59907786	59907927
ENSE00003508550	59904871	59905058
ENSE00003518060	59911608	59911768
ENSE00003537643	59900965	59901103
ENSE00003561352	59909784	59909960
ENSE00003662569	59915938	59916100

Expression profiles

Bgee: expression breadth ubiquitous, 243 present calls, max score 97.82.

FANTOM5 (CAGE): breadth broad, TPM avg 4.6938 / max 275.5549, expressed in 655 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
12590	3.1765	385
12591	1.5173	485

Top tissues by expression

284 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
jejunal mucosa	UBERON:0000399	97.82	gold quality
apex of heart	UBERON:0002098	96.42	gold quality
heart left ventricle	UBERON:0002084	94.95	gold quality
cardiac ventricle	UBERON:0002082	94.87	gold quality
right atrium auricular region	UBERON:0006631	94.76	gold quality
right lobe of liver	UBERON:0001114	94.65	gold quality
cardiac atrium	UBERON:0002081	94.50	gold quality
liver	UBERON:0002107	94.17	gold quality
bronchial epithelial cell	CL:0002328	93.71	gold quality
heart right ventricle	UBERON:0002080	93.68	gold quality
left ventricle myocardium	UBERON:0006566	93.14	gold quality
epithelium of bronchus	UBERON:0002031	92.99	gold quality
myocardium	UBERON:0002349	92.90	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	92.48	gold quality
bronchus	UBERON:0002185	92.15	gold quality
duodenum	UBERON:0002114	91.99	gold quality
ileal mucosa	UBERON:0000331	91.31	gold quality
mucosa of transverse colon	UBERON:0004991	91.14	gold quality
mucosa of paranasal sinus	UBERON:0005030	91.13	gold quality
cardiac muscle of right atrium	UBERON:0003379	90.31	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	90.26	gold quality
rectum	UBERON:0001052	90.03	gold quality
heart	UBERON:0000948	89.99	gold quality
corpus callosum	UBERON:0002336	89.99	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	89.93	gold quality
colonic mucosa	UBERON:0000317	89.75	gold quality
nasal cavity epithelium	UBERON:0005384	89.72	gold quality
mucosa of sigmoid colon	UBERON:0004993	89.19	gold quality
jejunum	UBERON:0002115	88.94	gold quality
spinal cord	UBERON:0002240	88.93	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.01

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, FOS, JUN, NFE2L2, PPARG, SP1

miRNA regulators (miRDB)

24 targeting CYP2J2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-4496	99.88	68.89	2236
HSA-MIR-577	99.78	69.13	2479
HSA-MIR-548AG	99.77	69.25	1492
HSA-MIR-548M	99.70	68.87	1749
HSA-MIR-548AI	99.69	69.24	1494
HSA-MIR-548BA	99.69	69.14	1514
HSA-MIR-570-5P	99.69	69.24	1494
HSA-MIR-4261	99.59	70.30	3415
HSA-MIR-6740-3P	99.48	68.49	1392
HSA-MIR-6506-5P	99.04	65.66	1386
HSA-MIR-6814-5P	99.03	66.68	1273
HSA-MIR-452-3P	99.01	66.25	1241
HSA-MIR-4646-3P	98.65	66.98	693
HSA-MIR-299-5P	98.56	71.14	1140
HSA-MIR-9903	98.47	66.70	748
HSA-MIR-6780A-3P	98.42	67.49	1518
HSA-MIR-6881-3P	98.04	68.24	1777
HSA-MIR-4303	98.01	68.13	2304
HSA-MIR-3921	97.81	67.45	1431
HSA-MIR-1255B-2-3P	97.80	67.04	880
HSA-MIR-4653-5P	97.22	67.72	1429
HSA-MIR-4433B-5P	95.91	66.56	727
HSA-MIR-584-5P	95.82	68.05	848

Literature-anchored findings (GeneRIF, showing 40)

• expression levels of the immunoreactive protein with the CYP2J2 antibody in the small intestine were well correlated with the activities of the astemizole O-demethylation (PMID:12386130)
• role of activator protein-1 in the down-regulation of the human CYP2J2 gene in hypoxia (PMID:12737630)
• The CYP2J2*6 allele is rare in the Caucasian population, and no association is inferred between this allelic variant and type 1 or type 2 diabetic complications. (PMID:14575523)
• Transgenic mice overexpressing human CYP2J2 have improved postischemic recovery of left ventricular function. (PMID:15256482)
• Overexpressoin of CYP2J2 in transgenic mice increases l-type calcium channles in cardiomyocytes. (PMID:15361551)
• a functionally relevant polymorphism of the CYP2J2 gene is independently associated with an increased risk of coronary artery disease (PMID:15466638)
• characterization of novel CYP2J2 variants that cause loss of enzyme catalytic activity (PMID:15861034)
• there is an association between CYP2J2*7 (but not CYP2C8*3) genotype and hypertension in Caucasian males and Caucasians without a family history of hypertension (PMID:15864120)
• The c-Jun-responsive module between -122 and -50 in the CYP2J2 proximal promoter contains an atypical AP-1 element at -105/-95 that has a major role in c-Jun transactivation and acts in conjunction with the -56/-63 element to regulate expression. (PMID:16008525)
• No association was found between any of the variant alleles and hypertension. (PMID:16202848)
• comprehensive analysis of the distribution of sEH, CYP2C8, 2C9 and 2J2 in human neoplastic tissues using tissue micro-arrays (PMID:16957870)
• a CYP2J2*7 polymorphism may have a role in premature myocardial infarct (PMID:17126841)
• large inter-individual variation of the CYP2J2 suggests that this enzyme plays a significant role in the metabolism of xenobiotics (PMID:17162467)
• CYP2J2 gene is a susceptibility factor for essential hypertension, especially in females, and influences individual systolic blood pressure in the Chinese Han population (PMID:17286575)
• The G-50T polymorphism in CYP2J2 may be an important risk factor for the development of coronary heart disease events in African-Americans (PMID:17429317)
• These new selective inhibitors should be interesting tools to study the biological roles of CYP2J2. (PMID:17470359)
• Results indicate the CYP2J2 gene might be considered as a novel candidate gene for common susceptibility to asthma and highlight the importance of the P-450 epoxygenase pathway of metabolism of arachidonic acid in the pathogenesis of the disease. (PMID:17475630)
• CYP2J2 has a role in cancer metastasis (PMID:17638876)
• The structural features that have been found to be important for recognition of substrates or inhibitors by CYP2J2 were also interpreted on the basis of CYP2J2-substrate interactions in this model. (PMID:17705402)
• Genes encoding this enzyme modify cardiovascular disease risk at the population level in humans, providing support that modulation of this pathway may represent a novel approach to prevention. [REVIEW] (PMID:17979511)
• Flexible docking approaches were employed to dock 4 ligands into the active site of P450 2J2 to probe ligand-binding modes. Active site architecture and certain key residues responsible for substrate specificity were identified on the enzyme. (PMID:18004755)
• a CYP2J2*7 allele of the CYP2J2 gene is clearly associated with an increased risk of essential hypertension. (PMID:18219097)
• Two intronic CYP2J2 tag-single nucleotide polymorphisms, rs10889160 and rs11572325 were associated with an increased risk of myocardial infarction. No evidence of an association was found between variation in CYP2J2 and stroke. (PMID:18496133)
• These results suggest that expression of CYP2J2 was up-regulated when human monocytes differentiated into macrophages and that human monocytic cells and macrophages have a pathway to metabolize arachidonic acid using CYP epoxygenases. (PMID:18675280)
• Genotype distribution of CYP2J2*7 polymorphisms was investigated using polymerase chain reaction and restriction fragment length polymorphism assay in Japanese, Mongolian and Ovambo populations and the findings compared with other populations. (PMID:18729130)
• This study examined the association between calcineurin inhibitors-induced nephrotoxicity in liver transplant patients and CYP2C8 and CYP2J2 polymorphisms. (PMID:18769365)
• among patients with high cardiovascular risk profile, carriers of the G-50T-promoter polymorphism have significantly more myocardial infarctions (PMID:19105833)
• CYP epoxygenases efficiently promote the proliferation of tumor cells, which may be related with the activation of EGFR, ERK1/2 and PI3K/Akt signaling pathways. (PMID:19448409)
• Data show that CYP2J2 is highly and selectively expressed in human tumor tissues and cell lines and may be a novel biomarker of human tumors. (PMID:19550113)
• CYP2J2 activates the nuclear receptor PPARalpha in vitro and in vivo (PMID:19823578)
• data do not support a major role for the CYP2J2 -50G>T variant in determining blood pressure level and incident ischemic events (PMID:19851119)
• eight novel substrates for CP2J were identified that vary in size and overall topology; data suggest that CYP2J2 may be an unrecognized participant in first-pass metabolism, but its contribution is minor relative to that of CYP3A4 (PMID:19923256)
• Age of onset, family history, and obesity may modify typ3 2 diabetes polymorphism in younger onset typ32 diabetees. (PMID:20140850)
• The data indicate that epoxygenase 2J2 gene polymorphism is not a risk factor of acute coronary syndrome in Ukrainian population. (PMID:20480811)
• Haplotypes of CYP2J2 are associated with myocardial infarction in a Chinese Han population. (PMID:20597138)
• CYP2J2 overexpression in cultured human-derived malignant hematologic cell lines markedly accelerated proliferation and attenuated apoptosis (PMID:21030485)
• These data demonstrate that potentiation of the CYP epoxygenase pathway by either increased endothelial EET biosynthesis or globally decreased EET hydrolysis attenuates NF-kappaB-dependent vascular inflammatory responses in vivo. (PMID:21059750)
• This case-control study as well as meta-analysis suggested no association between CYP2J2 G-50T and EPHX2 R287Q and the risk of developing coronary artery disease (PMID:21642892)
• monocytes and macrophages express the epoxygenases CYP2J2 and CYP2C8 (PMID:22028915)
• No association has been found between the CYP2J2 (rs890293, -76G > T) or CYP2S1 (rs34971233, 13106C > T, P466L and rs338583, 13255A > G) gene polymorphisms and respiratory diseases. (PMID:22232929)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
mus_musculus	Cyp2j9	ENSMUSG00000015224
mus_musculus	Cyp2j13	ENSMUSG00000028571
rattus_norvegicus	Cyp2j9	ENSRNOG00000077186

Paralogs (15): CYP2W1 (ENSG00000073067), CYP2D6 (ENSG00000100197), CYP2C18 (ENSG00000108242), CYP2E1 (ENSG00000130649), CYP2C9 (ENSG00000138109), CYP2C8 (ENSG00000138115), CYP2U1 (ENSG00000155016), CYP2C19 (ENSG00000165841), CYP2S1 (ENSG00000167600), CYP2R1 (ENSG00000186104), CYP2B6 (ENSG00000197408), CYP2F1 (ENSG00000197446), CYP2A13 (ENSG00000197838), CYP2A7 (ENSG00000198077), CYP2A6 (ENSG00000255974)

Protein

Protein identifiers

Cytochrome P450 2J2 — P51589 (reviewed: P51589)

Alternative names: Albendazole monooxygenase (hydroxylating), Albendazole monooxygenase (sulfoxide-forming), Arachidonic acid epoxygenase, CYPIIJ2, Hydroperoxy icosatetraenoate isomerase

All UniProt accessions (4): A0A3B3IT99, A0A3B3ITF2, A0A3B3IU95, P51589

UniProt curated annotations — full annotation on UniProt →

Function. A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) in the cardiovascular system. 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 PUFA. Converts arachidonic acid to four regioisomeric epoxyeicosatrienoic acids (EpETrE), likely playing a major role in the epoxidation of endogenous cardiac arachidonic acid pools. In endothelial cells, participates in eicosanoids metabolism by converting hydroperoxide species into hydroxy epoxy metabolites. In combination with 15-lipoxygenase metabolizes arachidonic acid and converts hydroperoxyicosatetraenoates (HpETEs) into hydroxy epoxy eicosatrienoates (HEETs), which are precursors of vasodilatory trihydroxyicosatrienoic acids (THETAs). This hydroperoxide isomerase activity is NADPH- and O2-independent. Catalyzes the monooxygenation of a various xenobiotics, such as danazol, amiodarone, terfenadine, astemizole, thioridazine, tamoxifen, cyclosporin A and nabumetone. Catalyzes hydroxylation of the anthelmintics albendazole and fenbendazole. Catalyzes the sulfoxidation of fenbedazole.

Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.

Tissue specificity. Highly expressed in heart, present at lower levels in liver, kidney and skeletal muscle (at protein level).

Pathway. Lipid metabolism; arachidonate metabolism.

Similarity. Belongs to the cytochrome P450 family.

RefSeq proteins (1): NP_000766* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001128	Cyt_P450	Family
IPR002401	Cyt_P450_E_grp-I	Family
IPR008071	Cyt_P450_E_grp-I_CYP2J-like	Family
IPR017972	Cyt_P450_CS	Conserved_site
IPR036396	Cyt_P450_sf	Homologous_superfamily
IPR050182	Cytochrome_P450_fam2	Family

Pfam: PF00067

Enzyme classification (BRENDA):

• EC 1.14.14.24 — vitamin D 25-hydroxylase (BRENDA: 7 organisms, 34 substrates, 4 inhibitors, 22 Km, 14 kcat entries)
• EC 1.14.14.73 — albendazole monooxygenase (sulfoxide-forming) (BRENDA: 5 organisms, 12 substrates, 8 inhibitors, 0 Km, 0 kcat entries)
• EC 1.14.14.74 — albendazole monooxygenase (hydroxylating) (BRENDA: 1 organisms, 9 substrates, 6 inhibitors, 1 Km, 0 kcat entries)
• EC 1.14.14.75 — fenbendazole monooxygenase (4’-hydroxylating) (BRENDA: 1 organisms, 1 substrates, 0 inhibitors, 0 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
1ALPHA-HYDROXYVITAMIN D3	0.0006–0.0113	6
VITAMIN D3	0.0008–0.032	6
1ALPHA-HYDROXYVITAMIN D2	0.0042–0.018	4
BUFURALOL	0.001–0.0014	2
VITAMIN D2	0.0004–0.002	2
1ALPHA-HYDROXYCHOLECALCIFEROL	0.054	1
25-HYDROXY-VITAMIN D3	0.0071	1
2-AMINO-2-[2-[4-[4-(2-ETHYL-1,3-OXAZOL-4-YL)PHEN	0.0339	1

Catalyzed reactions (Rhea), 12 shown:

• (15S)-hydroperoxy-(5Z,8Z,11Z,13E)-eicosatetraenoate = (13R)-hydroxy-(14S,15S)-epoxy-(5Z,8Z,11Z)-eicosatrienoate (RHEA:37959)
• (5Z,8Z,11Z,14Z,17Z)-eicosapentaenoate + reduced [NADPH–hemoprotein reductase] + O2 = (17R,18S)-epoxy-(5Z,8Z,11Z,14Z)-eicosatetraenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:39779)
• (5Z,8Z,11Z,14Z,17Z)-eicosapentaenoate + reduced [NADPH–hemoprotein reductase] + O2 = (17S,18R)-epoxy-(5Z,8Z,11Z,14Z)-eicosatetraenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:39783)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (14S,15R)-epoxy-(5Z,8Z,11Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49856)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (14R,15S)-epoxy-(5Z,8Z,11Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49860)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (11S,12R)-epoxy-(5Z,8Z,14Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49876)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (11R,12S)-epoxy-(5Z,8Z,14Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49880)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (8R,9S)-epoxy-(5Z,11Z,14Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49884)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = (8S,9R)-epoxy-(5Z,11Z,14Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49928)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = 5,6-epoxy-(8Z,11Z,14Z)-eicosatrienoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:49936)
• (4Z,7Z,10Z,13Z,16Z,19Z)-docosahexaenoate + reduced [NADPH–hemoprotein reductase] + O2 = (19R,20S)-epoxy-(4Z,7Z,10Z,13Z,16Z)-docosapentaenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:52120)
• (4Z,7Z,10Z,13Z,16Z,19Z)-docosahexaenoate + reduced [NADPH–hemoprotein reductase] + O2 = (19S,20R)-epoxy-(4Z,7Z,10Z,13Z,16Z)-docosapentaenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:52124)

UniProt features (13 total): sequence variant 8, sequence conflict 3, chain 1, binding site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P51589-F1	93.90	0.85

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (1): 448 (axial binding residue)

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-211935	Fatty acids
R-HSA-211981	Xenobiotics
R-HSA-2142670	Synthesis of epoxy (EET) and dihydroxyeicosatrienoic acids (DHET)

MSigDB gene sets: 176 (showing top): MODULE_93, REACTOME_BIOLOGICAL_OXIDATIONS, BENPORATH_ES_WITH_H3K27ME3, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, GOBP_LONG_CHAIN_FATTY_ACID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, NEBEN_AML_WITH_FLT3_OR_NRAS_DN, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM4, HOSHIDA_LIVER_CANCER_SUBCLASS_S3, HSIAO_LIVER_SPECIFIC_GENES, CAIRO_HEPATOBLASTOMA_DN, GOTZMANN_EPITHELIAL_TO_MESENCHYMAL_TRANSITION_DN, GOBP_LIPID_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_METABOLIC_PROCESS

GO Biological Process (9): obsolete organic acid metabolic process (GO:0006082), fatty acid metabolic process (GO:0006631), icosanoid metabolic process (GO:0006690), xenobiotic metabolic process (GO:0006805), regulation of heart contraction (GO:0008016), epoxygenase P450 pathway (GO:0019373), linoleic acid metabolic process (GO:0043651), lipid metabolic process (GO:0006629), arachidonate metabolic process (GO:0019369)

GO Molecular Function (14): monooxygenase activity (GO:0004497), iron ion binding (GO:0005506), arachidonate epoxygenase activity (GO:0008392), arachidonate 14,15-epoxygenase activity (GO:0008404), arachidonate 11,12-epoxygenase activity (GO:0008405), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen (GO:0016712), isomerase activity (GO:0016853), heme binding (GO:0020037), linoleic acid epoxygenase activity (GO:0071614), hydroperoxy icosatetraenoate isomerase activity (GO:0106255), arachidonate 5,6-epoxygenase activity (GO:0106301), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen (GO:0016705), metal ion binding (GO:0046872)

GO Cellular Component (5): cytoplasm (GO:0005737), endoplasmic reticulum membrane (GO:0005789), extracellular exosome (GO:0070062), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	2
Arachidonate metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
arachidonate epoxygenase activity	3
long-chain fatty acid metabolic process	2
unsaturated fatty acid metabolic process	2
olefinic compound metabolic process	2
oxidoreductase activity	2
monooxygenase activity	2
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	2
catalytic activity	2
cellular anatomical structure	2
lipid metabolic process	1
monocarboxylic acid metabolic process	1
carboxylic acid metabolic process	1
metabolic process	1
cellular response to xenobiotic stimulus	1
heart contraction	1
regulation of blood circulation	1
arachidonate metabolic process	1
primary metabolic process	1
icosanoid metabolic process	1
transition metal ion binding	1
arachidonate monooxygenase activity	1
tetrapyrrole binding	1
intramolecular hydroxytransferase activity	1
cation binding	1
intracellular anatomical structure	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
extracellular vesicle	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1556 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CYP2J2	PPIG	Q13427	927
CYP2J2	TRPV4	Q9HBA0	791
CYP2J2	EPHX2	P34913	786
CYP2J2	CYP4F3	Q08477	587
CYP2J2	PPARG	P37231	583
CYP2J2	SLCO1A2	P46721	502
CYP2J2	POR	P16435	464
CYP2J2	ABCG2	Q9UNQ0	417
CYP2J2	ABCB1	P08183	414
CYP2J2	NR1I2	O75469	402
CYP2J2	CYP8B1	Q9UNU6	385
CYP2J2	UGT2B7	P16662	382
CYP2J2	SLC35A2	P78381	376
CYP2J2	PPARA	Q07869	370
CYP2J2	ALOX5	P09917	369

IntAct

12 interactions, top by confidence:

A	B	Type	Score
ELOC	CYP2J2	psi-mi:“MI:0915”(physical association)	0.370
ZBTB25	CYP2J2	psi-mi:“MI:0915”(physical association)	0.370
MINDY2	SLC27A2	psi-mi:“MI:0914”(association)	0.350
	ABCD4	psi-mi:“MI:0914”(association)	0.350
CYP2J2	NDUFS4	psi-mi:“MI:0914”(association)	0.350
CYP2J2	ECPAS	psi-mi:“MI:0914”(association)	0.350
SLC18A3	ORC4	psi-mi:“MI:0914”(association)	0.350
SLC2A14	ADCY3	psi-mi:“MI:0914”(association)	0.350
SLC39A7	ESYT2	psi-mi:“MI:0914”(association)	0.350
SLC52A3	TMEM120B	psi-mi:“MI:0914”(association)	0.350

BioGRID (37): CYP2J2 (Affinity Capture-MS), CYP2J2 (Affinity Capture-MS), CYP2J2 (Synthetic Lethality), CYP2J2 (Affinity Capture-MS), DYNC1LI2 (Affinity Capture-MS), NDUFB5 (Affinity Capture-MS), NDUFB8 (Affinity Capture-MS), NDUFB9 (Affinity Capture-MS), TBL1XR1 (Affinity Capture-MS), NELFE (Affinity Capture-MS), VPS28 (Affinity Capture-MS), TIPIN (Affinity Capture-MS), TTYH3 (Affinity Capture-MS), ND5 (Affinity Capture-MS), NDUFA7 (Affinity Capture-MS)

ESM2 similar proteins: A0A087X1C5, E9Q816, O18992, O46658, P00191, P03940, P08686, P10633, P10634, P10635, P11714, P12394, P12938, P12939, P15540, P24456, P24457, P30437, P51589, P51590, P52786, P70085, P78329, Q01361, Q0IIF9, Q29473, Q29488, Q2LA59, Q2LA60, Q2LCM1, Q2XNC8, Q2XNC9, Q4V8D1, Q64403, Q64562, Q64680, Q6GUQ4, Q6VVW9, Q6VVX0, Q7Z449

Diamond homologs: A0A087X1C5, E9Q5K4, F1Q8C3, O18809, O18992, O35293, O46658, O54749, O54750, O55071, O62671, O93297, P00176, P00178, P00179, P00180, P00181, P00182, P04167, P05178, P05179, P05180, P05181, P08682, P08683, P10610, P10632, P10633, P10634, P10635, P11371, P11712, P11714, P12789, P12790, P12791, P12938, P12939, P15123, P17666

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

76 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	63
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1421 predictions. Top by Δscore:

Variant	Effect	Δscore
1:59900989:C:A	donor_gain	1.0000
1:59904866:ATTAC:A	donor_loss	1.0000
1:59904867:TTA:T	donor_loss	1.0000
1:59904868:TACCT:T	donor_loss	1.0000
1:59904869:A:T	donor_loss	1.0000
1:59904870:C:CG	donor_loss	1.0000
1:59904914:T:TA	donor_gain	1.0000
1:59904915:C:A	donor_gain	1.0000
1:59907781:CTCA:C	donor_loss	1.0000
1:59907784:A:C	donor_loss	1.0000
1:59907785:C:A	donor_loss	1.0000
1:59907923:GTGTG:G	acceptor_gain	1.0000
1:59907924:TGTG:T	acceptor_gain	1.0000
1:59907925:GTG:G	acceptor_gain	1.0000
1:59907926:TG:T	acceptor_gain	1.0000
1:59907928:C:CC	acceptor_gain	1.0000
1:59909778:TCTCA:T	donor_loss	1.0000
1:59909779:CTCA:C	donor_loss	1.0000
1:59909780:TCACC:T	donor_loss	1.0000
1:59909781:CACCT:C	donor_loss	1.0000
1:59909783:C:CA	donor_loss	1.0000
1:59909940:CCA:C	acceptor_gain	1.0000
1:59909941:C:CT	acceptor_gain	1.0000
1:59909941:C:T	acceptor_gain	1.0000
1:59909942:A:C	acceptor_gain	1.0000
1:59909956:TAGAG:T	acceptor_gain	1.0000
1:59909957:AGAGC:A	acceptor_loss	1.0000
1:59909958:GAGCT:G	acceptor_loss	1.0000
1:59909959:AGCT:A	acceptor_loss	1.0000
1:59909960:GCTA:G	acceptor_loss	1.0000

AlphaMissense

3332 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:59900972:G:C	F441L	0.996
1:59900972:G:T	F441L	0.996
1:59900974:A:G	F441L	0.996
1:59912271:T:A	R138S	0.988
1:59912271:T:G	R138S	0.988
1:59901017:A:C	F426L	0.986
1:59901017:A:T	F426L	0.986
1:59901019:A:G	F426L	0.986
1:59915980:G:T	R111S	0.986
1:59900974:A:T	F441I	0.985
1:59893829:C:T	G444E	0.984
1:59904916:C:A	R382S	0.983
1:59904916:C:G	R382S	0.983
1:59904972:C:G	A364P	0.983
1:59904949:T:A	R371S	0.982
1:59904949:T:G	R371S	0.982
1:59907887:A:G	L301P	0.981
1:59901050:C:A	W415C	0.980
1:59901050:C:G	W415C	0.980
1:59912265:G:C	F140L	0.980
1:59912265:G:T	F140L	0.980
1:59912267:A:G	F140L	0.980
1:59893818:A:G	C448R	0.978
1:59893829:C:A	G444V	0.978
1:59901052:A:G	W415R	0.978
1:59901052:A:T	W415R	0.978
1:59909800:A:G	L282P	0.978
1:59912272:C:G	R138T	0.978
1:59893811:C:A	G450V	0.977
1:59893823:C:G	R446P	0.977

dbSNP variants (sampled 300 via entrez): RS1000041997 (1:59968654 C>T), RS1000067968 (1:59894763 T>C), RS1000248271 (1:59963637 TC>T), RS1000292785 (1:59943351 A>G), RS1000343727 (1:59907177 G>C), RS1000353962 (1:59899382 T>C), RS1000444230 (1:59949837 A>C,G), RS1000468891 (1:59905479 C>A), RS1000475850 (1:59925866 A>G), RS1000556872 (1:59941775 G>A), RS1000567188 (1:59911952 T>C,G), RS1000613072 (1:59901441 T>A), RS1000630261 (1:59942039 T>C), RS1000681399 (1:59906046 C>T), RS1000728377 (1:59958455 G>A)

Disease associations

OMIM: gene MIM:601258 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): pulmonary disease, chronic obstructive, susceptibility to (MONDO:0100167)

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST003542_146	Night sleep phenotypes	2.000000e-06
GCST004860_98	Alcoholic chronic pancreatitis	1.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3491 (SINGLE PROTEIN), CHEMBL4523986 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

25 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 762,254 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1008	BEPRIDIL	4	11,776
CHEMBL1017	TELMISARTAN	4	27,457
CHEMBL13	METOPROLOL	4	44,342
CHEMBL1428	NIMODIPINE	4	32,587
CHEMBL1451	TRIAMCINOLONE	4	81,668
CHEMBL1479	DANAZOL	4	16,256
CHEMBL1484	NICARDIPINE	4	30,866
CHEMBL161	CEFTRIAXONE	4	71,135
CHEMBL17157	TERFENADINE	4	25,393
CHEMBL193	NIFEDIPINE	4	74,353
CHEMBL388590	BENZBROMARONE	4	8,245
CHEMBL42	CLOZAPINE	4	37,581
CHEMBL45816	MIBEFRADIL	4	7,838
CHEMBL54	HALOPERIDOL	4	60,883
CHEMBL567	PERPHENAZINE	4	21,883
CHEMBL682	AMODIAQUINE	4	7,153
CHEMBL6966	VERAPAMIL	4	75,097
CHEMBL71	CHLORPROMAZINE	4	45,827
CHEMBL809	SERTRALINE	4	51,342
CHEMBL833	TICLOPIDINE	4	30,572
CHEMBL9	NORFLOXACIN	4
CHEMBL91	MICONAZOLE	4
CHEMBL477772	PAZOPANIB	4
CHEMBL74415	CANNABINOL	3
CHEMBL30008	FLUNARIZINE	2

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs890293	Toxicity	3	tacrolimus	Kidney Transplantation

PharmGKB variants

6 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs890293	CYP2J2	3	2.50	1	tacrolimus
rs2294950	CYP2J2, HOOK1		0.00	0
rs759510111	CYP2J2		0.00	0
rs201379188	CYP2J2		0.00	0
rs757528200	CYP2J2		0.00	0
rs199717190	CYP2J2		0.00	0

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — CYP2 family: drug metabolising subset

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
compound 4 [PMID: 16495056]	Inhibition	6.8	pIC50
terfenadine	Inhibition	5.09	pIC50

Binding affinities (BindingDB)

1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-chloro-N-formyl-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide	IC50	1400 nM	US-9359341: Aldehyde derivative of substitute oxazolidinones

ChEMBL bioactivities

68 potent at pChembl≥5 of 84 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.92	IC50	12	nM	DANAZOL
7.72	IC50	19	nM	DANAZOL
7.70	Ki	20	nM	DANAZOL
7.11	IC50	77	nM	DANAZOL
7.00	Ki	100	nM	FLUNARIZINE
7.00	Ki	100	nM	TELMISARTAN
6.89	Ki	130	nM	FLUNARIZINE
6.80	Ki	160	nM	CHEMBL208528
6.72	Ki	190	nM	TELMISARTAN
6.60	IC50	251.2	nM	CHEMBL601428
6.40	IC50	400	nM	CHEMBL207831
6.40	IC50	400	nM	CHEMBL208528
6.38	IC50	420	nM	TELMISARTAN
6.27	IC50	540	nM	TELMISARTAN
6.24	IC50	580	nM	MICONAZOLE
6.22	IC50	600	nM	CHEMBL207982
6.19	IC50	640	nM	MICONAZOLE
6.16	IC50	700	nM	CHEMBL207832
6.16	IC50	700	nM	CHEMBL207278
6.16	IC50	700	nM	TERFENADONE
6.16	IC50	700	nM	CHEMBL3330409
6.12	IC50	760	nM	FLUNARIZINE
6.05	IC50	900	nM	CHEMBL3330410
6.03	IC50	940	nM	FLUNARIZINE
6.02	IC50	950	nM	FLUNARIZINE
6.00	IC50	990	nM	AMODIAQUINE
5.96	IC50	1100	nM	CHEMBL2130955
5.95	IC50	1130	nM	TERFENADINE
5.89	IC50	1300	nM	CHEMBL207389
5.85	IC50	1400	nM	CHEMBL589135
5.77	IC50	1690	nM	NICARDIPINE
5.74	IC50	1830	nM	TERFENADINE
5.72	IC50	1900	nM	CHEMBL204362
5.72	IC50	1900	nM	CHEMBL2130955
5.70	IC50	2000	nM	CHEMBL560740
5.70	IC50	2000	nM	CHEMBL1082684
5.67	IC50	2140	nM	MIBEFRADIL
5.66	IC50	2200	nM	CHEMBL206576
5.60	IC50	2500	nM	CHEMBL378460
5.60	IC50	2500	nM	CHEMBL5612347
5.59	IC50	2560	nM	NORFLOXACIN
5.57	IC50	2700	nM	CHEMBL1085746
5.55	IC50	2800	nM	CHEMBL2130955
5.52	IC50	3000	nM	CHEMBL556716
5.51	IC50	3060	nM	NIFEDIPINE
5.47	IC50	3380	nM	NIMODIPINE
5.43	IC50	3700	nM	CHEMBL5406721
5.43	IC50	3700	nM	CHEMBL46909
5.42	IC50	3800	nM	CHEMBL5418617
5.41	IC50	3900	nM	CHEMBL5429178

PubChem BioAssay actives

71 with measured affinity, of 730 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
Danazol	1209989: Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation preincubated for 30 mins followed by substrate addition in presence of NADPH	ic50	0.0120	uM
8-imidazol-1-yl-5,6,7,8-tetrahydroquinoline	2022035: Inhibition of CYP450 (unknown origin)	ic50	0.0335	uM
Telmisartan	1210068: Non-competitive inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method and Dixon plot	ki	0.1000	uM
1-[bis(4-fluorophenyl)methyl]-4-[(E)-3-phenylprop-2-enyl]piperazine	1210068: Non-competitive inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method and Dixon plot	ki	0.1000	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-(4-propylphenyl)butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ki	0.1600	uM
N-(4-chlorophenyl)-5-ethyl-N-methyl-3-phenyl-1,2-oxazole-4-carboxamide	2108148: Inhibition of CYP450 (unknown origin)	ic50	0.2512	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-(4-prop-2-enylphenyl)butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	0.4000	uM
Miconazole	1209990: Inhibition of CYP2J2-mediated astemizole O-demethylation in human liver microsomes after 8 mins by LC-MS/MS analysis	ic50	0.5800	uM
1-(4-ethylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	0.6000	uM
2-(dimethylamino)-2-(2-ethylphenyl)-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]acetamide	2119433: Inhibition of CYP450 (unknown origin)	ic50	0.7000	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-(4-methylphenyl)butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	0.7000	uM
1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	0.7000	uM
1-(4-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	0.7000	uM
2-pyrrolidin-1-yl-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]-2-thiophen-3-ylacetamide	2119433: Inhibition of CYP450 (unknown origin)	ic50	0.9000	uM
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	0.9900	uM
2-[4-(trifluoromethyl)phenyl]chromen-4-one	1860369: Inhibition of CYP450 in human HCT-116 cells assessed as 20-HETE formation in presence of arachidonic acid incubated for 15 mins by multi-enzyme assay based LC-MS/MS analysis	ic50	1.1000	uM
1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol	1209990: Inhibition of CYP2J2-mediated astemizole O-demethylation in human liver microsomes after 8 mins by LC-MS/MS analysis	ic50	1.1300	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-[4-(2-hydroxyethyl)phenyl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	1.3000	uM
N-[(2,4-dichlorophenyl)methyl]-4-phenoxypiperidine-1-carboxamide	453482: Inhibition of CYP2J2	ic50	1.4000	uM
Nicardipine	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	1.6900	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-[4-(3-hydroxypropyl)phenyl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	1.9000	uM
N-[3,3-bis(4-fluorophenyl)propyl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide	431456: Inhibition of CYP2J2	ic50	2.0000	uM
4-pyrimidin-2-yloxy-N-[[2-(trifluoromethoxy)phenyl]methyl]piperidine-1-carboxamide	484179: Inhibition of CYP2J2	ic50	2.0000	uM
[(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] 2-methoxyacetate	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	2.1400	uM
1-[4-(2,2-difluoroethyl)phenyl]-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	2.2000	uM
4-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]-4-N-[[(7R)-5,6,7,8-tetrahydro-1,6-naphthyridin-7-yl]methyl]cyclohexane-1,4-diamine	2124397: Inhibition of CYP450 (unknown origin)	ic50	2.5000	uM
3-[4-[4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butanoyl]phenyl]propyl acetate	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	2.5000	uM
1-ethyl-6-fluoro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	2.5600	uM
N-[(2,4-dichlorophenyl)methyl]-4-pyridin-4-yloxypiperidine-1-carboxamide	484179: Inhibition of CYP2J2	ic50	2.7000	uM
4-cyano-N-[3-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)propyl]benzamide	431456: Inhibition of CYP2J2	ic50	3.0000	uM
Nifedipine	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	3.0600	uM
Nimodipine	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	3.3800	uM
1-[3-(2,4-dimethoxyphenyl)phenyl]-2,4-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.7000	uM
1-[(E)-2-(2,4-dimethoxyphenyl)ethenyl]-3,5-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.7000	uM
2,4-bis(3,5-dimethoxyphenyl)pyrimidine	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.8000	uM
2,5-bis(3,5-dimethoxyphenyl)thiophene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.9000	uM
1-(4-bromophenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	4.2000	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-1-benzofuran-3-yl)methanone	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	4.2600	uM
Haloperidol	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	4.6900	uM
Metoprolol	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	4.8700	uM
4-[2-(2,4-dimethoxyphenyl)-1,3-thiazol-4-yl]phenol	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	5.9000	uM
1-pyridin-4-yl-1a,2,3,7b-tetrahydro-1H-cyclopropa[a]naphthalen-4-ol	2022025: Inhibition of CYP450 in human liver microsomes	ic50	6.0534	uM
1-(1,3-benzodioxol-5-yl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	6.7000	uM
4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]-1-(4-methoxyphenyl)butan-1-one	264035: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells	ic50	7.6000	uM
(5R)-3-[1-(1H-indol-2-ylmethyl)piperidin-4-yl]-5-(6-methoxyquinolin-4-yl)-1,3-oxazolidin-2-one	306257: Inhibition of CYP450	ic50	7.9433	uM
Triamcinolone	1210069: Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	ic50	9.4700	uM
3-[1-[(3,4-dimethylphenyl)methyl]piperidin-4-yl]-5-(6-methoxyquinolin-4-yl)-1,3-oxazolidin-2-one	306257: Inhibition of CYP450	ic50	10.0000	uM
4-pyridin-4-yloxy-N-[[2-(trifluoromethoxy)phenyl]methyl]piperidine-1-carboxamide	484179: Inhibition of CYP2J2	ic50	10.0000	uM
3-pyridin-4-yl-N-[[2-(trifluoromethoxy)phenyl]methyl]pyrrolidine-1-carboxamide	484179: Inhibition of CYP2J2	ic50	10.0000	uM
1-[3-(3,5-dimethoxyphenyl)phenyl]-3,5-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	10.0000	uM

CTD chemical–gene interactions

93 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	4
ebastine	increases hydroxylation, decreases methylation, decreases reaction, decreases activity	4
Benzo(a)pyrene	decreases expression, increases expression	4
Astemizole	increases metabolic processing, decreases methylation, decreases reaction, affects metabolic processing	4
Tetrachlorodibenzodioxin	affects cotreatment, increases expression	3
Tobacco Smoke Pollution	decreases expression, affects expression	3
Terfenadine	increases hydroxylation, decreases activity	3
pirinixic acid	affects expression, affects binding, increases activity, increases expression	2
norclozapine	increases metabolic processing, increases chemical synthesis, decreases reaction, increases abundance	2
Aerosols	affects expression, decreases expression	2
Clozapine	decreases reaction, increases chemical synthesis, increases metabolic processing, increases abundance	2
Danazol	decreases activity	2
Tretinoin	decreases expression	2
Valproic Acid	increases expression	2
Cyclosporine	decreases expression	2
Arachidonic Acid	decreases methylation, decreases reaction, increases chemical synthesis, increases metabolic processing, increases abundance	2
Cadmium Chloride	decreases expression	2
salvianolic acid C	decreases activity	1
3,19-(2-bromobenzylidene)andrographolide	decreases response to substance, increases expression	1
synaptamide	increases metabolic processing	1
propionaldehyde	increases expression	1
bisphenol A	decreases methylation	1
cannabichromene	decreases reaction, increases metabolic processing	1
alpha-naphthoflavone	decreases activity	1
butyraldehyde	increases expression	1
perfluorooctanoic acid	increases expression	1
4-hydroxy-2-nonenal	increases chemical synthesis, increases oxidation, increases reduction	1
nilvadipine	decreases activity	1
delta-8-tetrahydrocannabinol	increases metabolic processing, decreases reaction	1
cannabigerol	decreases reaction, increases metabolic processing	1

ChEMBL screening assays

260 unique, capped per target: 255 admet, 5 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1058985	ADMET	Inhibition of CYP2J2	Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase. — J Med Chem
CHEMBL1119168	Binding	Inhibition of CYP2J2	Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method. — Bioorg Med Chem Lett

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_UH13	HEK293 CYP2J2*1-V5	Transformed cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.