CYP3A7

Summary

CYP3A7 (cytochrome P450 family 3 subfamily A member 7, HGNC:2640) is a protein-coding gene on chromosome 7q22.1, encoding Cytochrome P450 3A7 (P24462). A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis.

This gene encodes a member of the cytochrome P450 superfamily of enzymes, which participate in drug metabolism and the synthesis of cholesterol, steroids and other lipids. This enzyme hydroxylates testosterone and dehydroepiandrosterone 3-sulphate, which is involved in the formation of estriol during pregnancy. This gene is part of a cluster of related genes on chromosome 7q21.1. Naturally-occurring readthrough transcription occurs between this gene and the downstream CYP3A51P pseudogene and is represented by GeneID:100861540.

Source: NCBI Gene 1551 — RefSeq curated summary.

At a glance

• GWAS associations: 20
• Clinical variants (ClinVar): 69 total
• Druggable target: yes — 10 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000765

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2640
Approved symbol	CYP3A7
Name	cytochrome P450 family 3 subfamily A member 7
Location	7q22.1
Locus type	gene with protein product
Status	Approved
Aliases	CP37, P450-HFLA
Ensembl gene	ENSG00000160870
Ensembl biotype	protein_coding
OMIM	605340
Entrez	1551

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 3 retained_intron, 1 protein_coding

ENST00000336374, ENST00000467776, ENST00000477357, ENST00000498080

RefSeq mRNA: 1 — MANE Select: NM_000765 NM_000765

CCDS: CCDS5673

Canonical transcript exons

ENST00000336374 — 13 exons

Exon	Start	End
ENSE00001815831	99705036	99705595
ENSE00003775466	99715758	99715906
ENSE00003775823	99731059	99731152
ENSE00003776025	99710732	99710892
ENSE00003777225	99709035	99709261
ENSE00003777543	99714555	99714682
ENSE00003777918	99717526	99717639
ENSE00003778047	99713469	99713535
ENSE00003779778	99717177	99717265
ENSE00003779919	99722296	99722348
ENSE00003781453	99707812	99707974
ENSE00003781796	99720313	99720412
ENSE00003841371	99735023	99735196

Expression profiles

Bgee: expression breadth ubiquitous, 166 present calls, max score 90.44.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.7745 / max 858.8707, expressed in 60 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
85115	0.7745	60

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
buccal mucosa cell	CL:0002336	90.44	gold quality
liver	UBERON:0002107	89.74	gold quality
right lobe of liver	UBERON:0001114	84.76	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.57	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	83.40	gold quality
nephron tubule	UBERON:0001231	79.82	gold quality
gall bladder	UBERON:0002110	79.19	gold quality
jejunal mucosa	UBERON:0000399	78.85	gold quality
adrenal tissue	UBERON:0018303	74.92	gold quality
kidney epithelium	UBERON:0004819	73.79	gold quality
jejunum	UBERON:0002115	72.17	gold quality
duodenum	UBERON:0002114	71.09	gold quality
metanephric glomerulus	UBERON:0004736	70.42	gold quality
epithelium of nasopharynx	UBERON:0001951	70.20	gold quality
renal glomerulus	UBERON:0000074	70.19	gold quality
mammary duct	UBERON:0001765	70.13	gold quality
cortex of kidney	UBERON:0001225	67.79	gold quality
corpus callosum	UBERON:0002336	67.28	gold quality
secondary oocyte	CL:0000655	66.82	gold quality
kidney	UBERON:0002113	66.23	gold quality
sperm	CL:0000019	66.10	gold quality
male germ cell	CL:0000015	64.91	gold quality
ventral tegmental area	UBERON:0002691	64.87	gold quality
subthalamic nucleus	UBERON:0001906	64.69	gold quality
inferior vagus X ganglion	UBERON:0005363	64.65	gold quality
metanephros	UBERON:0000081	64.55	gold quality
superficial temporal artery	UBERON:0001614	64.48	gold quality
nipple	UBERON:0002030	64.45	gold quality
endothelial cell	CL:0000115	64.27	gold quality
trigeminal ganglion	UBERON:0001675	64.05	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-GEOD-130473	yes	3618.09
E-ANND-3	no	2.58

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, FOXA2, FOXA3, NFAT5, NFIB, NFIC, NFIX, NFKB1, NFKB, NR1I2, NR3C1, PPARG, RELA, SP1, SP3, USF1, VDR

miRNA regulators (miRDB)

55 targeting CYP3A7, 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-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548J-5P	99.94	71.14	3489
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502
HSA-MIR-548B-5P	99.94	71.23	3502
HSA-MIR-548BB-5P	99.94	71.27	3509
HSA-MIR-548C-5P	99.94	71.24	3488
HSA-MIR-548D-5P	99.94	71.23	3502
HSA-MIR-548H-5P	99.94	71.24	3488
HSA-MIR-548I	99.94	71.25	3481
HSA-MIR-548O-5P	99.94	71.24	3488
HSA-MIR-548W	99.94	71.24	3488
HSA-MIR-548Y	99.94	71.28	3514
HSA-MIR-539-5P	99.93	70.30	2855
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-202-5P	99.78	67.65	991

Literature-anchored findings (GeneRIF, showing 40)

• presence of the ER6 motif of CYP3A4 mediates the high expression of CYP3A7 in subjects carrying CYP3A7*1C allele (PMID:11940601)
• Expression of CYP3A7 in the endometrium is significantly greater in the proliferative phase compared with the secretory phase of the menstrual cycle. (PMID:12485945)
• A novel mechanism, consisting of the splicing of the pseudogene CYP3AP1 to CYP3A7, causes the formation of the novel CYP3A7.1L (PMID:15937338)
• CYP3A7*1C polymorphism causes the persistence of enzymatic activity of CYP3A7 during adult life, resulting in lower circulating DHEAS and estrone levels. (PMID:15985487)
• analysis of CYP3A7 protein expression in adult human livers (PMID:16041241)
• the CYP3A7*1C polymorphism might have an influence on bone mass at the lumbar spine independently of serum DHEAS concentrations (PMID:17334880)
• Genetic polymorphisms in the CYP3A7 gene in the Han, She and Dong populations may contribute to interindividual differences in metabolic clearance of CYP3A7 substrates. (PMID:17559345)
• Differences in CYP3A41G genotype distribution and haplotypes of CYP3A4, CYP3A5 and CYP3A7 in 3 different Chinese ethnic groups; close linkage is demonstrated (PMID:17582393)
• CYP3A7 polymorphism might have an influence on bone mass at the lumbar spine independently of serum dehydroepiandrosterone sulphate concentrations. (PMID:17604264)
• Adult expression of CYP3A7 may modify the polycystic ovary syndrome phenotype by ameliorating adrenal androgen excess. (PMID:18445661)
• The genetic variations of CYP3A7 in a Korean population, were analyzed. (PMID:19585271)
• The single nucleotide polymorphism P450 oxidoreductase*28 seems to be a better genetic marker of the variability of total CYP3A activity in vivo than CYP3A4, CYP3A5 and CYP3A7 genetic variants. (PMID:19801957)
• The expression level of CYP3A7 messenger RNA is highest in chorion/decidua at a level which is about 3-fold of placenta and amnion, with the metabolic function to protect the fetus from exposure to drugs. (PMID:20118548)
• There were no statistically significant differences in the distribution of CYP3A7 polymorphic alleles between testicular cancer cases and controls suggesting no contribution to individual susceptibility to testicular cancer. (PMID:20345875)
• Recombinant CYP3A4, CYP3A5 and CYP3A7 metabolized R- and S-warfarin to 10- and 4’-hydroxywarfarin with efficiencies that depended on the individual enzymes. (PMID:20615193)
• Data show that both isoforms of CYP3A7 did not metabolize the anti-cancer drug sorafenib, and suggest that CYP3A7 activity does not influence the effectiveness of this anti-cancer drug against HCC. (PMID:20637317)
• Expression and regulation of human fetal-specific CYP3A7 in mice (PMID:22253426)
• Report distinctive response patterns of HIF-1alpha, CYP3A4 and CYP3A7 to cobalt chloride in human fetal liver cells. (PMID:22277676)
• Report CYP3A7 metabolism of inhaled glucocorticoids. (PMID:23143891)
• Only CYP1A1, CYP1B1, CYP3A4, CYP3A5 and CYP3A7 expressed in lymphocytes and monocytes. (PMID:24168324)
• Differences in the expression of nuclear receptors might determine the variability in CYP3A4 and CYP3A7 expression observed in foetal liver. (PMID:25689036)
• CYP3A4, CYP3A7, UGT2B11 and UGT2B15 genes are significantly downregulated in melanosis coli. (PMID:26238215)
• Methylation status of cytosine in the CYP3A7 proximal promoter correlated with changes in developmental expression of mRNA. (PMID:26772622)
• Occupancy by modified histones was consistent with chromatin structural changes contributing to the mechanisms regulating CYP3A7 ontogeny. (PMID:26921389)
• CYP3A7*1C influences outcome are required. (PMID:26964624)
• These results suggest the existence of a marked inter-individual variability regarding the presence of the isoforms of CYP3A. In addition, since sorafenib is metabolized by CYP3A4, but not by CYP3A7, an overexpression of CYP3A4 may lead to an increase in the degradation of the drug and then to clinical ineffectiveness. (PMID:27349315)
• data suggested that hepatocyte nuclear factor 4 alpha and glucocorticoid receptor, and epigenetic changes of H3K4me2 and H3K27me3 are associated with the ontogenic expressions of CYP3A4/3A7 in the livers of the Chinese Han population. (PMID:27727071)
• The CYP3A7*1C allele is associated with a lower urinary estrone levels, a more pronounced reduction in 2-hydroxylation pathway estrone metabolites (EMs) and a lower ratio of 2-hydroxylation:16alpha-hydroxylation EMs in premenopausal women. (PMID:28072767)
• polymorphisms may modify the response to dietary methylmercury exposure during early life development (PMID:28500872)
• All three neonicotinoid pesticides induced the expression of CYP3A7 in H295R cells; induction was reversed by co-treatment of H295R cells with exogenous estriol. CYP3A7 is normally expressed in fetal liver and is a key enzyme involved in estriol synthesis. (PMID:28750898)
• our data indicate an alternative binding mode for testosterone in CYP3A7 that favors the 2alpha-hydroxylation, suggesting significant structural differences in its active site compared with CYP3A4/5 (PMID:28986474)
• CYP3A7 rs2257401 is associated with tacrolimus pharmacokinetics in kidney transplantation. (PMID:30584253)
• Scaling in vitro activity of CYP3A7 suggests human fetal livers do not clear retinoic acid entering from maternal circulation. (PMID:30874620)
• CYP3A7 showed abnormally elevated activities at 500 and 750 muM. (PMID:30918015)
• role of CYP3A7 in development, disease, and xenobiotic metaboolism (PMID:31445893)
• kcat values, rather than Km values, for 6beta-hydroxylation of three steroid hormones by CYP3A7 are different from those of CYP3A4 and CYP3A5 (PMID:32001245)
• CYP3A Polymorphism and Chronic Mercury Intoxication. (PMID:32146629)
• Urinary Bile Acid Profile of Newborns Born by Cesarean Section Is Characterized by Oxidative Metabolism of Primary Bile Acids: Limited Roles of Fetal-Specific CYP3A7 in Cholate Oxidations. (PMID:32499339)
• Human Fetal Liver Metabolism of Oxycodone Is Mediated by CYP3A7. (PMID:33438174)
• CYP3A7*1C allele: linking premenopausal oestrone and progesterone levels with risk of hormone receptor-positive breast cancers. (PMID:33495599)

Cross-species orthologs

20 orthologs

Organism	Symbol	Gene ID
danio_rerio	cyp3c1	ENSDARG00000015575
danio_rerio	cyp3c3	ENSDARG00000037873
danio_rerio	cyp3c2	ENSDARG00000037874
danio_rerio	cyp3c4	ENSDARG00000070021
danio_rerio	cyp3a65	ENSDARG00000103295
mus_musculus	Cyp3a25	ENSMUSG00000029630
mus_musculus	Cyp3a13	ENSMUSG00000029727
mus_musculus	Cyp3a16	ENSMUSG00000038656
mus_musculus	Cyp3a44	ENSMUSG00000054417
mus_musculus	Cyp3a11	ENSMUSG00000056035
mus_musculus	Cyp3a59	ENSMUSG00000061292
mus_musculus	Cyp3a57	ENSMUSG00000070419
mus_musculus	Cyp3a41a	ENSMUSG00000075551
mus_musculus	Cyp3a41b	ENSMUSG00000075552
rattus_norvegicus	Cyp3a18	ENSRNOG00000000969
rattus_norvegicus	Cyp3a73	ENSRNOG00000000978
rattus_norvegicus	Cyp3a62	ENSRNOG00000001379
rattus_norvegicus	Cyp3a23-3a1	ENSRNOG00000032560
rattus_norvegicus	Cyp3a9	ENSRNOG00000046643
rattus_norvegicus	Cyp3a23-3a1	ENSRNOG00000067532

Paralogs (3): CYP3A43 (ENSG00000021461), CYP3A5 (ENSG00000106258), CYP3A4 (ENSG00000160868)

Protein

Protein identifiers

Cytochrome P450 3A7 — P24462 (reviewed: P24462)

Alternative names: CYPIIIA7, Cytochrome P450-HFLA, P450HLp2

All UniProt accessions (1): P24462

UniProt curated annotations — full annotation on UniProt →

Function. A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis. 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 hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones. Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position. Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development. Also involved in the oxidative metabolism of xenobiotics including anticonvulsants.

Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.

Tissue specificity. Expressed in fetal liver (at protein level).

Pathway. Steroid hormone biosynthesis. Cofactor metabolism; retinol metabolism.

Similarity. Belongs to the cytochrome P450 family.

Isoforms (2)

UniProt ID	Names	Canonical?
P24462-1	1	yes
P24462-2	2

RefSeq proteins (1): NP_000756* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001128	Cyt_P450	Family
IPR002402	Cyt_P450_E_grp-II	Family
IPR008072	Cyt_P450_E_CYP3A	Family
IPR017972	Cyt_P450_CS	Conserved_site
IPR036396	Cyt_P450_sf	Homologous_superfamily
IPR050705	Cytochrome_P450_3A	Family

Pfam: PF00067

Enzyme classification (BRENDA):

• EC 1.14.14.1 — unspecific monooxygenase (BRENDA: 53 organisms, 363 substrates, 53 inhibitors, 69 Km, 40 kcat entries)

Substrate kinetics (BRENDA)

24 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
FENTHION	0.0016–0.131	18
NADH	0.004–1.43	13
NADPH	0.002–0.13	6
(1R)-CIS-PERMETHRIN	0.055–0.061	2
(1R)-TRANS-PERMETHRIN	0.115–0.131	2
(1S)-CIS-PERMETHRIN	0.057–0.063	2
(1S)-TRANS-PERMETHRIN	0.101–0.106	2
7-ETHOXYRESORUFIN	0.0001–0.0012	2
MYRISTIC ACID	0.023–0.11	2
OLEIC ACID	0.075–0.084	2
OMEGA-(P-NITROPHENYL)DECANOIC ACID	0.0064–0.0245	2
OMEGA-(P-NITROPHENYL)DODECANOIC ACID	0.0065–0.0104	2
OMEGA-(P-NITROPHENYL)OCTANOIC ACID	0.0319–0.0618	2
12-METHYL-TETRADECANOIC ACID	0.0129	1
13-METHYL-TETRADECANOIC ACID	0.0165	1

Catalyzed reactions (Rhea), 11 shown:

• an organic molecule + reduced [NADPH–hemoprotein reductase] + O2 = an alcohol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:17149)
• testosterone + reduced [NADPH–hemoprotein reductase] + O2 = 6beta,17beta-dihydroxyandrost-4-en-3-one + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:46296)
• estrone + reduced [NADPH–hemoprotein reductase] + O2 = 16alpha-hydroxyestrone + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47204)
• estrone + reduced [NADPH–hemoprotein reductase] + O2 = 2-hydroxyestrone + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47208)
• 17beta-estradiol + reduced [NADPH–hemoprotein reductase] + O2 = 2-hydroxy-17beta-estradiol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47212)
• 17beta-estradiol + reduced [NADPH–hemoprotein reductase] + O2 = 6beta-hydroxyestradiol-17beta + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47216)
• 3beta-hydroxyandrost-5-en-17-one + reduced [NADPH–hemoprotein reductase] + O2 = 3beta,16alpha-dihydroxy-androst-5-en-17-one + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47220)
• dehydroepiandrosterone 3-sulfate + reduced [NADPH–hemoprotein reductase] + O2 = 16alpha-hydroxydehydroepiandrosterone 3-sulfate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47224)
• estrone + reduced [NADPH–hemoprotein reductase] + O2 = 4-hydroxyestrone + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47292)
• all-trans-retinoate + reduced [NADPH–hemoprotein reductase] + O2 = all-trans-4-hydroxyretinoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:51984)
• all-trans-retinoate + reduced [NADPH–hemoprotein reductase] + O2 = all-trans-18-hydroxyretinoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:55856)

UniProt features (53 total): helix 25, strand 11, mutagenesis site 6, turn 6, sequence variant 2, chain 1, binding site 1, splice variant 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
7MK8	X-RAY DIFFRACTION	2.15
8GK3	X-RAY DIFFRACTION	2.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P24462-F1	92.44	0.81

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): 442 (axial binding residue)

Mutagenesis-validated functional residues (6):

Position	Phenotype
262	has no effect on catalytic activity.
116	has no effect on catalytic activity.
174	increases catalytic activity.
214	increases catalytic activity.
224	reduces affinity for substrate and catalytic efficiency.
244	reduces affinity for substrate and catalytic efficiency.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-211981	Xenobiotics

MSigDB gene sets: 149 (showing top): GOBP_LIPID_MODIFICATION, MODULE_93, REACTOME_BIOLOGICAL_OXIDATIONS, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, GOBP_OXIDATIVE_DEMETHYLATION, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_RETINOL_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_DEMETHYLATION, HOSHIDA_LIVER_CANCER_SUBCLASS_S3, ACEVEDO_LIVER_TUMOR_VS_NORMAL_ADJACENT_TISSUE_DN, HSIAO_LIVER_SPECIFIC_GENES, GOBP_STEROID_BIOSYNTHETIC_PROCESS, GOBP_RETINOIC_ACID_METABOLIC_PROCESS, GOBP_LIPID_METABOLIC_PROCESS

GO Biological Process (9): lipid hydroxylation (GO:0002933), steroid biosynthetic process (GO:0006694), xenobiotic metabolic process (GO:0006805), steroid metabolic process (GO:0008202), estrogen metabolic process (GO:0008210), retinol metabolic process (GO:0042572), retinoic acid metabolic process (GO:0042573), oxidative demethylation (GO:0070989), lipid metabolic process (GO:0006629)

GO Molecular Function (14): monooxygenase activity (GO:0004497), iron ion binding (GO:0005506), steroid hydroxylase activity (GO:0008395), retinoic acid 4-hydroxylase activity (GO:0008401), oxygen binding (GO:0019825), heme binding (GO:0020037), testosterone 6-beta-hydroxylase activity (GO:0050649), all-trans retinoic acid 18-hydroxylase activity (GO:0062183), estrogen 16-alpha-hydroxylase activity (GO:0101020), estrogen 2-hydroxylase activity (GO:0101021), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen (GO:0016705), 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), metal ion binding (GO:0046872)

GO Cellular Component (3): endoplasmic reticulum membrane (GO:0005789), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
monooxygenase activity	4
hormone metabolic process	3
steroid hydroxylase activity	3
steroid metabolic process	2
retinoid metabolic process	2
oxidoreductase activity	2
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	2
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	2
lipid modification	1
lipid biosynthetic process	1
metabolic process	1
cellular response to xenobiotic stimulus	1
lipid metabolic process	1
primary alcohol metabolic process	1
olefinic compound metabolic process	1
monocarboxylic acid metabolic process	1
demethylation	1
primary metabolic process	1
transition metal ion binding	1
small molecule binding	1
tetrapyrrole binding	1
catalytic activity	1
cation binding	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1616 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CYP3A7	NR1I2	O75469	865
CYP3A7	PPIG	Q13427	771
CYP3A7	NR1I3	Q14994	770
CYP3A7	NDC80	O14777	763
CYP3A7	UGT1A6	P19224	580
CYP3A7	UGT1A4	P22310	579
CYP3A7	CYP2C9	P11712	558
CYP3A7	CYP2C8	P10632	553
CYP3A7	UGT1A10	Q9HAW8	551
CYP3A7	CYP2C19	P33259	550
CYP3A7	CYP2C18	P33260	533
CYP3A7	UGT1A8	Q9HAW9	529
CYP3A7	UGT1A7	Q9HAW7	524
CYP3A7	PGR	P06401	521
CYP3A7	CYP2B6	P20813	520

IntAct

5 interactions, top by confidence:

A	B	Type	Score
CYP3A5	IGHG1	psi-mi:“MI:0914”(association)	0.530
CYP3A7	VAPB	psi-mi:“MI:0914”(association)	0.350
CYP3A7	ODR4	psi-mi:“MI:0914”(association)	0.350

BioGRID (6): CYP3A7 (Affinity Capture-MS), VAPB (Affinity Capture-MS), CYP3A7 (Affinity Capture-MS), CYSTM1 (Affinity Capture-MS), C1orf27 (Affinity Capture-MS), PDZD8 (Affinity Capture-MS)

ESM2 similar proteins: A2A974, F1Q8C3, H1A988, O18993, O35728, O88833, P00186, P04799, P08516, P08684, P13584, P14579, P14581, P15128, P15129, P20815, P20816, P20817, P24453, P24462, P24463, P24464, P33268, P33274, P51869, P51871, P78329, P79102, P79401, P98187, Q00557, Q08477, Q29496, Q3MID2, Q64391, Q64462, Q64464, Q6A152, Q6NT55, Q86W10

Diamond homologs: A0A0C2W6G6, A0A1L9WQK2, A0A1V0QSE7, A0A2H3CSA7, A0A2H3CZX2, A0A3G9HRC2, A0A3S5HYN5, A0A8K1AW54, A2A974, A2RRT9, A8NCK6, B0XZV0, B8QHP5, F1SY62, F1SY74, F1SYB6, F1SYH7, F2K081, F2ZAF9, I1RE80, I1S2J5, I3PLR1, L7X3S1, O08336, O17624, O18993, O43174, O44221, O48786, O49396, O55127, O70537, O88833, P05183, P08684, P0DKI7, P0DOX0, P11372, P11707, P13584

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	58
Likely benign	8
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1933 predictions. Top by Δscore:

Variant	Effect	Δscore
7:99705514:CGGT:C	donor_gain	1.0000
7:99709029:TCCTA:T	donor_loss	1.0000
7:99709030:CCTA:C	donor_loss	1.0000
7:99709031:CTAC:C	donor_loss	1.0000
7:99709032:TAC:T	donor_loss	1.0000
7:99709032:TACCT:T	donor_loss	1.0000
7:99709033:A:C	donor_loss	1.0000
7:99709033:A:T	donor_loss	1.0000
7:99709034:C:CT	donor_loss	1.0000
7:99709257:GGTGC:G	acceptor_gain	1.0000
7:99709258:GTGC:G	acceptor_gain	1.0000
7:99709259:TGC:T	acceptor_gain	1.0000
7:99709260:GC:G	acceptor_gain	1.0000
7:99709261:CC:C	acceptor_gain	1.0000
7:99709262:C:CA	acceptor_loss	1.0000
7:99709262:C:CC	acceptor_gain	1.0000
7:99709263:T:C	acceptor_loss	1.0000
7:99710728:TCA:T	donor_loss	1.0000
7:99710729:CAC:C	donor_loss	1.0000
7:99710730:A:AT	donor_loss	1.0000
7:99710730:ACCTT:A	donor_loss	1.0000
7:99710731:CCTT:C	donor_gain	1.0000
7:99710843:A:T	acceptor_gain	1.0000
7:99710888:CAGAG:C	acceptor_gain	1.0000
7:99710889:AGAG:A	acceptor_gain	1.0000
7:99710890:GAG:G	acceptor_gain	1.0000
7:99710890:GAGCT:G	acceptor_loss	1.0000
7:99710891:AG:A	acceptor_gain	1.0000
7:99710892:GC:G	acceptor_loss	1.0000
7:99710893:C:A	acceptor_loss	1.0000

AlphaMissense

3319 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:99717582:A:G	W126R	0.998
7:99717582:A:T	W126R	0.998
7:99707923:A:C	F435L	0.997
7:99707923:A:T	F435L	0.997
7:99707925:A:G	F435L	0.997
7:99707908:T:A	R440S	0.996
7:99707908:T:G	R440S	0.996
7:99717569:C:G	R130P	0.996
7:99717580:C:A	W126C	0.996
7:99717580:C:G	W126C	0.996
7:99707909:C:G	R440T	0.994
7:99717547:G:C	F137L	0.993
7:99717547:G:T	F137L	0.993
7:99717549:A:G	F137L	0.993
7:99707909:C:A	R440I	0.992
7:99707971:G:C	F419L	0.992
7:99707971:G:T	F419L	0.992
7:99707973:A:G	F419L	0.992
7:99715888:G:C	S180R	0.992
7:99715888:G:T	S180R	0.992
7:99715890:T:G	S180R	0.992
7:99707915:C:T	G438E	0.991
7:99709203:T:A	E362V	0.991
7:99717581:C:G	W126S	0.991
7:99717219:A:G	L160P	0.990
7:99717570:G:C	R130G	0.990
7:99717581:C:A	W126L	0.990
7:99707902:G:C	C442W	0.989
7:99707925:A:T	F435I	0.989
7:99710796:A:G	L321P	0.989

dbSNP variants (sampled 300 via entrez): RS1000189515 (7:99723701 A>T), RS1000318792 (7:99735367 T>C,G), RS1000472813 (7:99722816 A>G), RS1000781448 (7:99716579 G>A,C,T), RS1000916923 (7:99716245 C>A), RS1001115135 (7:99709566 C>T), RS1001527437 (7:99727067 T>G), RS1001559924 (7:99727297 C>G), RS1001746795 (7:99720973 G>C), RS1001803465 (7:99708714 A>G), RS1001865668 (7:99708411 C>A,G), RS1001867755 (7:99725735 G>A), RS1002098364 (7:99726218 C>T), RS1002134760 (7:99719235 C>G), RS1002328665 (7:99732551 GCAACCCAT>G)

Disease associations

OMIM: gene MIM:605340 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

20 associations (top):

Study	Trait	p-value
GCST002925_11	Sex hormone levels	2.000000e-14
GCST002925_12	Sex hormone levels	2.000000e-07
GCST002925_6	Sex hormone levels	6.000000e-14
GCST006249_47	Serum metabolite levels	1.000000e-45
GCST006464_11	Endometrial cancer	3.000000e-07
GCST009733_13	Urinary metabolite levels in chronic kidney disease	1.000000e-13
GCST009733_131	Urinary metabolite levels in chronic kidney disease	4.000000e-12
GCST009735_6	Urinary metabolite modules (eigenmetabolites) in chronic kidney disease	1.000000e-10
GCST012020_383	Serum metabolite levels	4.000000e-49
GCST012020_384	Serum metabolite levels	5.000000e-60
GCST012020_385	Serum metabolite levels	1.000000e-23
GCST012020_386	Serum metabolite levels	1.000000e-48
GCST012020_387	Serum metabolite levels	4.000000e-36
GCST012020_388	Serum metabolite levels	2.000000e-37
GCST012020_389	Serum metabolite levels	4.000000e-75
GCST012020_390	Serum metabolite levels	1.000000e-12
GCST012020_391	Serum metabolite levels	4.000000e-60
GCST012020_392	Serum metabolite levels	9.000000e-12
GCST90020091_5	Estradiol levels	1.000000e-09
GCST90020092_1	Estradiol levels	8.000000e-12

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004730	hormone measurement
EFO:0007001	dehydroepiandrosterone sulphate measurement
EFO:0004908	testosterone measurement
EFO:0005116	urinary metabolite measurement
EFO:0004697	estradiol measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL2364675 (PROTEIN FAMILY), CHEMBL3341582 (SINGLE PROTEIN), CHEMBL4523986 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

10 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 486,015 (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
CHEMBL1136	TELITHROMYCIN	4	15,927
CHEMBL157101	KETOCONAZOLE	4	75,361
CHEMBL160	CYCLOSPORINE	4	168,247
CHEMBL163	RITONAVIR	4	53,773
CHEMBL269732	TACROLIMUS ANHYDROUS	4	95,168
CHEMBL451887	CARFILZOMIB	4	12,508
CHEMBL638	VORICONAZOLE	4	23,088
CHEMBL190461	CANNABIDIOL	4	26,379
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL5314518	GLECIRASIB	2	24

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
CYP3A71A, CYP3A71C	Metabolism/PK	3	tacrolimus	Kidney Transplantation

PharmGKB variants

9 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2257401	CYP3A7, ZSCAN25		0.00	0
rs10211	CYP3A7, ZSCAN25		0.00	0
rs45446698	CYP3A7, ZSCAN25		0.00	1
rs11568824	CYP3A7, ZSCAN25		0.00	1
rs45494802	CYP3A7, ZSCAN25		0.00	1
rs45575938	CYP3A7, ZSCAN25		0.00	1
rs45467892	CYP3A7, ZSCAN25		0.00	1
rs11568825	CYP3A7, ZSCAN25		0.00	1
rs11568826	CYP3A7, ZSCAN25		0.00	1

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — CYP3 family

ChEMBL bioactivities

47 potent at pChembl≥5 of 60 total, top 47 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.92	Ki	1.2	nM	CHEMBL583090
8.62	Ki	2.4	nM	TELITHROMYCIN
8.28	Ki	5.3	nM	CHEMBL583093
8.25	Ki	5.6	nM	CHEMBL583091
7.89	Ki	13	nM	RITONAVIR
7.62	Ki	24	nM	CHEMBL583299
7.60	Ki	25	nM	CHEMBL583298
6.96	IC50	110	nM	KETOCONAZOLE
6.85	IC50	140	nM	RITONAVIR
6.80	IC50	160	nM	CHEMBL3527048
6.80	IC50	160	nM	KETOCONAZOLE
6.60	IC50	251.2	nM	CHEMBL601428
6.48	IC50	330	nM	CHEMBL3527048
6.44	Ki	360	nM	TACROLIMUS ANHYDROUS
6.31	IC50	490	nM	CARFILZOMIB
6.24	IC50	570	nM	CHEMBL5435851
6.21	Ki	610	nM	TACROLIMUS ANHYDROUS
6.18	Ki	660	nM	VORICONAZOLE
6.16	IC50	700	nM	CHEMBL3330409
6.13	IC50	740	nM	TACROLIMUS ANHYDROUS
6.05	IC50	900	nM	CHEMBL3330410
6.03	IC50	940	nM	TACROLIMUS ANHYDROUS
6.01	Ki	980	nM	CYCLOSPORINE
5.96	IC50	1100	nM	CHEMBL2130955
5.96	IC50	1100	nM	RITONAVIR
5.91	IC50	1240	nM	CYCLOSPORINE
5.85	IC50	1400	nM	CHEMBL3527048
5.84	IC50	1450	nM	GLECIRASIB
5.83	IC50	1470	nM	CYCLOSPORINE
5.75	IC50	1800	nM	CHEMBL3542335
5.72	IC50	1900	nM	CHEMBL2130955
5.60	IC50	2500	nM	CHEMBL5612347
5.55	IC50	2800	nM	CHEMBL2130955
5.54	IC50	2900	nM	VORICONAZOLE
5.53	Ki	2970	nM	VORICONAZOLE
5.43	IC50	3700	nM	CHEMBL5406721
5.43	IC50	3700	nM	CHEMBL46909
5.42	IC50	3800	nM	CHEMBL5418617
5.41	IC50	3900	nM	CHEMBL5429178
5.34	IC50	4600	nM	RITONAVIR
5.31	IC50	4900	nM	CHEMBL2130955
5.23	IC50	5900	nM	CHEMBL5406218
5.22	IC50	6053	nM	CHEMBL65590
5.17	IC50	6830	nM	GLECIRASIB
5.14	IC50	7300	nM	CHEMBL6190745
5.10	IC50	7900	nM	PAZOPANIB
5.00	IC50	1e+04	nM	CHEMBL5395150

PubChem BioAssay actives

82 with measured affinity, of 1182 total; 29 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
(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-hydroxy-1,5,7,9,11,13-hexamethyl-15-[1-(1,5-naphthyridin-4-ylmethyl)azetidin-3-yl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0012	uM
Telithromycin	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0024	uM
(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-hydroxy-1,5,7,9,11,13-hexamethyl-15-[1-[(1R)-1-(1,8-naphthyridin-4-yl)ethyl]azetidin-3-yl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0053	uM
(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-hydroxy-1,5,7,9,11,13-hexamethyl-15-[1-(1,8-naphthyridin-4-ylmethyl)azetidin-3-yl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0056	uM
Ritonavir	2033231: Inhibition of CYP3A-mediated metabolism in human liver microsomes	ki	0.0130	uM
(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-hydroxy-15-[1-[(3-hydroxy-1,5-naphthyridin-4-yl)methyl]azetidin-3-yl]-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0240	uM
(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-hydroxy-15-[1-[(3-hydroxy-1,8-naphthyridin-4-yl)methyl]azetidin-3-yl]-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone	440648: Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	ki	0.0250	uM
8-imidazol-1-yl-5,6,7,8-tetrahydroquinoline	2022035: Inhibition of CYP450 (unknown origin)	ic50	0.0335	uM
1-methyl-3-[1-methyl-5-(4-methylphenyl)pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]pyrazolo[5,4-d]pyrimidine	1217207: Reversible inhibition of human CYP3A felodipine oxidase activity	ic50	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
Tacrolimus	1209606: Competitive inhibition of CYP3A in human liver microsomes	ki	0.3600	uM
Carfilzomib	1219229: Inhibition of CYP3A in human liver microsomes assessed as substrate metabolite formation using midazolam as substrate preincubated with microsomes for 30 mins prior to substrate addition measured after 5 mins by LC-MS/MS analysis	ic50	0.4900	uM
(3S,3aS,6aR)-2-[(2S)-2-[[2-(1-adamantyl)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(1S)-1-cyclohexyl-3-(cyclopropylamino)-2,3-dioxopropyl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide	2020327: Inhibition of CYP3A (unknown origin)	ic50	0.5700	uM
Voriconazole	541854: Competitive inhibition of CYP3A in human liver microsomes assessed as midazolam 4-hydroxylation after 5 mins by Dixon plot analysis	ki	0.6600	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
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
cyclosporine	1209614: Reversible competitive inhibition of CYP3A-mediated 1’-OH midazolam formation in human liver microsomes after 7.5 mins by nonlinear regression study	ki	0.9800	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
N-[1-[(1,2-dihydroxy-2,6-dimethyl-3-oxoheptan-4-yl)amino]-1-oxo-3-phenylpropan-2-yl]-4-methyl-2-[[2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide	1219244: Time-dependent inhibition of CYP3A in human liver microsomes preincubated for 30 mins with carfilzomib by LC-MS/MS analysis	ic50	1.8000	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
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
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
(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
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
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

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

Chemical	Actions (top 5)	PubMed papers
Rifampin	increases expression	6
Aflatoxin B1	affects expression, decreases expression, decreases methylation, increases expression, affects cotreatment (+1 more)	6
Phenobarbital	affects expression, increases expression	5
Benzo(a)pyrene	decreases expression, increases expression, increases methylation	4
Dehydroepiandrosterone	affects metabolic processing, increases hydroxylation	4
Cyclosporine	decreases expression, increases expression	4
Acetaminophen	decreases expression, increases expression	3
Parathion	affects metabolic processing, increases expression	3
perfluorooctanoic acid	affects binding, decreases activity, increases expression	2
thiacloprid	decreases reaction, increases expression	2
Calcitriol	increases expression	2
Dexamethasone	increases expression	2
Chlorpyrifos	affects metabolic processing	2
Estradiol	decreases expression	2
Malathion	affects metabolic processing, increases expression	2
Tetrachlorodibenzodioxin	increases expression	2
Tretinoin	affects metabolic processing, decreases expression	2
Dehydroepiandrosterone Sulfate	increases oxidation, decreases reaction, affects abundance, increases hydroxylation	2
ammonium 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate	decreases expression	1
fluorene-9-bisphenol	decreases expression	1
dicrotophos	decreases expression	1
helenalin	increases oxidation	1
4-oxoretinoic acid	decreases expression	1
bufotalin	increases expression	1
methyleugenol	decreases expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
senecionine	increases expression	1
VX-agent	increases expression	1
heliotrine	decreases expression	1
enilconazole	decreases expression	1

ChEMBL screening assays

303 unique, capped per target: 301 admet, 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1042375	ADMET	Inhibition of CYP3A in human liver microsomes assessed as hydroxymidazolam formation by time dependent inhibition assay	Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections. — J Med Chem
CHEMBL4614611	Binding	Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 12-OHNVP by measuring Kcat/Km ratio in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis	Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. — J Med Chem

Cellosaurus cell lines

20 cell lines: 16 spontaneously immortalized cell line, 3 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_UH20	HEK293 CYP3A7*2-V5	Transformed cell line	Female
CVCL_UU87	MCF-7 M13	Cancer cell line	Female
CVCL_UU88	MCF-7 M21	Cancer cell line	Female
CVCL_UU89	MCF-7 M27	Cancer cell line	Female
CVCL_UU97	CHL 7-20	Spontaneously immortalized cell line	Female
CVCL_UU98	CHL 7-33	Spontaneously immortalized cell line	Female
CVCL_UU99	CHL 7-38	Spontaneously immortalized cell line	Female
CVCL_UV00	CHL 7-40	Spontaneously immortalized cell line	Female
CVCL_UV01	CHL 7P-101	Spontaneously immortalized cell line	Female
CVCL_UV02	CHL 7P-142	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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