CYP3A5
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Also known as PCN3P450PCN3CP35
Summary
CYP3A5 (cytochrome P450 family 3 subfamily A member 5, HGNC:2638) is a protein-coding gene on chromosome 7q22.1, encoding Cytochrome P450 3A5 (P20815). A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins.
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. The encoded protein metabolizes drugs as well as the steroid hormones testosterone and progesterone. This gene is part of a cluster of cytochrome P450 genes on chromosome 7q21.1. Two pseudogenes of this gene have been identified within this cluster on chromosome 7. Expression of this gene is widely variable among populations, and a single nucleotide polymorphism that affects transcript splicing has been associated with susceptibility to hypertensions. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 1577 — RefSeq curated summary.
At a glance
- GWAS associations: 16
- Clinical variants (ClinVar): 74 total
- Phenotypes (HPO): 4
- Druggable target: yes — 17 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_000777
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2638 |
| Approved symbol | CYP3A5 |
| Name | cytochrome P450 family 3 subfamily A member 5 |
| Location | 7q22.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PCN3, P450PCN3, CP35 |
| Ensembl gene | ENSG00000106258 |
| Ensembl biotype | protein_coding |
| OMIM | 605325 |
| Entrez | 1577 |
Gene structure
Transcript identifiers
Ensembl transcripts: 24 — 11 protein_coding, 9 retained_intron, 2 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined
ENST00000222982, ENST00000439761, ENST00000456417, ENST00000461920, ENST00000463364, ENST00000463907, ENST00000466061, ENST00000469622, ENST00000469887, ENST00000473347, ENST00000480723, ENST00000481825, ENST00000488187, ENST00000489231, ENST00000646887, ENST00000882630, ENST00000882631, ENST00000882632, ENST00000882633, ENST00000882634, ENST00000882635, ENST00000882636, ENST00000882637, ENST00000882638
RefSeq mRNA: 4 — MANE Select: NM_000777
NM_000777, NM_001190484, NM_001291829, NM_001291830
CCDS: CCDS55134, CCDS5672
Canonical transcript exons
ENST00000222982 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001865277 | 99648194 | 99648400 |
| ENSE00003462743 | 99650073 | 99650232 |
| ENSE00003476604 | 99674533 | 99674585 |
| ENSE00003476809 | 99660499 | 99660659 |
| ENSE00003488439 | 99663968 | 99664095 |
| ENSE00003517661 | 99662816 | 99662882 |
| ENSE00003520008 | 99666952 | 99667065 |
| ENSE00003567838 | 99676115 | 99676208 |
| ENSE00003582326 | 99665166 | 99665314 |
| ENSE00003583387 | 99652553 | 99652779 |
| ENSE00003604856 | 99666601 | 99666689 |
| ENSE00003620637 | 99679826 | 99679996 |
| ENSE00003690910 | 99672580 | 99672679 |
Expression profiles
Bgee: expression breadth ubiquitous, 243 present calls, max score 99.55.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.6883 / max 159.9341, expressed in 79 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 85112 | 0.6883 | 79 |
Top tissues by expression
287 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| jejunal mucosa | UBERON:0000399 | 99.55 | gold quality |
| right lobe of liver | UBERON:0001114 | 99.27 | gold quality |
| liver | UBERON:0002107 | 98.51 | gold quality |
| gall bladder | UBERON:0002110 | 98.00 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 97.93 | gold quality |
| duodenum | UBERON:0002114 | 97.60 | gold quality |
| rectum | UBERON:0001052 | 97.20 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 97.06 | gold quality |
| colonic mucosa | UBERON:0000317 | 96.64 | gold quality |
| body of pancreas | UBERON:0001150 | 96.53 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 96.45 | gold quality |
| buccal mucosa cell | CL:0002336 | 95.94 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 94.97 | gold quality |
| pylorus | UBERON:0001166 | 94.79 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 94.47 | gold quality |
| skin of abdomen | UBERON:0001416 | 94.46 | gold quality |
| small intestine | UBERON:0002108 | 94.39 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 94.30 | gold quality |
| esophagus mucosa | UBERON:0002469 | 94.08 | gold quality |
| skin of leg | UBERON:0001511 | 93.49 | gold quality |
| transverse colon | UBERON:0001157 | 92.41 | gold quality |
| body of stomach | UBERON:0001161 | 92.39 | gold quality |
| right lung | UBERON:0002167 | 91.89 | gold quality |
| pancreas | UBERON:0001264 | 91.82 | gold quality |
| mucosa of stomach | UBERON:0001199 | 91.47 | gold quality |
| zone of skin | UBERON:0000014 | 91.46 | gold quality |
| stomach | UBERON:0000945 | 91.34 | gold quality |
| left adrenal gland | UBERON:0001234 | 90.56 | gold quality |
| right adrenal gland | UBERON:0001233 | 90.53 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 90.25 | gold quality |
Single-cell (SCXA)
Detected in 10 experiment(s), a significant marker in 8.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-23 | yes | 2585.96 |
| E-GEOD-130473 | yes | 1706.34 |
| E-GEOD-125970 | yes | 75.34 |
| E-CURD-119 | yes | 56.07 |
| E-MTAB-8410 | yes | 23.68 |
| E-MTAB-10553 | yes | 21.08 |
| E-HCAD-9 | yes | 9.78 |
| E-CURD-135 | no | 2774.86 |
| E-MTAB-9801 | no | 2.75 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AR, HNF4A, NR1I2, NR1I3, NR3C1, SP1, SP3, VDR, YY1
miRNA regulators (miRDB)
4 targeting CYP3A5, 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-329-5P | 99.27 | 68.11 | 1597 |
| HSA-MIR-4635 | 98.74 | 67.63 | 1339 |
| HSA-MIR-6764-3P | 98.44 | 67.64 | 1153 |
| HSA-MIR-6824-3P | 98.44 | 67.62 | 1154 |
Literature-anchored findings (GeneRIF, showing 40)
- genetic determinants of the CYP3A5 polymorphism (PMID:11740341)
- CYP3A5 polymorphism is associated with myeloid leukemia (PMID:11836601)
- High activity CYP3A4, but not CYP3A5, which primarily metabolizes testosterone, showed a striking association with the onset of puberty. (PMID:12692107)
- a high cytochrome P450, family 3, subfamily A, polypeptide 5 expressor allele frequency among African-Americans may contribute to a high prevalence of sodium-sensitive hypertension in this population (PMID:12754175)
- Carriers of this genotype require a high dose of tacrolimus to achieve the target concentration after liver transplantation. (PMID:15226679)
- CYP3A5 induction in the human liver and intestine is mediated by the xenobiotic sensors pregnane X receptor (PXR) and constitutively activated receptor (CAR) (PMID:15252010)
- Polymorphic CYP3A5 haplotypes reflecting high CYP3A5 protein expression were associated with increased levels of aflatoxin-albumin adducts. (PMID:15454734)
- Although untreated blood pressure may be higher in blacks with the CYP3A5*3/*3 genotype, the CYP3A5*1 allele may be associated with hypertension that is more refractory to treatment in this ethnic group. (PMID:15596575)
- Our results demonstrate that the CYP3A5*1 allele, previously reported as a marker for CYP3A5 expression in human kidney, is associated with increased risk for BEN, while CYP3A4*1B and CYP2D6 genotypes do not significantly modify the risk for the disease. (PMID:15708542)
- Patients with the CYP3A5*3/*3 genotype require less tacrolimus to reach target concentrations compared to those with the CYP3A5*1 allele in kidney transplantation. (PMID:15808586)
- The CYP3A5 A6986G polymorphism may be specifically associated with a decreased risk of low-grade or early stage prostate cancer (PMID:15876487)
- Renal transplant recipients who were CYP3A5*1 carriers required a higher dose of tacrolimus than CYP3A5*3/*3, indicating a significantly lower dose-adjusted area under the curveof tacrolimus. (PMID:15919447)
- possible role of CYP3A5 as a genetic contributor to hypertension susceptibility (PMID:15952872)
- Individuals homozygous for defective CYP3A5 had reduced risk of developing oesophageal cancer (PMID:15978331)
- genotyping tests for defective CYP3A4/CYP3A5 haplotypes will be necessary to understand the variations in the metabolism and clinical toxicity of a wide variety of clinical drugs–REVIEW (PMID:16004554)
- CYP3A5*3 is the primary allelic variant in Chinese population. CYP3A5 genotypes are closely associated with blood CsA concentrations in hemopoietic stem cell transplant recipients. (PMID:16086282)
- Polymorphism in CYP3A5 is associated with elevated blood pressure (PMID:16141800)
- Transcription of CYP3A5 gene in leukemia cells directly induces resistance to anthracyclines and alkaloids, the cells are still sensitive to epipodophyllotoxins. (PMID:16188140)
- mRNA level of CYP3A5 is significantly lower in the ascending colon in comparison to the descending and sigmoid colon. (PMID:16253141)
- The CYP3A5*1 genotype is associated with increased saquinavir oral clearance. (PMID:16338276)
- intestinal CYP3A5, as well as hepatic CYP3A5, plays an important role in the first-pass effect of orally administered tacrolimus (PMID:16424824)
- There is a preliminary indication that the CYP3A5 genotype might affect plasma levels of budesonide. (PMID:16584389)
- analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5 (PMID:16684709)
- CYP3A5*1 exhibits no significant effect on blood pressure, left ventricular mass and left ventricular geometry (PMID:16822233)
- The effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine dose adjusted trough blood concentration during the early period after renal transplantation in Chinese patients is reported. (PMID:17042920)
- Genetic polymorphisms in CYP3A5are known to influence tacrolimus (Tac) dose requirements and trough blood levels in stable transplant patients. (PMID:17049058)
- the frequency of the CYP3A5*3C null allele in French Caucasians (81.3%) and in Tunisians (80.0%) is higher than in the Gabonese population (12.5%) (p < 0.001) (PMID:17162466)
- genetic variation in CYP3A5 may predict response to tamoxifen therapy (PMID:17244352)
- there is no significant association between polymorphisms in CYP3A4, CYP3A5, MDR1, GSTM1 and GSTT1 and outcome either after treatment with induction chemotherapy or after high-dose therapy for multiple myeloma (PMID:17296590)
- The AUC for saquinavir among individuals with two functional CYP3A5 alleles was lower than among those with no functional alleles (PMID:17329995)
- ABCB1 and CYP3A5 genes interact with urinary sodium excretion in their effect on ambulatory blood pressure, suggesting a gene-gene-environment interaction. (PMID:17372036)
- Differences exist in protein levels of certain CYPs in non-malignant esophageal tissue (e.g. CYP2C8, CYP3A4, CYP3A5, and CYP2E1) between SCC patients and healthy subjects and may contribute to the development of squamous-cell carcinoma in the esophagus. (PMID:17373732)
- Relationship between reduced presence of CYP3A5 in kidney tubules and nephrotoxicity should be further explored to elucidate role of this enzyme in mediating toxicity. (PMID:17395652)
- A possible influence of CYP3A5 polymorphism on tacrolimus pharmacodynamics. (PMID:17430486)
- CYP3A5, a highly polymorphic member of the CYP3A family, plays an important role in the metabolism of verapamil in vivo. CYP3A5 genotype is associated with variations in verapamil disposition and response in healthy volunteers. (PMID:17443134)
- CYP3A4 plays a major role in TPA023 metabolism, and CYP3A5 may also contribute at higher concentrations of the compound. (PMID:17460031)
- CYP3A5 genotype had no effect on the systemic or apparent oral clearances, or pharmacodynamics, of the CYP3A probes alfentanil and midazolam. (PMID:17554244)
- Differences in CYP3A41G genotype distribution and haplotypes of CYP3A4, CYP3A5 and CYP3A7 in 3 different Chinese ethnic groups; close linkage is demonstrated (PMID:17582393)
- Common polymorphisms on CYP3A4 and CYP3A5 genes do not modify the risk of developing digestive cancers in Western Europe. (PMID:17605821)
- Patients carrying a CYP3A5*1 allele require a twofold higher tacrolimus dose compared with homozygous carriers of the CYP3A5*3 variant allele to maintain the target dnAUC(0-12). (PMID:17635182)
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), CYP3A4 (ENSG00000160868), CYP3A7 (ENSG00000160870)
Protein
Protein identifiers
Cytochrome P450 3A5 — P20815 (reviewed: P20815)
Alternative names: CYPIIIA5, Cytochrome P450-PCN3
All UniProt accessions (2): P20815, Q7Z3N0
UniProt curated annotations — full annotation on UniProt →
Function. A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins. 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. Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2. Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione. Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance. Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine.
Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.
Induction. By glucocorticoids, such as dexamethesone.
Pathway. Steroid hormone biosynthesis. Cofactor metabolism; retinol metabolism.
Miscellaneous. Chimeric transcripts, characterized by CYP3A43 exon 1 joined at canonical splice sites to distinct sets of CYP3A5 exons, have been detected. All are possibly produced by trans-splicing. The chimeric transcripts exist in 2 different combinations: CYP3A43 exon 1 joined in frame to CYP3A5 exon 11-13 and CYP3A43 exon 1 joined in frame to CYP3A5 exon 12-13. All chimeric transcripts are expressed at very low levels in the liver.
Similarity. Belongs to the cytochrome P450 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P20815-1 | 1 | yes |
| P20815-2 | 2 |
RefSeq proteins (4): NP_000768, NP_001177413, NP_001278758, NP_001278759 (=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), 10 shown:
- an organic molecule + reduced [NADPH–hemoprotein reductase] + O2 = an alcohol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:17149)
- all-trans-retinol + reduced [NADPH–hemoprotein reductase] + O2 = all-trans-retinal + oxidized [NADPH–hemoprotein reductase] + 2 H2O + H(+) (RHEA:42092)
- 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 = 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)
- progesterone + reduced [NADPH–hemoprotein reductase] + O2 = 6beta-hydroxyprogesterone + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47252)
- androst-4-ene-3,17-dione + reduced [NADPH–hemoprotein reductase] + O2 = 6beta-hydroxyandrost-4-ene-3,17-dione + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47256)
- 17beta-estradiol + reduced [NADPH–hemoprotein reductase] + O2 = 4-hydroxy-17beta-estradiol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:47280)
- 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)
UniProt features (59 total): helix 24, strand 13, sequence variant 9, turn 5, sequence conflict 4, splice variant 2, chain 1, binding site 1
Structure
Experimental structures (PDB)
6 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6MJM | X-RAY DIFFRACTION | 2.2 |
| 9MS2 | X-RAY DIFFRACTION | 2.25 |
| 7SV2 | X-RAY DIFFRACTION | 2.46 |
| 7LAD | X-RAY DIFFRACTION | 2.65 |
| 8SG5 | X-RAY DIFFRACTION | 2.8 |
| 5VEU | X-RAY DIFFRACTION | 2.91 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P20815-F1 | 93.52 | 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): 441 (axial binding residue)
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-211981 | Xenobiotics |
| R-HSA-5423646 | Aflatoxin activation and detoxification |
MSigDB gene sets: 168 (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, SAENZ_DETOX_PATHWAY_AND_CARCINOGENESIS_DN, GOBP_RETINOL_METABOLIC_PROCESS, DARWICHE_PAPILLOMA_PROGRESSION_RISK, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_DEMETHYLATION, KIM_RESPONSE_TO_TSA_AND_DECITABINE_UP, ACEVEDO_LIVER_TUMOR_VS_NORMAL_ADJACENT_TISSUE_DN, GOBP_TOXIN_METABOLIC_PROCESS, CAIRO_HEPATOBLASTOMA_DN
GO Biological Process (11): lipid hydroxylation (GO:0002933), xenobiotic metabolic process (GO:0006805), steroid metabolic process (GO:0008202), estrogen metabolic process (GO:0008210), alkaloid catabolic process (GO:0009822), xenobiotic catabolic process (GO:0042178), retinol metabolic process (GO:0042572), retinoic acid metabolic process (GO:0042573), aflatoxin metabolic process (GO:0046222), oxidative demethylation (GO:0070989), lipid metabolic process (GO:0006629)
GO Molecular Function (13): monooxygenase activity (GO:0004497), iron ion binding (GO:0005506), retinoic acid 4-hydroxylase activity (GO:0008401), oxidoreductase activity (GO:0016491), oxygen binding (GO:0019825), heme binding (GO:0020037), testosterone 6-beta-hydroxylase activity (GO:0050649), estrogen 16-alpha-hydroxylase activity (GO:0101020), estrogen 2-hydroxylase activity (GO:0101021), protein binding (GO:0005515), 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 (4): endoplasmic reticulum membrane (GO:0005789), intracellular membrane-bounded organelle (GO:0043231), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Cytochrome P450 - arranged by substrate type | 1 |
| Biological oxidations | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| hormone metabolic process | 3 |
| steroid hydroxylase activity | 3 |
| catabolic process | 2 |
| retinoid metabolic process | 2 |
| oxidoreductase activity | 2 |
| monooxygenase 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 |
| metabolic process | 1 |
| cellular response to xenobiotic stimulus | 1 |
| lipid metabolic process | 1 |
| steroid metabolic process | 1 |
| alkaloid metabolic process | 1 |
| xenobiotic metabolic process | 1 |
| primary alcohol metabolic process | 1 |
| olefinic compound metabolic process | 1 |
| monocarboxylic acid metabolic process | 1 |
| mycotoxin metabolic process | 1 |
| demethylation | 1 |
| primary metabolic process | 1 |
| transition metal ion binding | 1 |
| catalytic activity | 1 |
| small molecule binding | 1 |
| tetrapyrrole binding | 1 |
| binding | 1 |
| cation binding | 1 |
| organelle membrane | 1 |
| nuclear outer membrane-endoplasmic reticulum membrane network | 1 |
| endoplasmic reticulum subcompartment | 1 |
| intracellular anatomical structure | 1 |
| membrane-bounded organelle | 1 |
| intracellular organelle | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1846 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CYP3A5 | PPIG | Q13427 | 926 |
| CYP3A5 | ABCB1 | P08183 | 914 |
| CYP3A5 | NR1I2 | O75469 | 804 |
| CYP3A5 | SLCO1B1 | Q9Y6L6 | 787 |
| CYP3A5 | UGT1A4 | P22310 | 769 |
| CYP3A5 | CYB5A | P00167 | 751 |
| CYP3A5 | CYP2E1 | P05181 | 739 |
| CYP3A5 | UGT1A6 | P19224 | 734 |
| CYP3A5 | UGT1A8 | Q9HAW9 | 731 |
| CYP3A5 | UGT2B7 | P16662 | 726 |
| CYP3A5 | UGT1A1 | P22309 | 726 |
| CYP3A5 | P2RY12 | Q9H244 | 726 |
| CYP3A5 | UGT1A7 | Q9HAW7 | 726 |
| CYP3A5 | UGT1A10 | Q9HAW8 | 726 |
| CYP3A5 | VKORC1 | Q9BQB6 | 720 |
IntAct
12 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CYP3A5 | HTT | psi-mi:“MI:0915”(physical association) | 0.560 |
| CYP3A5 | IGHG1 | psi-mi:“MI:0914”(association) | 0.530 |
| CYP3A5 | CYB5A | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| CYP3A5 | CALU | psi-mi:“MI:0915”(physical association) | 0.400 |
| CYP3A5 | CYP3A4 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ETV5 | CYP3A5 | psi-mi:“MI:0915”(physical association) | 0.370 |
| CYP3A5 | ATOH8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| CYP3A5 | RDH13 | psi-mi:“MI:0915”(physical association) | 0.370 |
BioGRID (14): CYP3A7 (Affinity Capture-MS), IGHG2 (Affinity Capture-MS), SERPINB4 (Affinity Capture-MS), IGHG1 (Affinity Capture-MS), CYP3A5 (Proximity Label-MS), CYP3A5 (Negative Genetic), CYP3A5 (Affinity Capture-MS), CYP3A7 (Affinity Capture-MS), IGHG1 (Affinity Capture-MS), SERPINB4 (Affinity Capture-MS), CYP3A4 (Affinity Capture-MS), RDH13 (Two-hybrid), ETV5 (Two-hybrid), CYP3A5 (Two-hybrid)
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
74 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 34 |
| Likely benign | 14 |
| Benign | 3 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2441 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 7:99650068:CTGA:C | donor_loss | 1.0000 |
| 7:99650070:GAC:G | donor_loss | 1.0000 |
| 7:99650071:ACC:A | donor_loss | 1.0000 |
| 7:99650072:C:CT | donor_loss | 1.0000 |
| 7:99650252:T:TC | acceptor_gain | 1.0000 |
| 7:99660655:CAGAG:C | acceptor_gain | 1.0000 |
| 7:99660656:AGAG:A | acceptor_gain | 1.0000 |
| 7:99660657:GAG:G | acceptor_gain | 1.0000 |
| 7:99660660:C:CC | acceptor_gain | 1.0000 |
| 7:99663962:TTTTA:T | donor_loss | 1.0000 |
| 7:99663963:TTTA:T | donor_loss | 1.0000 |
| 7:99663964:TTA:T | donor_loss | 1.0000 |
| 7:99663965:TA:T | donor_loss | 1.0000 |
| 7:99663966:A:AG | donor_loss | 1.0000 |
| 7:99663967:C:CA | donor_loss | 1.0000 |
| 7:99664093:GTA:G | acceptor_gain | 1.0000 |
| 7:99664096:C:CC | acceptor_gain | 1.0000 |
| 7:99665161:CATA:C | donor_gain | 1.0000 |
| 7:99665164:A:AC | donor_gain | 1.0000 |
| 7:99665165:C:CC | donor_gain | 1.0000 |
| 7:99665168:A:AC | donor_gain | 1.0000 |
| 7:99665169:T:C | donor_gain | 1.0000 |
| 7:99665211:T:TA | donor_gain | 1.0000 |
| 7:99665215:A:AC | donor_gain | 1.0000 |
| 7:99665222:T:A | donor_gain | 1.0000 |
| 7:99665313:TG:T | acceptor_gain | 1.0000 |
| 7:99665315:C:CC | acceptor_gain | 1.0000 |
| 7:99672676:CGTT:C | acceptor_gain | 1.0000 |
| 7:99676415:G:C | donor_gain | 1.0000 |
| 7:99679820:A:AC | donor_gain | 1.0000 |
AlphaMissense
3296 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 7:99650184:A:C | F434L | 0.998 |
| 7:99650184:A:T | F434L | 0.998 |
| 7:99650186:A:G | F434L | 0.998 |
| 7:99650169:T:A | R439S | 0.997 |
| 7:99650169:T:G | R439S | 0.997 |
| 7:99650170:C:G | R439T | 0.997 |
| 7:99652681:C:A | R375S | 0.997 |
| 7:99652681:C:G | R375S | 0.997 |
| 7:99667006:C:A | W126C | 0.997 |
| 7:99667006:C:G | W126C | 0.997 |
| 7:99667008:A:G | W126R | 0.997 |
| 7:99667008:A:T | W126R | 0.997 |
| 7:99650170:C:A | R439I | 0.996 |
| 7:99652712:C:G | R365T | 0.996 |
| 7:99650176:C:T | G437E | 0.995 |
| 7:99650182:C:T | G435E | 0.995 |
| 7:99652711:T:A | R365S | 0.995 |
| 7:99652711:T:G | R365S | 0.995 |
| 7:99652721:T:A | E362V | 0.995 |
| 7:99666995:C:G | R130P | 0.995 |
| 7:99650229:G:C | F419L | 0.994 |
| 7:99650229:G:T | F419L | 0.994 |
| 7:99650231:A:G | F419L | 0.994 |
| 7:99660533:A:G | L331P | 0.994 |
| 7:99650185:A:C | F434C | 0.992 |
| 7:99650186:A:T | F434I | 0.992 |
| 7:99665296:G:C | S180R | 0.992 |
| 7:99665296:G:T | S180R | 0.992 |
| 7:99665298:T:G | S180R | 0.992 |
| 7:99666973:G:C | F137L | 0.992 |
dbSNP variants (sampled 300 via entrez): RS1000111953 (7:99680238 C>T), RS1000188828 (7:99654881 T>C), RS1000203154 (7:99654534 A>G), RS1000298793 (7:99663016 C>G,T), RS1000610190 (7:99678432 C>A,T), RS1000780511 (7:99670611 T>G), RS1000811433 (7:99653887 G>A,T), RS1000977865 (7:99673455 T>G), RS1001047699 (7:99666223 T>C), RS1001064188 (7:99678177 G>C), RS1001078689 (7:99665723 G>A), RS1001191704 (7:99658148 C>G,T), RS1001276904 (7:99671929 A>C), RS1001346902 (7:99673934 G>T), RS1001385686 (7:99664252 C>T)
Disease associations
OMIM: gene MIM:605325 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): essential hypertension (MONDO:0001134)
Orphanet (1): NON RARE IN EUROPE: Essential hypertension (Orphanet:243761)
HPO phenotypes
4 total (4 of 4 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0001426 | Non-Mendelian inheritance |
| HP:0004421 | Elevated systolic blood pressure |
| HP:0004972 | Elevated mean arterial pressure |
| HP:0005117 | Elevated diastolic blood pressure |
GWAS associations
16 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002882_2 | Ticagrelor levels in individuals with acute coronary syndromes treated with ticagrelor | 3.000000e-12 |
| GCST005991_15 | Platelet count | 4.000000e-09 |
| GCST006249_46 | Serum metabolite levels | 4.000000e-21 |
| GCST006249_47 | Serum metabolite levels | 1.000000e-45 |
| GCST009733_69 | Urinary metabolite levels in chronic kidney disease | 9.000000e-30 |
| GCST009735_5 | Urinary metabolite modules (eigenmetabolites) in chronic kidney disease | 3.000000e-18 |
| 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 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007007 | ticagrelor measurement |
| EFO:0004309 | platelet count |
| EFO:0005116 | urinary metabolite measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D000075222 | Essential Hypertension | C14.907.489.165 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2111472 (PROTEIN FAMILY), CHEMBL2364675 (PROTEIN FAMILY), CHEMBL3019 (SINGLE PROTEIN), CHEMBL4523986 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 652,907 (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 |
|---|---|---|---|
| CHEMBL157101 | KETOCONAZOLE | 4 | 75,361 |
| CHEMBL1136 | TELITHROMYCIN | 4 | 15,927 |
| 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 |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | 4 | 30,865 |
| CHEMBL116 | AMPRENAVIR | 4 | 29,221 |
| CHEMBL190461 | CANNABIDIOL | 4 | 26,379 |
| CHEMBL554 | LAPATINIB | 4 | 69,326 |
| CHEMBL584 | NELFINAVIR | 4 | 36,859 |
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL4068611 | RELACORILANT | 3 | 530 |
| CHEMBL5314518 | GLECIRASIB | 2 | 24 |
| CHEMBL4646510 | COFROGLIPTIN | 2 | 25 |
| CHEMBL5095174 | CEDIROGANT | 2 | 66 |
PharmGKB: 1 entry (VIP=true, CPIC=true)
PharmGKB clinical annotations
69 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| CYP3A51, CYP3A53 | Metabolism/PK | 1B | tacrolimus | Liver transplantation |
| CYP3A51, CYP3A53 | Toxicity | 3 | tacrolimus | Kidney Transplantation |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | nimodipine | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | dextropropoxyphene | |
| CYP3A51, CYP3A53 | Toxicity | 3 | fentanyl | Neoplasms;Pain |
| CYP3A51, CYP3A53 | Dosage | 3 | oxycodone | |
| CYP3A51, CYP3A53 | Dosage | 3 | sufentanil | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | dabigatran | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | sirolimus | Transplantation |
| CYP3A51, CYP3A53 | Dosage | 3 | sirolimus | |
| CYP3A51, CYP3A53 | Dosage | 3 | cyclosporine | Kidney Transplantation |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | cyclosporine | Kidney Transplantation |
| CYP3A51, CYP3A53 | Toxicity | 3 | olanzapine | Somnolence |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | everolimus | Breast Neoplasms;Heart transplantation;Kidney Neoplasms;Kidney Transplantation;Lung transplantation;Neuroendocrine Tumors |
| CYP3A51, CYP3A53 | Toxicity | 3 | paclitaxel | Neoplasms;Neurotoxicity Syndromes |
| CYP3A51, CYP3A53 | Toxicity | 3 | carboplatin;paclitaxel | Leukopenia;Neutropenia;Ovarian Neoplasms |
| CYP3A51, CYP3A53 | Toxicity | 4 | cyclosporine;tacrolimus | Kidney Transplantation;Transplant rejection |
| CYP3A51, CYP3A53 | Metabolism/PK | 4 | methadone | |
| CYP3A51, CYP3A53 | Efficacy | 4 | tacrolimus | Hematopoietic stem cell transplantation;Kidney Transplantation;Transplant rejection |
| CYP3A51, CYP3A53 | Toxicity | 4 | tacrolimus | Nephrotoxicity |
| CYP3A51, CYP3A53 | Metabolism/PK | 4 | olanzapine | |
| CYP3A51, CYP3A53 | Dosage | 2A | tacrolimus | Liver transplantation |
| CYP3A51, CYP3A53 | Efficacy,Toxicity | 3 | atorvastatin | Myalgia |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | cilostazol | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | granisetron | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | midazolam | |
| CYP3A51, CYP3A53 | Metabolism/PK | 3 | tacrolimus | Nephrotic Syndrome |
| CYP3A51, CYP3A53, CYP3A5*6 | Metabolism/PK | 3 | fentanyl | Pain;Pain;Postoperative |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Metabolism/PK | 1A | tacrolimus | Heart transplantation;Hematopoietic stem cell transplantation;Kidney Transplantation;Lung transplantation |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Dosage | 1A | tacrolimus | Heart transplantation;Hematopoietic stem cell transplantation;Kidney Transplantation;Liver transplantation;Lung transplantation |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Metabolism/PK | 3 | atazanavir;ritonavir | HIV infectious disease |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Metabolism/PK | 3 | atazanavir | |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Efficacy,Metabolism/PK | 3 | maraviroc | HIV infectious disease |
| CYP3A51, CYP3A53, CYP3A56, CYP3A57 | Metabolism/PK | 3 | amlodipine | |
| rs10264272 | Metabolism/PK | 3 | lumefantrine | Malaria |
| rs15524 | Metabolism/PK | 3 | carbamazepine | Epilepsy |
| rs15524 | Metabolism/PK | 3 | tacrolimus | Kidney Transplantation;Liver transplantation |
| rs15524 | Toxicity | 3 | opioids | Opioid-Related Disorders |
PharmGKB variants
15 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs15524 | CYP3A5, ZSCAN25 | 3 | 4.00 | 3 | tacrolimus;carbamazepine;opioids |
| rs776746 | CYP3A5, ZSCAN25 | 3 | 6.25 | 62 | sunitinib;atorvastatin;carbamazepine;lumefantrine;lovastatin;simvastatin;nifedipine;ondansetron;apixaban;tacrolimus |
| rs10264272 | CYP3A5, ZSCAN25 | 3 | 0.00 | 8 | lumefantrine |
| rs17161788 | CYP3A5, ZSCAN25 | 3 | 1.75 | 1 | atorvastatin |
| rs28383479 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs41279854 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs41303343 | CYP3A5, ZSCAN25 | 4 | -1.25 | 7 | lumefantrine |
| rs55817950 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs56244447 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs72552791 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs4646450 | CYP3A5, ZSCAN25 | 3 | 4.75 | 1 | tacrolimus |
| rs3800959 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs4646453 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs6977165 | CYP3A5, ZSCAN25 | 0.00 | 0 | ||
| rs4646449 | CYP3A5, ZSCAN25 | 0.00 | 0 |
PharmGKB dosing guidelines
4 guidelines.
| Source | Drug | Guideline | Dosing? | Recommendation? |
|---|---|---|---|---|
| CPIC | atorvastatin;fluvastatin;lovastatin;pitavastatin;pravastatin;rosuvastatin;simvastatin | Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin and CYP3A4, CYP3A5, HMGCR | ||
| CPIC | tacrolimus | Annotation of CPIC Guideline for tacrolimus and CYP3A5 | yes | yes |
| DPWG | tacrolimus | Annotation of DPWG Guideline for tacrolimus and CYP3A5 | yes | yes |
| RNPGx | tacrolimus | Annotation of RNPGx Guideline for tacrolimus and CYP3A4, CYP3A5 | yes | yes |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — CYP3 family
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| ritonavir | Inhibition | 6.92 | pKi |
Binding affinities (BindingDB)
5 measured of 10 human assays (10 total across all organisms); most potent 5 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 1-[4-[4-[[2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone | IC50 | 127 nM | US-9394290: Selective CYP11B1 inhibitors for the treatment of cortisol dependent diseases |
| 4-[3-[4-[[(3S,4R)-3-fluoro-1-methylpiperidin-4-yl]amino]-1-(2,2,2-trifluoroethyl)indol-2-yl]prop-2-ynylamino]-3-methoxy-N-methylbenzenesulfinamide | IC50 | 2300 nM | US-20250304578: NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUNDS OF N-SULFONAMIDE AND USE THEREOF |
| 4-[3-[8-[[(3S,4R)-3-fluoropiperidin-4-yl]amino]-3-(2,2,2-trifluoroethyl)indolizin-2-yl]prop-2-ynylamino]-3-methoxy-N-methylbenzamide | IC50 | 3800 nM | US-20250304578: NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUNDS OF N-SULFONAMIDE AND USE THEREOF |
| N-[(3S,4R)-3-fluoro-1-methylpiperidin-4-yl]-2-[3-(2-methoxy-4-methylsulfonylanilino)prop-1-ynyl]-3-(2,2,2-trifluoroethyl)imidazo[1,2-a]pyridin-8-amine | IC50 | 5800 nM | US-20250304578: NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUNDS OF N-SULFONAMIDE AND USE THEREOF |
| (2S,5S,8S)-14-methoxy-5-methyl-2-(2-methylpropyl)-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione | IC50 | 15400 nM | US-9695174: Inhibitor of breast cancer resistance protein (BCRP) |
ChEMBL bioactivities
130 potent at pChembl≥5 of 174 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
117 with measured affinity, of 1183 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 |
|---|---|---|---|---|
| (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 |
| 1-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone | 1756369: Inhibition of CYP3A4/5 in human liver microsomes using Midazolam as substrate measured after 20 mins by LC-MS/MS analysis | ic50 | 0.0125 | uM |
| Ritonavir | 2033231: Inhibition of CYP3A-mediated metabolism in human liver microsomes | ki | 0.0130 | uM |
| 1-[4-[4-[[2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone | 2099950: Inhibition of CYP3A4/5 in human liver microsomes incubated for 15 mins by LC-MS/MS analysis | ic50 | 0.0200 | uM |
| Clobetasol Propionate | 1529076: Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for 24 hrs by LC-MS/MS analysis | ic50 | 0.0210 | 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 |
| Tacrolimus | 1209595: Inhibition of human CYP3A5 expressed in supersomes assessed inhibition of 1’-OH midazolam formation preincubated with compound before substrate addition by LC-MS method | ic50 | 0.1400 | 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 |
| Cannabidiol | 1692725: Competitive inhibition of human recombinant CYP3A5 expressed in baculovirus-infected insect cells using diltiazem as substrate incubated for 15 mins followed by NADPH-generating system addition by Michaelis-Menten plot analysis | ki | 0.1900 | uM |
| Amprenavir | 589169: Mechanism based inhibition of human cytochrome P450 3A5 measured by testosterone hydroxylation | ki | 0.2000 | 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-chloro-2-fluorophenyl)-pyrimidin-5-ylmethyl]-N-(4-chlorophenyl)piperazine-1-carboxamide | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 0.3000 | 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 |
| 4-[(E)-1-[4-(2-aminoethoxy)phenyl]-1-(4-hydroxyphenyl)but-1-en-2-yl]phenol | 1203268: Inhibition of human recombinant CYP3A5 assessed as metabolism of 7-benzyloxy-4-trifluoromethylcoumarin to HFC after 30 mins by fluorescence assay | ic50 | 0.5560 | 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 |
| Nelfinavir | 589169: Mechanism based inhibition of human cytochrome P450 3A5 measured by testosterone hydroxylation | ki | 0.5700 | uM |
| (2-chlorophenyl)-(4-chlorophenyl)-pyridin-3-ylmethanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 0.6000 | uM |
| 1-(benzenesulfonyl)-4-[(4-chloro-2-fluorophenyl)-pyridin-3-ylmethyl]piperazine | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 0.6000 | 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 |
| 4-[(E)-1-[4-(2-aminoethoxy)phenyl]-2-phenylbut-1-enyl]phenol | 1203268: Inhibition of human recombinant CYP3A5 assessed as metabolism of 7-benzyloxy-4-trifluoromethylcoumarin to HFC after 30 mins by fluorescence assay | ic50 | 0.7230 | uM |
| 1-[(4-chlorophenyl)-pyridin-3-ylmethyl]-4-propan-2-ylsulfonylpiperazine | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 0.8100 | uM |
| N-[(1R)-1-[1-ethyl-6-(trifluoromethyl)benzimidazol-2-yl]ethyl]pyridine-3-sulfonamide | 1241584: Inhibition of CYP3A5 in human liver microsomes incubated for 5 mins in presence of NADPH and specific substrates by LC/MS/MS method | ic50 | 0.8300 | 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-chloro-2-fluorophenyl)-(4-chlorophenyl)-pyridin-3-ylmethanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | 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 |
| N-propan-2-yl-3-[(4-pyridin-4-ylphenyl)carbamoylamino]benzamide | 645226: Inhibition of recombinant human CYP3A5 in supersomes using midazolam as substrate after 5 mins by LC-MS/MS analysis | ic50 | 0.9800 | uM |
| 1-[[2-fluoro-4-(trifluoromethyl)phenyl]-pyridin-3-ylmethyl]-4-methylsulfonylpiperazine | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.0000 | uM |
| 1-[4-[(4-chloro-2-fluorophenyl)-pyridin-3-ylmethyl]piperazin-1-yl]-2,2-dimethylpropan-1-one | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.0000 | 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 |
| (4-chloro-2-fluorophenyl)-(4-propan-2-yloxyphenyl)-pyridin-3-ylmethanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 1.1000 | uM |
| 1-[(4-chloro-2-fluorophenyl)-pyridin-3-ylmethyl]-4-methylsulfonylpiperazine | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.3000 | uM |
| (4-propan-2-yloxyphenyl)-pyridin-3-yl-[4-(trifluoromethyl)phenyl]methanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 1.4000 | uM |
| (4-chloro-2-fluorophenyl)-pyridin-3-yl-[4-(trifluoromethyl)phenyl]methanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 1.4000 | uM |
| 3-[[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]-N,N-di(propan-2-yl)benzamide | 645226: Inhibition of recombinant human CYP3A5 in supersomes using midazolam as substrate after 5 mins by LC-MS/MS analysis | ic50 | 1.6000 | 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-[(4-chloro-2-fluorophenyl)-pyridin-3-ylmethyl]piperazin-1-yl]-cyclopropylmethanone | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.8000 | uM |
| (4-chlorophenyl)-(4-propan-2-yloxyphenyl)-pyridin-3-ylmethanol | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 1.9000 | uM |
| tert-butyl 4-[(4-chloro-2-fluorophenyl)-pyridin-3-ylmethyl]piperazine-1-carboxylate | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.9000 | uM |
| 1-(benzenesulfonyl)-4-[(4-chlorophenyl)-pyridin-3-ylmethyl]piperazine | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 1.9000 | uM |
| 2,2-dimethyl-1-[4-[pyridin-3-yl-[4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]propan-1-one | 730416: Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ic50 | 2.3000 | uM |
| 5-[(5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-oxo-2,4,5,6,7,8,9,11,12,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pyran-2-one | 1822697: Time dependent inhibition of recombinant human CYP3A5 using midazolam as substrate preincubated for 30 mins in presence of NADPH generating system followed by substrate addition incubated for 30 mins by LC-MS/MS analysis | ic50 | 2.3400 | 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-chlorophenyl)-hydroxy-pyridin-3-ylmethyl]benzamide | 673462: Inhibition of CYP3A4/5 in human liver microsomes | ic50 | 2.6000 | uM |
| 5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one | 1822701: Time dependent inhibition of recombinant human CYP3A5 incubated for 30 mins in presence of NADPH generating system by LC-MS/MS analysis | ic50 | 2.7600 | uM |
CTD chemical–gene interactions
265 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Testosterone | decreases reaction, increases hydroxylation, affects cotreatment, increases expression, decreases expression (+3 more) | 11 |
| Tacrolimus | affects response to substance, affects metabolic processing, affects reaction, decreases metabolic processing, decreases methylation (+1 more) | 10 |
| Rifampin | increases expression | 9 |
| Ketoconazole | affects response to substance, increases expression, increases hydroxylation, increases oxidation, affects reaction (+4 more) | 8 |
| Cyclosporine | decreases expression, increases expression, affects metabolic processing, affects cotreatment | 8 |
| Midazolam | affects metabolic processing, increases hydroxylation, increases chemical synthesis, increases metabolic processing, decreases reaction (+1 more) | 7 |
| Aflatoxin B1 | affects expression, decreases expression, increases expression, increases activity | 7 |
| Phenobarbital | affects expression, increases expression | 6 |
| Benzo(a)pyrene | decreases expression, increases expression | 5 |
| Dexamethasone | increases expression, decreases reaction, affects reaction | 4 |
| Chlorpyrifos | increases expression, affects metabolic processing | 4 |
| Tobacco Smoke Pollution | affects expression, decreases expression, increases expression | 4 |
| ochratoxin A | decreases expression, increases expression, increases response to substance | 3 |
| 6 beta-hydroxytestosterone | increases chemical synthesis, increases hydroxylation, decreases reaction | 3 |
| 1-hydroxymethylmidazolam | decreases reaction, increases chemical synthesis, increases hydroxylation | 3 |
| Acetaminophen | decreases expression, increases expression, affects cotreatment | 3 |
| Beclomethasone | decreases reaction, increases expression | 3 |
| Calcitriol | increases expression, affects cotreatment | 3 |
| Parathion | affects metabolic processing | 3 |
| Tamoxifen | affects metabolic processing, increases metabolic processing, increases abundance, decreases activity | 3 |
| Tetrachlorodibenzodioxin | increases expression | 3 |
| Thalidomide | increases chemical synthesis, increases metabolic processing, increases expression, increases hydroxylation | 3 |
| Alfentanil | affects metabolic processing, increases reaction, decreases reaction | 3 |
| tetrandrine | decreases abundance, increases reaction, decreases expression, increases abundance, increases expression (+2 more) | 2 |
| afimoxifene | decreases activity, increases metabolic processing, increases abundance | 2 |
| sodium arsenite | decreases expression, increases abundance, increases expression | 2 |
| N-desmethyltamoxifen | increases abundance, decreases activity, increases metabolic processing | 2 |
| fipronil | increases expression, affects cotreatment | 2 |
| Fluticasone | affects response to substance, increases metabolic processing, decreases activity, increases expression, decreases reaction | 2 |
| Clopidogrel | affects response to substance, increases cleavage, increases oxidation | 2 |
ChEMBL screening assays
604 unique, capped per target: 585 admet, 19 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1919560 | ADMET | Inhibition of CYP3A4/5-mediated testosterone 6beta-hydroxylation in human liver microsomes by LCMS analysis | Novel orally active antimalarial thiazoles. — J Med Chem |
| CHEMBL6077306 | Binding | Time dependent inhibition of CYP3A4/5 (unknown origin) at 30 uM measured after 30 mins relative to control | Discovery of a Novel Mutant-Selective Epidermal Growth Factor Receptor Inhibitor Using an In Silico Enabled Drug Discovery Platform. — J Med Chem |
Cellosaurus cell lines
5 cell lines: 3 induced pluripotent stem cell, 2 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_UH17 | HEK293 CYP3A5*1 | Transformed cell line | Female |
| CVCL_UH18 | HEK293 CYP3A5*1-V5 | Transformed cell line | Female |
| CVCL_UM09 | LSCTRi006-A | Induced pluripotent stem cell | Female |
| CVCL_VE29 | LSCTRi001-A | Induced pluripotent stem cell | Female |
| CVCL_VE30 | LSCTRi002-A | Induced pluripotent stem cell | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00157963 | PHASE4 | COMPLETED | Hydrochlorothiazide (+) Losartan Potassium vs. Amlodipine Comparative Study (0954A-314) |
| NCT00295555 | PHASE4 | COMPLETED | Doxazosin Effects on ABPM in Hypertensive Patients With Diabetic Nephropathy |
| NCT00311155 | PHASE4 | COMPLETED | Olmesartan and an add-on Treatment in Patients With Mild to Moderate Hypertension |
| NCT00328965 | PHASE4 | COMPLETED | Lacidipine In Mild To Moderate Essential Hypertension Patients With Type 2 Diabetes In Korea |
| NCT00366119 | PHASE4 | UNKNOWN | Safety and Efficacy of Ramipril in the Treatment of Essential Hypertension |
| NCT00408512 | PHASE4 | COMPLETED | Pharmacosurveillance and Pharmacogenetics of First-line Diuretics in Hypertension: The StayOnDiur Study |
| NCT00438945 | PHASE4 | COMPLETED | The Effect of Eprosartan on Hormones and Kidney Function in Patients With Essential Hypertension |
| NCT00457483 | PHASE4 | COMPLETED | Nijmegen Antihypertensive Management Improvement Study |
| NCT00509470 | PHASE4 | COMPLETED | Evaluation of Effect of Combination With Telmisartan and Hydrochlorothiazide in Hypertensives Uncontrolled on Amlodipine |
| NCT00654875 | PHASE4 | COMPLETED | Efficacy and Safety of Once Daily Dosing of Aliskiren (300 mg (qd) Once a Day) to Twice Daily Dosing of Aliskiren (150 mg (Bid) Twice a Day) in Treating Moderate Hypertension. |
| NCT00716950 | PHASE4 | UNKNOWN | Valsartan and Amlodipine Compared to Losartan and Amlodipine in Hypertensive Patients |
| NCT00741585 | PHASE4 | COMPLETED | Prognostic Value of the Circadian Pattern of Ambulatory Blood Pressure for Multiple Risk Assessment |
| NCT00765947 | PHASE4 | COMPLETED | Efficacy and Tolerability of an Aliskiren-based Treatment Algorithm in Patients With Mild to Moderate Hypertension |
| NCT00794885 | PHASE4 | COMPLETED | China Stroke Primary Prevention Trial |
| NCT00819104 | PHASE4 | COMPLETED | A Study to Compare the Efficacy, Safety and Tolerability of Selomax With Its Individual Components |
| NCT00841308 | PHASE4 | UNKNOWN | Home Blood Pressure in Hypertension Management |
| NCT00890591 | PHASE4 | COMPLETED | Efficacy and Safety of Olmesartan Medoxomil in Stage 1 and 2 Essential Hypertension |
| NCT00994617 | PHASE4 | UNKNOWN | Monotherapy Versus Dual Therapy for Initial Treatment for Hypertension |
| NCT01011660 | PHASE4 | UNKNOWN | Effects of Angiotensin II Receptor Blocker Compared With Diuretics in High-risk Hypertensive Patients |
| NCT01042392 | PHASE4 | COMPLETED | Efficacy of Aliskiren Compared to Ramipril in the Treatment of Moderate Systolic Hypertensive Patients |
| NCT01120990 | PHASE4 | COMPLETED | Hybrid Blood Pressure Monitor Validation |
| NCT01131546 | PHASE4 | COMPLETED | Efficacy and Safety of Levamlodipine Besylate Compared to Amlodipine Maleate in Patients With Essential Hypertension |
| NCT01132768 | PHASE4 | TERMINATED | The Confirmatory Olmesartan Plaque Regression Study |
| NCT01180413 | PHASE4 | COMPLETED | Intensive Vasodilator Therapy in Patients With Essential Hypertension |
| NCT01241487 | PHASE4 | COMPLETED | A National Multicentre Study to Assess the Efficacy of the Fixed Combination of Valsartan and Amlodipine in Hypertensive Patients Not Controlled by Monotherapy |
| NCT01629225 | PHASE4 | UNKNOWN | GRK4 Polymorphisms Blood Pressure Response to Candesartan |
| NCT01825759 | PHASE4 | UNKNOWN | Danshen Dropping Pill for Coronary Heart Disease Heart and Artery Structure and Function |
| NCT02031861 | PHASE4 | COMPLETED | Efficacy Study of Nifedipine Controlled-Release Tablets (Xin Ran) to Treat Mild to Moderate Essential Hypertension |
| NCT02058446 | PHASE4 | COMPLETED | PMS Study of Amlodipine/Valsartan for the Treatment of Hypertension |
| NCT02062645 | PHASE4 | COMPLETED | Study of Efficacy and Safety of CVAA489 in Hypertensive Patients |
| NCT02184858 | PHASE4 | COMPLETED | Dose Titration of Lisinopril in Children Aged 1 to 18 Years With Primary or Secondary Hypertension |
| NCT02214498 | PHASE4 | UNKNOWN | Treatment of HYpertension: Morning Versus Evening |
| NCT02357615 | PHASE4 | UNKNOWN | Efficacy Study of Nifedipine Controlled-Release Tablets (Xin Ran) to Treat Early Morning Blood Pressure and Central Arterial Pressure |
| NCT02517866 | PHASE4 | COMPLETED | Azilsartan Medoxomil in the Treatment of Essential Hypertension and Type 2 Diabetes in Asia |
| NCT02612298 | PHASE4 | COMPLETED | Efficacy and Safety of Arotinolol Hydrochloride on Morning Blood Pressure and Heart Rate |
| NCT02687178 | PHASE4 | COMPLETED | Canrenone as Add-on in Patients With Essential Hypertension |
| NCT03226340 | PHASE4 | UNKNOWN | S-amlodipine+Chlorthalidone vs S-amlodipine+Telmisartan in Hypertension |
| NCT04306627 | PHASE4 | UNKNOWN | Effect of Atorvastatin on Carotid Intima Media Thickness |
| NCT05683301 | PHASE4 | COMPLETED | Treatment Optimisation for Blood Pressure With Single-Pill Combinations in India |
| NCT05843162 | PHASE4 | UNKNOWN | A Clinical Trial to Evaluate the Blood Pressure Control of Telmisartan or Losartan in Essential Hypertensive Patients With Metabolic Syndrome |
Related Atlas pages
- Targeted by drugs: Ritonavir
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): essential hypertension