Page last updated: 2024-08-07 18:31:38
Cytochrome P450 3A5
A cytochrome P450 3A5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P20815]
Synonyms
EC 1.14.14.1;
CYPIIIA5;
Cytochrome P450-PCN3
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (4.17) | 29.6817 |
| 2010's | 15 (62.50) | 24.3611 |
| 2020's | 8 (33.33) | 2.80 |
Compounds (32)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| niacinamide | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 2,2-dimethylbutyric acid | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| tranylcypromine | Homo sapiens (human) | IC50 | 6.2000 | 1 | 1 |
| clobetasol propionate | Homo sapiens (human) | IC50 | 3.1692 | 5 | 5 |
| nelfinavir | Homo sapiens (human) | Ki | 0.5700 | 1 | 1 |
| amprenavir | Homo sapiens (human) | Ki | 0.2000 | 1 | 1 |
| proadifen hydrochloride | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
| pirlindole | Homo sapiens (human) | IC50 | 36.0000 | 1 | 1 |
| norverapamil | Homo sapiens (human) | Ki | 4.5300 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | Ki | 0.0220 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Ki | 37.6000 | 1 | 1 |
| ritonavir | Homo sapiens (human) | Ki | 0.1200 | 1 | 1 |
| tacrolimus | Homo sapiens (human) | IC50 | 0.3850 | 2 | 2 |
| ketoconazole | Homo sapiens (human) | IC50 | 0.2535 | 5 | 5 |
| cannabidiol | Homo sapiens (human) | Ki | 0.1900 | 1 | 1 |
| sirtinol | Homo sapiens (human) | IC50 | 194.0000 | 1 | 1 |
| cyclosporine | Homo sapiens (human) | IC50 | 2.0600 | 1 | 1 |
| cyclosporine | Homo sapiens (human) | Ki | 7.6000 | 1 | 2 |
| geldanamycin | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| bergamottin | Homo sapiens (human) | Ki | 20.0000 | 1 | 1 |
| (3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| belinostat | Homo sapiens (human) | IC50 | 0.2147 | 1 | 1 |
| panobinostat | Homo sapiens (human) | IC50 | 0.0033 | 1 | 1 |
| bufalin | Homo sapiens (human) | IC50 | 2.7600 | 1 | 1 |
| mgl-3196 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| kaf156 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| teriflunomide | Homo sapiens (human) | IC50 | 0.3000 | 1 | 2 |
| azd3759 | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dysJournal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| monooxygenase activity | molecular function | Catalysis of the incorporation of one atom from molecular oxygen into a compound and the reduction of the other atom of oxygen to water. [ISBN:0198506732] |
| iron ion binding | molecular function | Binding to an iron (Fe) ion. [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| retinoic acid 4-hydroxylase activity | molecular function | Catalysis of the conversion of retinoic acid to 4-hydroxy-retinoic acid. [PMID:19519282, PMID:9250660] |
| oxidoreductase activity | molecular function | Catalysis of an oxidation-reduction (redox) reaction, a reversible chemical reaction in which the oxidation state of an atom or atoms within a molecule is altered. One substrate acts as a hydrogen or electron donor and becomes oxidized, while the other acts as hydrogen or electron acceptor and becomes reduced. [GOC:go_curators] |
| oxygen binding | molecular function | Binding to oxygen (O2). [GOC:jl] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| aromatase activity | molecular function | Catalysis of the reduction of an aliphatic ring to yield an aromatic ring. [GOC:cb] |
| estrogen 16-alpha-hydroxylase activity | molecular function | Catalysis of the reaction: estrogen + donor-H2 + O2 = 16-alpha-hydroxyestrogen + H2O. [GOC:BHF] |
| testosterone 6-beta-hydroxylase activity | molecular function | Catalysis of the reaction: testosterone + donor-H2 + O2 = 6-beta-hydroxytestosterone + H2O. [GOC:ai, PMID:11726664] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| lipid hydroxylation | biological process | The covalent attachment of a hydroxyl group to one or more fatty acids in a lipid. [GOC:hjd, PMID:15658937] |
| xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
| steroid metabolic process | biological process | The chemical reactions and pathways involving steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus. [ISBN:0198547684] |
| estrogen metabolic process | biological process | The chemical reactions and pathways involving estrogens, C18 steroid hormones that can stimulate the development of female sexual characteristics. Also found in plants. [ISBN:0198506732] |
| alkaloid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of alkaloids, nitrogen containing natural products not otherwise classified as peptides, nonprotein amino acids, amines, cyanogenic glycosides, glucosinolates, cofactors, phytohormones or primary metabolites (such as purine or pyrimidine bases). [GOC:lr, ISBN:0122146743] |
| xenobiotic catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| retinol metabolic process | biological process | The chemical reactions and pathways involving retinol, one of the three compounds that makes up vitamin A. [GOC:jl, http://www.indstate.edu/thcme/mwking/vitamins.html, PMID:1924551] |
| retinoic acid metabolic process | biological process | The chemical reactions and pathways involving retinoic acid, one of the three components that makes up vitamin A. [GOC:jl, http://www.indstate.edu/thcme/mwking/vitamins.html] |
| aflatoxin metabolic process | biological process | The chemical reactions and pathways involving aflatoxin, a fungal metabolite found as a contaminant in moldy grains that induces liver cancer. Aflatoxin induces a G to T transversion at codon 249 of p53, leading to its inactivation. Aflatoxin is converted to a chemical carcinogen by P450. [GOC:ai] |
| oxidative demethylation | biological process | The process of removing one or more methyl groups from a molecule, involving the oxidation (i.e. electron loss) of one or more atoms in the substrate. [GOC:BHF, GOC:mah, GOC:rl] |