Page last updated: 2024-08-07 18:31:31
Cytochrome P450 2B6
A cytochrome P450 2B6 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P20813]
Synonyms
EC 1.14.13.-;
1,4-cineole 2-exo-monooxygenase;
CYPIIB6;
Cytochrome P450 IIB1
Research
Bioassay Publications (45)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 6 (13.33) | 29.6817 |
| 2010's | 29 (64.44) | 24.3611 |
| 2020's | 10 (22.22) | 2.80 |
Compounds (57)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| acetazolamide | Homo sapiens (human) | Ki | 0.0398 | 2 | 4 |
| alosetron | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| beta-naphthoflavone | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| cannabinol | Homo sapiens (human) | Ki | 20.7750 | 2 | 2 |
| methadone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| thiotepa | Homo sapiens (human) | Ki | 26.1000 | 2 | 2 |
| ticlopidine | Homo sapiens (human) | IC50 | 0.4050 | 2 | 2 |
| ticlopidine | Homo sapiens (human) | Ki | 0.8000 | 1 | 2 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 0.8500 | 2 | 2 |
| phencyclidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2,2-dimethylbutyric acid | Homo sapiens (human) | IC50 | 10,000.0000 | 2 | 2 |
| alpha-naphthoflavone | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| tranylcypromine | Homo sapiens (human) | IC50 | 9.8400 | 3 | 4 |
| nitrogenase stabilizing-protective protein, bacteria | Homo sapiens (human) | GI50 | 1.8000 | 1 | 3 |
| clopidogrel | Homo sapiens (human) | Ki | 1.1000 | 1 | 1 |
| proadifen hydrochloride | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
| pirlindole | Homo sapiens (human) | IC50 | 36.0000 | 1 | 1 |
| voriconazole | Homo sapiens (human) | IC50 | 12.2000 | 1 | 1 |
| 6-paradol | Homo sapiens (human) | IC50 | 6.2000 | 1 | 1 |
| tazobactam | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| tariquidar | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pumosetrag | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | Ki | 0.0218 | 2 | 5 |
| anidulafungin | Homo sapiens (human) | IC50 | 17.5000 | 1 | 1 |
| atorvastatin calcium | Homo sapiens (human) | Ki | 1.2000 | 1 | 1 |
| bay 57-1293 | Homo sapiens (human) | Ki | 0.2350 | 2 | 4 |
| cannabidiol | Homo sapiens (human) | Ki | 0.6900 | 1 | 1 |
| tamoxifen | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 0 |
| clavulanic acid | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| guttiferone e | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| bergamottin | Homo sapiens (human) | Ki | 5.2000 | 1 | 1 |
| opc-67683 | Homo sapiens (human) | IC50 | 100.0000 | 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 | 0.0340 | 1 | 1 |
| orteronel | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| gw 803430 | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| phenobarbital sodium | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
| phenobarbital sodium | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| 6-(3-hydroxyphenyl)-2-naphthol | Homo sapiens (human) | IC50 | 13.4000 | 1 | 1 |
| artenimol | Homo sapiens (human) | IC50 | 125.0000 | 1 | 1 |
| bms-626529 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| cannabidivarin | Homo sapiens (human) | IC50 | 7.4000 | 1 | 1 |
| cannabidivarin | Homo sapiens (human) | Ki | 1.3000 | 1 | 1 |
| dihydrotetrabenazine, (2alpha,3beta,11bbeta)-isomer | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| buparlisib | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 5.6005 | 2 | 2 |
| e-52862 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| glpg0634 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| kaf156 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| (5s,6s,9r)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta(b)pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxylate | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| onc201 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd3759 | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| 2-[(4-chlorophenyl)methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 4-[[(4-oxo-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)thio]methyl]benzoic acid methyl ester | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| carbamazepine | Homo sapiens (human) | EC50 | 145.0000 | 1 | 1 |
| rifampin | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
Drugs with Other Measurements
[no title available]Journal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.Current drug metabolism, , Volume: 6, Issue:5, 2005
Development of Robust 17(Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseaseJournal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 28, Issue:21, 2018
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in cJournal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Enables
This protein enables 11 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] |
| testosterone 16-alpha-hydroxylase activity | molecular function | Catalysis of the reaction: testosterone + donor-H2 + O2 = 16-alpha-hydroxytestosterone + H2O. [GOC:ai] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| testosterone 16-beta-hydroxylase activity | molecular function | Catalysis of the reaction: O2 + reduced [NADPH--hemoprotein reductase] + testosterone = 16beta,17beta-dihydroxyandrost-4-en-3-one + H+ + H2O + oxidized [NADPH--hemoprotein reductase]. [PMID:21289075, RHEA:46304] |
| anandamide 8,9 epoxidase activity | molecular function | Catalysis of the reaction: N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine + O2 + reduced [NADPH--hemoprotein reductase] = H+ + H2O + N-(8,9-epoxy-5Z,11Z,14Z-eicosatrienoyl)-ethanolamine + oxidized [NADPH--hemoprotein reductase]. [PMID:21289075, RHEA:53140] |
| anandamide 11,12 epoxidase activity | molecular function | Catalysis of the reaction: N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine + O2 + reduced [NADPH--hemoprotein reductase] = H+ + H2O + N-(11,12-epoxy-5Z,8Z,14Z-eicosatrienoyl)-ethanolamine + oxidized [NADPH--hemoprotein reductase]. [PMID:21289075, RHEA:53144] |
| anandamide 14,15 epoxidase activity | molecular function | Catalysis of the reaction: N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine + O2 + reduced [NADPH--hemoprotein reductase] = H+ + H2O + N-(14,15-epoxy-5Z,8Z,11Z-eicosatrienoyl)-ethanolamine + oxidized [NADPH--hemoprotein reductase]. [PMID:21289075, RHEA:53148] |
| estrogen 2-hydroxylase activity | molecular function | Catalysis of the reaction: estrogen + donor-H2 + O2 = 2-hydroxyestrogen + H2O. [GOC:BHF, GOC:rl, PMID:14559847] |
| 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 | molecular function | Catalysis of an oxidation-reduction (redox) reaction in which hydrogen or electrons are transferred from reduced flavin or flavoprotein and one other donor, and one atom of oxygen is incorporated into one donor. [GOC:mah] |
| arachidonic acid epoxygenase activity | molecular function | Catalysis of an NADPH- and oxygen-dependent reaction that converts arachidonic acid to a cis-epoxyeicosatrienoic acid. [http://lipidlibrary.aocs.org/Lipids/eic_hete/index.htm, PMID:10681399, PMID:18952572] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| cellular ketone metabolic process | biological process | The chemical reactions and pathways involving any of a class of organic compounds that contain the carbonyl group, CO, and in which the carbonyl group is bonded only to carbon atoms, as carried out by individual cells. The general formula for a ketone is RCOR, where R and R are alkyl or aryl groups. [GOC:jl, ISBN:0787650153] |
| epoxygenase P450 pathway | biological process | The chemical reactions and pathways by which arachidonic acid is converted to other compounds including epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids. [GOC:mah, PMID:17979511] |