Proteins > Bifunctional epoxide hydrolase 2
Page last updated: 2024-08-07 18:34:03
Bifunctional epoxide hydrolase 2
An epoxide hydrolase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P34913]
Synonyms
Research
Bioassay Publications (48)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (6.25) | 29.6817 |
| 2010's | 29 (60.42) | 24.3611 |
| 2020's | 16 (33.33) | 2.80 |
Compounds (51)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| t-tucb | Homo sapiens (human) | Km | 200.0000 | 1 | 1 |
Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Stacking with No Planarity?ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
Challenges of docking in large, flexible and promiscuous binding sites.Bioorganic & medicinal chemistry, , 10-15, Volume: 24, Issue:20, 2016
Structural insights into binding of inhibitors to soluble epoxide hydrolase gained by fragment screening and X-ray crystallography.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
Symmetric adamantyl-diureas as soluble epoxide hydrolase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Orally bioavailable potent soluble epoxide hydrolase inhibitors.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
The structure-activity relationship of urea derivatives as anti-tuberculosis agents.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Development of Robust 17(Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Anti-inflammatory components of Euphorbia humifusa Willd.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
From the Design to the Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative.Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 2021
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
1-(1-acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Orally bioavailable potent soluble epoxide hydrolase inhibitors.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 16, Issue:19, 2006
Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 70, 2022
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
From the Design to the Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors.Bioorganic & medicinal chemistry, , 12-01, Volume: 51, 2021
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Multitarget PPARĪ³ agonists as innovative modulators of the metabolic syndrome.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Screening a library of 1600 adamantyl ureas for anti-Mycobacterium tuberculosis activity in vitro and for better physical chemical properties for bioavailability.Bioorganic & medicinal chemistry, , May-15, Volume: 20, Issue:10, 2012
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Orally bioavailable potent soluble epoxide hydrolase inhibitors.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
Bioisosteric substitution of adamantane with bicyclic lipophilic groups improves water solubility of human soluble epoxide hydrolase inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 30, Issue:18, 2020
Imidazolidine-2,4,5- and pirimidine-2,4,6-triones - New primary pharmacophore for soluble epoxide hydrolase inhibitors with enhanced water solubility.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 30, Issue:3, 2020
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
From the Design to the Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
The structure-activity relationship of urea derivatives as anti-tuberculosis agents.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 2022
Design, Synthesis, and Structure-Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
DNA-Encoded Library Screening as Core Platform Technology in Drug Discovery: Its Synthetic Method Development and Applications in DEL Synthesis.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Chemical Space of DNA-Encoded Libraries.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| magnesium ion binding | molecular function | Binding to a magnesium (Mg) ion. [GOC:ai] |
| epoxide hydrolase activity | molecular function | Catalysis of the reaction: an epoxide + H2O = an ethanediol. [EC:3.3.2.10] |
| toxic substance binding | molecular function | Binding to a toxic substance, a poisonous substance that causes damage to biological systems. [GOC:bf, GOC:curators, GOC:jl, GOC:pr] |
| phosphatase activity | molecular function | Catalysis of the hydrolysis of phosphoric monoesters, releasing phosphate ions. [GOC:curators, GOC:pg] |
| 10-hydroxy-9-(phosphonooxy)octadecanoate phosphatase activity | molecular function | Catalysis of the reaction: (9S,10S)-10-hydroxy-9-(phosphonooxy)octadecanoate + H2O = (9S,10S)-9,10-dihydroxyoctadecanoate + phosphate. [EC:3.1.3.76, RHEA:16537] |
| lipid phosphatase activity | molecular function | Catalysis of the reaction: a phospholipid + H2O = a lipid + phosphate. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| lysophosphatidic acid phosphatase activity | molecular function | Catalysis of the reaction: lysophosphatidic acid + H2O = phosphate + monoacylglycerol. [PMID:20045079, PMID:7966317] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
| peroxisomal matrix | cellular component | The volume contained within the membranes of a peroxisome; in many cells the matrix contains a crystalloid core largely composed of urate oxidase. [GOC:curators, ISBN:0815316194] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| response to toxic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a toxic stimulus. [GOC:lr] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| dephosphorylation | biological process | The process of removing one or more phosphoric (ester or anhydride) residues from a molecule. [ISBN:0198506732] |
| cholesterol homeostasis | biological process | Any process involved in the maintenance of an internal steady state of cholesterol within an organism or cell. [GOC:go_curators] |
| stilbene catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of stilbenes, a class of polyketide compounds formed from cinnamic acid and three molecules of malonyl CoA. [GOC:ai] |
| phospholipid dephosphorylation | biological process | The process of removing one or more phosphate groups from a phosphorylated lipid, any member of a group of substances soluble in lipid solvents but only sparingly soluble in aqueous solvents. [ISBN:0198506732] |
| regulation of cholesterol metabolic process | biological process | Any process that modulates the rate, frequency, or extent of cholesterol metabolism, the chemical reactions and pathways involving cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:BHF, GOC:dph, GOC:tb] |
| epoxide metabolic process | biological process | The chemical reactions and pathways involving epoxides, compounds in which an oxygen atom is directly attached to two adjacent or non-adjacent carbon atoms of a carbon chain or ring system; thus cyclic ethers. [GOC:rs, PMID:15822179] |