Target Information

Target General Infomation
Target ID
T35734
Former ID
TTDR01203
Target Name
Soluble epoxide hydrolase
Gene Name
EPHX2
Synonyms
CEH; Cytosolic epoxide hydrolase; Epoxide Hydrolase; Epoxide hydratase; SEH; EPHX2
Target Type
Clinical Trial
Disease Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Hypertension [ICD9: 401; ICD10: I10-I16]
Function
This enzyme acts on epoxides (alkene oxides, oxiranes) and arene oxides. plays a role in xenobiotic metabolism by degrading potential toxic epoxides. also determines steady- state levels of physiological mediators.
BioChemical Class
Etherhydrolase
Target Validation
T35734
UniProt ID
P34913
EC Number
EC 3.1.3.76
Sequence
MTLRAAVFDLDGVLALPAVFGVLGRTEEALALPRGLLNDAFQKGGPEGATTRLMKGEITL
SQWIPLMEENCRKCSETAKVCLPKNFSIKEIFDKAISARKINRPMLQAALMLRKKGFTTA
ILTNTWLDDRAERDGLAQLMCELKMHFDFLIESCQVGMVKPEPQIYKFLLDTLKASPSEV
VFLDDIGANLKPARDLGMVTILVQDTDTALKELEKVTGIQLLNTPAPLPTSCNPSDMSHG
YVTVKPRVRLHFVELGSGPAVCLCHGFPESWYSWRYQIPALAQAGYRVLAMDMKGYGESS
APPEIEEYCMEVLCKEMVTFLDKLGLSQAVFIGHDWGGMLVWYMALFYPERVRAVASLNT
PFIPANPNMSPLESIKANPVFDYQLYFQEPGVAEAELEQNLSRTFKSLFRASDESVLSMH
KVCEAGGLFVNSPEEPSLSRMVTEEEIQFYVQQFKKSGFRGPLNWYRNMERNWKWACKSL
GRKILIPALMVTAEKDFVLVPQMSQHMEDWIPHLKRGHIEDCGHWTQMDKPTEVNQILIK
WLDSDARNPPVVSKM
Drugs and Mode of Action
Drug(s) GSK2256294 Drug Info Phase 1 Chronic obstructive pulmonary disease [532153]
Inhibitor 1,3-DIPHENYLUREA Drug Info [551374]
1-(1-Adamantyl)-3-(1-propionylpiperidin-4-yl)urea Drug Info [531143]
1-(1-Propionylpiperidin-4-yl)-3-m-tolylurea Drug Info [531143]
1-(1-Propionylpiperidin-4-yl)-3-o-tolylurea Drug Info [531143]
1-(1-Propionylpiperidin-4-yl)-3-p-tolylurea Drug Info [531143]
1-(3-(3-morpholinopropoxy)phenyl)-3-phenylurea Drug Info [530204]
1-(3-Chloro-phenyl)-3-(4-hydroxy-decyl)-urea Drug Info [527552]
1-(3-Chloro-phenyl)-3-cyclohexyl-urea Drug Info [527552]
1-(4-(3-morpholinopropoxy)phenyl)-3-phenylurea Drug Info [530204]
1-adamantan-1-yl-3-((R)-1-phenyl-ethyl)-urea Drug Info [528417]
1-adamantan-1-yl-3-(1-benzyl-piperidin-4-yl)-urea Drug Info [528339]
1-adamantan-1-yl-3-(1-butyl-piperidin-4-yl)-urea Drug Info [528339]
1-adamantan-1-yl-3-(1-ethyl-piperidin-4-yl)-urea Drug Info [528339]
1-adamantan-1-yl-3-(1-propyl-piperidin-4-yl)-urea Drug Info [528339]
1-adamantan-1-yl-3-(2-heptyloxyethyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-(2-hydroxy-phenyl)-urea Drug Info [529961]
1-adamantan-1-yl-3-(2-hydroxyethyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-(2-methoxy-phenyl)-urea Drug Info [529961]
1-adamantan-1-yl-3-(3-hexyloxypropyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-(3-hydroxy-phenyl)-urea Drug Info [529961]
1-adamantan-1-yl-3-(3-hydroxypropyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-(3-methoxy-phenyl)-urea Drug Info [529961]
1-Adamantan-1-yl-3-(4-hydroxy-decyl)-urea Drug Info [527552]
1-Adamantan-1-yl-3-(4-hydroxy-phenyl)-urea Drug Info [529961]
1-adamantan-1-yl-3-(4-hydroxybutyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-(4-methoxy-phenyl)-urea Drug Info [529961]
1-adamantan-1-yl-3-(4-pentyloxybutyl)urea Drug Info [529063]
1-adamantan-1-yl-3-(4-pentyloxycylclohexyl)urea Drug Info [529063]
1-adamantan-1-yl-3-(5-butoxypentyl)urea Drug Info [529063]
1-adamantan-1-yl-3-(5-hydroxypentyl)urea Drug Info [529063]
1-adamantan-1-yl-3-(6-hydroxyhexyl)urea Drug Info [529063]
1-adamantan-1-yl-3-(6-propyloxyhexyl)urea Drug Info [529063]
1-Adamantan-1-yl-3-decyl-urea Drug Info [527552]
1-Adamantan-1-yl-3-phenyl-urea Drug Info [529961]
1-adamantan-1-yl-3-piperidin-4-yl-urea Drug Info [528339]
1-adamantan-1-yl-3-piperidin-4-ylmethyl-urea Drug Info [528339]
1-adamantan-1-yl-3-[4-(4-fluorophenoxy)butyl]urea Drug Info [528938]
1-Cycloheptyl-3-(1-propionylpiperidin-4-yl)urea Drug Info [531143]
1-Cyclohexyl-3-(1-propionylpiperidin-4-yl)urea Drug Info [531143]
1-Cyclohexyl-3-(4-methoxy-phenyl)-urea Drug Info [527552]
1-Cyclohexyl-3-phenethyl-urea Drug Info [527552]
1-Cyclohexyl-3-phenyl-urea Drug Info [527552]
1-Octyl-3-(1-propionylpiperidin-4-yl)urea Drug Info [531143]
1-Phenyl-3-(1-propionylpiperidin-4-yl)urea Drug Info [531143]
12-(3-Adamantan-1-yl-ureido)-dodeca noic acid Drug Info [530286]
12-(3-n-Hexylureido)dodec-8(Z)-enoic acid Drug Info [530294]
12-(3-n-Pentylureidooxy)dodec-8(Z)-enoic acid Drug Info [530294]
13-(3-n-Pentylthioureido)tridec-8(Z)-enoic Acid Drug Info [530294]
13-(3-n-Pentylureido)tridec-5(Z)-enoic acid Drug Info [530294]
13-(3-n-Pentylureido)tridec-8(E)-enoic acid Drug Info [530294]
13-(3-n-Pentylureido)tridec-8-ynoic acid Drug Info [530294]
13-(3-Pentyluredo)tridec-8(Z)-enoic acid Drug Info [530294]
13-(5-n-Pentylfuran-2-yl)tridec-8(Z)-enoic acid Drug Info [530294]
13-(N-Isopropylheptanamido)tridec-8(Z)-enoic acid Drug Info [530294]
13-(N-Methyl-n-heptnamido)tridec-8(Z)-enoic acid Drug Info [530294]
13-(n-Pentylcarbamoyloxy)tridec-8(Z)-enoic acid Drug Info [530294]
13-n-Heptanamidotridec-5-ynoic acid Drug Info [530294]
13-n-Heptanamidotridec-8(Z)-enoic acid Drug Info [530294]
14-(n-Hexylamino)-14-oxotetradec-8(Z)-enoic acid Drug Info [530294]
16-(3-Ethylureido)hexadec-11(Z)-enoic acid Drug Info [530294]
2-Adamantan-1-yl-N-decyl-acetamide Drug Info [527552]
2-Cyclohexyl-N-(4-methoxy-phenyl)-acetamide Drug Info [527552]
2-Cyclohexyl-N-phenethyl-acetamide Drug Info [527552]
2-Cyclohexyl-N-phenyl-acetamide Drug Info [527552]
3-(3-Adamantan-1-yl-ureido)-benzoic acid Drug Info [529961]
4,4-Diphenyl-N-(pyridin-3-yl)-butyramide Drug Info [530375]
4-(3-Adamantan-1-yl-ureido)-benzoic acid Drug Info [529961]
4-(3-cyclohexylureido)butanoic acid Drug Info [528366]
4-{[(CYCLOHEXYLAMINO)CARBONYL]AMINO}BUTANOIC ACID Drug Info [551374]
6-amino-N-(2,4-dichlorobenzyl)nicotinamide Drug Info [530386]
6-amino-N-(3,3-diphenylpropyl)nicotinamide Drug Info [530386]
6-{[(CYCLOHEXYLAMINO)CARBONYL]AMINO}HEXANOIC ACID Drug Info [551374]
9-(3-n-Pentylureido)non-4(Z)-enoic acid Drug Info [530294]
9-(3-n-Pentylureido)non-4-ynoic acid Drug Info [530294]
Cis-1-adamantan-1-yl-3-(4-hydroxycyclohexyl)urea Drug Info [528938]
Cis-1-adamantan-1-yl-3-(4-methoxycyclohexyl)urea Drug Info [528938]
Dodecanoic acid adamantan-1-ylamide Drug Info [527552]
EXRD-4605 Drug Info [532153]
Methyl 14-(3-n-butylureido)tetradec-8(Z)-enoate Drug Info [530294]
Methyl 4-(3-cyclohexylureido)butanoate Drug Info [528366]
Methyl 6-(3-cyclohexylureido)hexanoate Drug Info [528366]
N,N'-dicyclohexyl-urea Drug Info [528938]
N-(1-acetylpiperidin-4-yl)-N'-(adamant-1-yl)urea Drug Info [528938]
N-(3,3-Diphenyl-propyl)-2-pyridine-3-ylacetamide Drug Info [530375]
N-(3,3-Diphenyl-propyl)-isonicotinamide Drug Info [530375]
N-(3,3-diphenyl-propyl)-nicotinamide Drug Info [530375]
N-(3-Chloro-phenyl)-2-cyclohexyl-acetamide Drug Info [527552]
N-(3-Phenyl-propyl)-nicotinamide Drug Info [530375]
N-(4,4-Diphenyl-butyl)-nicotinamide Drug Info [530375]
N-(biphenyl-3-yl)benzo[d]isoxazol-3-amine Drug Info [530329]
N-(biphenyl-4-yl)benzo[d]isoxazol-3-amine Drug Info [530329]
N-(naphthalen-1-yl)benzo[d]isoxazol-3-amine Drug Info [530329]
N-(naphthalen-2-yl)benzo[d]isoxazol-3-amine Drug Info [530329]
N-adamantyl-N'-cyclohexylurea Drug Info [528938]
N-benzyl-6-(3,3,3-trifluoropropoxy)nicotinamide Drug Info [530386]
N-Cyclohexyl-2-(4-methoxy-phenyl)-acetamide Drug Info [527552]
N-Cyclohexyl-2-phenyl-acetamide Drug Info [527552]
N-Cyclohexyl-4-phenyl-butyramide Drug Info [527552]
N-Cyclohexyl-N'-(4-Iodophenyl)Urea Drug Info [551393]
N-Cyclohexyl-N'-(Propyl)Phenyl Urea Drug Info [551374]
N-Cyclohexyl-N'-Decylurea Drug Info [551374]
N-[(CYCLOHEXYLAMINO)CARBONYL]GLYCINE Drug Info [551374]
N-[3,3-Bis-(4-fluorophenyl)-propyl]-benzamide Drug Info [530375]
N-[3,3-Bis-(4-fluorophenyl)-propyl]-nicotinamide Drug Info [530375]
SEH inhibitors Drug Info [532153]
Trans,trans-1,3-bis-(4-hydroxycyclohexyl)urea Drug Info [528938]
[4-(3-Adamantan-1-yl-ureido)-phenyl]-acetic acid Drug Info [529961]
Modulator GSK2256294 Drug Info [532153], [532245]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Arachidonic acid metabolism
Metabolic pathways
Peroxisome
PathWhiz Pathway Arachidonic Acid Metabolism
WikiPathways Metapathway biotransformation
Arachidonate Epoxygenase / Epoxide Hydrolase
Arachidonic acid metabolism
References
Ref 532153Soluble epoxide hydrolase inhibition does not prevent cardiac remodeling and dysfunction after aortic constriction in rats and mice. J Cardiovasc Pharmacol. 2013 Apr;61(4):291-301.
Ref 527552J Med Chem. 2005 May 19;48(10):3621-9.Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility.
Ref 528339Bioorg Med Chem Lett. 2006 Oct 1;16(19):5212-6. Epub 2006 Jul 25.Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase.
Ref 528366Bioorg Med Chem Lett. 2006 Oct 15;16(20):5439-44.Peptidyl-urea based inhibitors of soluble epoxide hydrolases.
Ref 528417Bioorg Med Chem Lett. 2006 Nov 15;16(22):5773-7. Epub 2006 Sep 1.Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors.
Ref 528938J Med Chem. 2007 Aug 9;50(16):3825-40. Epub 2007 Jul 6.Orally bioavailable potent soluble epoxide hydrolase inhibitors.
Ref 529063J Med Chem. 2007 Oct 18;50(21):5217-26. Epub 2007 Sep 26.1,3-disubstituted ureas functionalized with ether groups are potent inhibitors of the soluble epoxide hydrolase with improved pharmacokineticproperties.
Ref 529961Bioorg Med Chem Lett. 2009 Mar 15;19(6):1784-9. Epub 2009 Jan 27.Salicylate-urea-based soluble epoxide hydrolase inhibitors with high metabolic and chemical stabilities.
Ref 530204Bioorg Med Chem Lett. 2009 Aug 1;19(15):4259-63. Epub 2009 May 30.Unsymmetrical non-adamantyl N,N'-diaryl urea and amide inhibitors of soluble expoxide hydrolase.
Ref 530286J Med Chem. 2009 Aug 27;52(16):5009-12.Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Ref 530294J Med Chem. 2009 Aug 27;52(16):5069-75.14,15-Epoxyeicosa-5,8,11-trienoic acid (14,15-EET) surrogates containing epoxide bioisosteres: influence upon vascular relaxation and soluble epoxide hydrolase inhibition.
Ref 530329Bioorg Med Chem Lett. 2009 Oct 1;19(19):5716-21. Epub 2009 Aug 7.A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.
Ref 530375J Med Chem. 2009 Oct 8;52(19):5880-95.Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase.
Ref 530386Bioorg Med Chem Lett. 2009 Oct 15;19(20):5864-8. Epub 2009 Aug 26.Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase.
Ref 531143J Med Chem. 2010 Oct 14;53(19):7067-75.1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain.
Ref 532153Soluble epoxide hydrolase inhibition does not prevent cardiac remodeling and dysfunction after aortic constriction in rats and mice. J Cardiovasc Pharmacol. 2013 Apr;61(4):291-301.
Ref 532245In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013 Jul-Aug;104-105:25-31.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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