Target Validation Information
TTD ID T35734
Target Name Soluble epoxide hydrolase (EPHX2)
Type of Target
Clinical trial
Drug Potency against Target 1-(1-Adamantyl)-3-(1-propionylpiperidin-4-yl)urea Drug Info IC50 = 1.2 nM [14]
1-(1-Propionylpiperidin-4-yl)-3-m-tolylurea Drug Info IC50 = 8.7 nM [14]
1-(1-Propionylpiperidin-4-yl)-3-o-tolylurea Drug Info IC50 = 1700 nM [14]
1-(1-Propionylpiperidin-4-yl)-3-p-tolylurea Drug Info IC50 = 55 nM [14]
1-(3-(3-morpholinopropoxy)phenyl)-3-phenylurea Drug Info IC50 = 38 nM [8]
1-(3-Chloro-phenyl)-3-(4-hydroxy-decyl)-urea Drug Info IC50 = 3100 nM [1]
1-(3-Chloro-phenyl)-3-cyclohexyl-urea Drug Info IC50 = 190 nM [1]
1-(4-(3-morpholinopropoxy)phenyl)-3-phenylurea Drug Info IC50 = 39 nM [8]
1-adamantan-1-yl-3-((R)-1-phenyl-ethyl)-urea Drug Info IC50 = 100 nM [4]
1-adamantan-1-yl-3-(1-benzyl-piperidin-4-yl)-urea Drug Info IC50 = 10 nM [2]
1-adamantan-1-yl-3-(1-butyl-piperidin-4-yl)-urea Drug Info IC50 = 1200 nM [2]
1-adamantan-1-yl-3-(1-ethyl-piperidin-4-yl)-urea Drug Info IC50 = 3800 nM [2]
1-adamantan-1-yl-3-(1-propyl-piperidin-4-yl)-urea Drug Info IC50 = 810 nM [2]
1-adamantan-1-yl-3-(2-heptyloxyethyl)urea Drug Info IC50 = 29 nM [6]
1-Adamantan-1-yl-3-(2-hydroxy-phenyl)-urea Drug Info IC50 = 139 nM [7]
1-adamantan-1-yl-3-(2-hydroxyethyl)urea Drug Info IC50 = 482 nM [6]
1-Adamantan-1-yl-3-(2-methoxy-phenyl)-urea Drug Info IC50 = 8544 nM [7]
1-adamantan-1-yl-3-(3-hexyloxypropyl)urea Drug Info IC50 = 5.6 nM [6]
1-Adamantan-1-yl-3-(3-hydroxy-phenyl)-urea Drug Info IC50 = 28 nM [7]
1-adamantan-1-yl-3-(3-hydroxypropyl)urea Drug Info IC50 = 746 nM [6]
1-Adamantan-1-yl-3-(3-methoxy-phenyl)-urea Drug Info IC50 = 4.7 nM [7]
1-Adamantan-1-yl-3-(4-hydroxy-decyl)-urea Drug Info IC50 = 130 nM [1]
1-Adamantan-1-yl-3-(4-hydroxy-phenyl)-urea Drug Info IC50 = 24 nM [7]
1-adamantan-1-yl-3-(4-hydroxybutyl)urea Drug Info IC50 = 531 nM [6]
1-Adamantan-1-yl-3-(4-methoxy-phenyl)-urea Drug Info IC50 = 14 nM [7]
1-adamantan-1-yl-3-(4-pentyloxybutyl)urea Drug Info IC50 = 4.4 nM [6]
1-adamantan-1-yl-3-(4-pentyloxycylclohexyl)urea Drug Info IC50 = 1.2 nM [6]
1-adamantan-1-yl-3-(5-butoxypentyl)urea Drug Info IC50 = 4.1 nM [6]
1-adamantan-1-yl-3-(5-hydroxypentyl)urea Drug Info IC50 = 84 nM [6]
1-adamantan-1-yl-3-(6-hydroxyhexyl)urea Drug Info IC50 = 12 nM [6]
1-adamantan-1-yl-3-(6-propyloxyhexyl)urea Drug Info IC50 = 3.7 nM [6]
1-Adamantan-1-yl-3-decyl-urea Drug Info IC50 = 110 nM [1]
1-Adamantan-1-yl-3-phenyl-urea Drug Info IC50 = 17 nM [7]
1-adamantan-1-yl-3-piperidin-4-yl-urea Drug Info IC50 = 300 nM [2]
1-adamantan-1-yl-3-piperidin-4-ylmethyl-urea Drug Info IC50 = 4200 nM [2]
1-adamantan-1-yl-3-[4-(4-fluorophenoxy)butyl]urea Drug Info IC50 = 3.9 nM [5]
1-Cycloheptyl-3-(1-propionylpiperidin-4-yl)urea Drug Info IC50 = 0.9 nM [14]
1-Cyclohexyl-3-(1-propionylpiperidin-4-yl)urea Drug Info IC50 = 3.5 nM [14]
1-Cyclohexyl-3-(4-methoxy-phenyl)-urea Drug Info IC50 = 230 nM [1]
1-Cyclohexyl-3-phenethyl-urea Drug Info IC50 = 160 nM [1]
1-Cyclohexyl-3-phenyl-urea Drug Info IC50 = 1390 nM [1]
1-Octyl-3-(1-propionylpiperidin-4-yl)urea Drug Info IC50 = 0.4 nM [14]
1-Phenyl-3-(1-propionylpiperidin-4-yl)urea Drug Info IC50 = 49 nM [14]
12-(3-Adamantan-1-yl-ureido)-dodeca noic acid Drug Info IC50 = 5 nM [9]
12-(3-n-Hexylureido)dodec-8(Z)-enoic acid Drug Info IC50 = 16 nM [10]
12-(3-n-Pentylureidooxy)dodec-8(Z)-enoic acid Drug Info IC50 = 1374 nM [10]
13-(3-n-Pentylthioureido)tridec-8(Z)-enoic Acid Drug Info IC50 = 770 nM [10]
13-(3-n-Pentylureido)tridec-5(Z)-enoic acid Drug Info IC50 = 793 nM [10]
13-(3-n-Pentylureido)tridec-8(E)-enoic acid Drug Info IC50 = 48.5 nM [10]
13-(3-n-Pentylureido)tridec-8-ynoic acid Drug Info IC50 = 43 nM [10]
13-(3-Pentyluredo)tridec-8(Z)-enoic acid Drug Info IC50 = 46 nM [10]
13-(5-n-Pentylfuran-2-yl)tridec-8(Z)-enoic acid Drug Info IC50 = 7147 nM [10]
13-(N-Isopropylheptanamido)tridec-8(Z)-enoic acid Drug Info IC50 = 10712 nM [10]
13-(N-Methyl-n-heptnamido)tridec-8(Z)-enoic acid Drug Info IC50 = 11194 nM [10]
13-(n-Pentylcarbamoyloxy)tridec-8(Z)-enoic acid Drug Info IC50 = 3480 nM [10]
13-n-Heptanamidotridec-5-ynoic acid Drug Info IC50 = 272 nM [10]
13-n-Heptanamidotridec-8(Z)-enoic acid Drug Info IC50 = 79 nM [10]
14-(n-Hexylamino)-14-oxotetradec-8(Z)-enoic acid Drug Info IC50 = 66 nM [10]
16-(3-Ethylureido)hexadec-11(Z)-enoic acid Drug Info IC50 = 2596 nM [10]
2-Adamantan-1-yl-N-decyl-acetamide Drug Info IC50 = 100 nM [1]
2-Cyclohexyl-N-(4-methoxy-phenyl)-acetamide Drug Info IC50 = 6200 nM [1]
2-Cyclohexyl-N-phenethyl-acetamide Drug Info IC50 = 4000 nM [1]
2-Cyclohexyl-N-phenyl-acetamide Drug Info IC50 = 16000 nM [1]
3-(3-Adamantan-1-yl-ureido)-benzoic acid Drug Info IC50 = 365 nM [7]
4,4-Diphenyl-N-(pyridin-3-yl)-butyramide Drug Info IC50 = 18 nM [12]
4-(3-Adamantan-1-yl-ureido)-benzoic acid Drug Info IC50 = 1411 nM [7]
4-(3-cyclohexylureido)butanoic acid Drug Info IC50 = 1900 nM [3]
6-amino-N-(2,4-dichlorobenzyl)nicotinamide Drug Info IC50 = 430 nM [13]
6-amino-N-(3,3-diphenylpropyl)nicotinamide Drug Info IC50 = 8.5 nM [13]
9-(3-n-Pentylureido)non-4(Z)-enoic acid Drug Info IC50 = 1355 nM [10]
9-(3-n-Pentylureido)non-4-ynoic acid Drug Info IC50 = 8110 nM [10]
AR9281 Drug Info IC50 = 6 nM [5]
Cis-1-adamantan-1-yl-3-(4-hydroxycyclohexyl)urea Drug Info IC50 = 76 nM [5]
Cis-1-adamantan-1-yl-3-(4-methoxycyclohexyl)urea Drug Info IC50 = 4 nM [5]
Dodecanoic acid adamantan-1-ylamide Drug Info IC50 = 5000 nM [1]
Methyl 14-(3-n-butylureido)tetradec-8(Z)-enoate Drug Info IC50 = 152 nM [10]
Methyl 4-(3-cyclohexylureido)butanoate Drug Info IC50 = 330 nM [3]
Methyl 6-(3-cyclohexylureido)hexanoate Drug Info IC50 = 110 nM [3]
N,N'-dicyclohexyl-urea Drug Info IC50 = 52 nM [5]
N-(3,3-Diphenyl-propyl)-2-pyridine-3-ylacetamide Drug Info IC50 = 150 nM [12]
N-(3,3-Diphenyl-propyl)-isonicotinamide Drug Info IC50 = 7.6 nM [12]
N-(3,3-diphenyl-propyl)-nicotinamide Drug Info IC50 = 4.8 nM [12]
N-(3-Chloro-phenyl)-2-cyclohexyl-acetamide Drug Info IC50 = 2100 nM [1]
N-(3-Phenyl-propyl)-nicotinamide Drug Info IC50 = 70 nM [12]
N-(4,4-Diphenyl-butyl)-nicotinamide Drug Info IC50 = 26 nM [12]
N-(biphenyl-3-yl)benzo[d]isoxazol-3-amine Drug Info IC50 = 960 nM [11]
N-(biphenyl-4-yl)benzo[d]isoxazol-3-amine Drug Info IC50 = 740 nM [11]
N-(naphthalen-1-yl)benzo[d]isoxazol-3-amine Drug Info IC50 = 4600 nM [11]
N-(naphthalen-2-yl)benzo[d]isoxazol-3-amine Drug Info IC50 = 1200 nM [11]
N-adamantyl-N'-cyclohexylurea Drug Info IC50 = 1.6 nM [5]
N-benzyl-6-(3,3,3-trifluoropropoxy)nicotinamide Drug Info IC50 = 50 nM [13]
N-Cyclohexyl-2-(4-methoxy-phenyl)-acetamide Drug Info IC50 = 4800 nM [1]
N-Cyclohexyl-2-phenyl-acetamide Drug Info IC50 = 14000 nM [1]
N-Cyclohexyl-4-phenyl-butyramide Drug Info IC50 = 1400 nM [1]
N-[3,3-Bis-(4-fluorophenyl)-propyl]-benzamide Drug Info IC50 = 7.2 nM [12]
N-[3,3-Bis-(4-fluorophenyl)-propyl]-nicotinamide Drug Info IC50 = 7 nM [12]
Trans,trans-1,3-bis-(4-hydroxycyclohexyl)urea Drug Info IC50 = 1400 nM [5]
[4-(3-Adamantan-1-yl-ureido)-phenyl]-acetic acid Drug Info IC50 = 392 nM [7]
References
REF 1 Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility. J Med Chem. 2005 May 19;48(10):3621-9.
REF 2 Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5212-6.
REF 3 Peptidyl-urea based inhibitors of soluble epoxide hydrolases. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5439-44.
REF 4 Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5773-7.
REF 5 Orally bioavailable potent soluble epoxide hydrolase inhibitors. J Med Chem. 2007 Aug 9;50(16):3825-40.
REF 6 1,3-disubstituted ureas functionalized with ether groups are potent inhibitors of the soluble epoxide hydrolase with improved pharmacokinetic prope... J Med Chem. 2007 Oct 18;50(21):5217-26.
REF 7 Salicylate-urea-based soluble epoxide hydrolase inhibitors with high metabolic and chemical stabilities. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1784-9.
REF 8 Unsymmetrical non-adamantyl N,N'-diaryl urea and amide inhibitors of soluble expoxide hydrolase. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4259-63.
REF 9 Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement. J Med Chem. 2009 Aug 27;52(16):5009-12.
REF 10 14,15-Epoxyeicosa-5,8,11-trienoic acid (14,15-EET) surrogates containing epoxide bioisosteres: influence upon vascular relaxation and soluble epoxi... J Med Chem. 2009 Aug 27;52(16):5069-75.
REF 11 A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5716-21.
REF 12 Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase. J Med Chem. 2009 Oct 8;52(19):5880-95.
REF 13 Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5864-8.
REF 14 1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, a... J Med Chem. 2010 Oct 14;53(19):7067-75.

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