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rdf:type |
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lifeskim:mentions |
umls-concept:C0014628,
umls-concept:C0205250,
umls-concept:C0425152,
umls-concept:C0935763,
umls-concept:C1521840,
umls-concept:C1551022,
umls-concept:C1657294,
umls-concept:C1749467,
umls-concept:C1880355,
umls-concept:C1961132,
umls-concept:C1961136,
umls-concept:C2348480
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pubmed:issue |
16
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pubmed:dateCreated |
2010-6-21
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pubmed:abstractText |
4-Substituted piperidine-derived trisubstituted ureas are reported as highly potent and selective inhibitors for sEH. The SAR outlines approaches to improve activity against sEH and reduce ion channel and CYP liability. With minimal off-target activity and a good PK profile, the benchmark 2d exhibited remarkable in vitro and ex vivo target engagement. The eutomer entA-2d also elicited vasodilation effect in rat mesenteric artery.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:Alonso-GaliciaMagdalenaM,
pubmed-author:BergerJoel PJP,
pubmed-author:ChenHsuan-ShenHS,
pubmed-author:ChenXiaoliX,
pubmed-author:ChenYuliY,
pubmed-author:CollettiSteven LSL,
pubmed-author:DengQiaolinQ,
pubmed-author:DingFa-XiangFX,
pubmed-author:KumarSanjeevS,
pubmed-author:MitraKaushikK,
pubmed-author:PaiLee-YuhLY,
pubmed-author:RoySophieS,
pubmed-author:ShenHong CHC,
pubmed-author:SoissonStephen MSM,
pubmed-author:StevensonAndra SAS,
pubmed-author:TataJames RJR,
pubmed-author:TongVincentV,
pubmed-author:TongXinchunX,
pubmed-author:TsaiChristineC,
pubmed-author:WangSiyiS,
pubmed-author:XuSuoyuS,
pubmed-author:ZhangBeiB,
pubmed-author:ZhangXiaopingX,
pubmed-author:ZhouGaochaoG
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pubmed:issnType |
Electronic
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pubmed:day |
27
|
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5009-12
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pubmed:meshHeading |
pubmed-meshheading:19645482-Animals,
pubmed-meshheading:19645482-Biological Availability,
pubmed-meshheading:19645482-Cell Line,
pubmed-meshheading:19645482-Crystallography, X-Ray,
pubmed-meshheading:19645482-Cytochrome P-450 Enzyme System,
pubmed-meshheading:19645482-Eicosanoids,
pubmed-meshheading:19645482-Epoxide Hydrolases,
pubmed-meshheading:19645482-Epoxy Compounds,
pubmed-meshheading:19645482-Humans,
pubmed-meshheading:19645482-Ion Channels,
pubmed-meshheading:19645482-Kidney,
pubmed-meshheading:19645482-Mesenteric Arteries,
pubmed-meshheading:19645482-Models, Molecular,
pubmed-meshheading:19645482-Molecular Conformation,
pubmed-meshheading:19645482-Muscle, Smooth, Vascular,
pubmed-meshheading:19645482-Muscle Relaxation,
pubmed-meshheading:19645482-Piperidines,
pubmed-meshheading:19645482-Rats,
pubmed-meshheading:19645482-Rats, Inbred SHR,
pubmed-meshheading:19645482-Solubility,
pubmed-meshheading:19645482-Stereoisomerism,
pubmed-meshheading:19645482-Structure-Activity Relationship,
pubmed-meshheading:19645482-Urea
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
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pubmed:affiliation |
Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA. hong_shen@merck.com
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pubmed:publicationType |
Journal Article,
In Vitro
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