Synonyms: AR9281 | compound 14a [PMID: 21211973]
Compound class:
Synthetic organic
Comment: An orally available inhibitor of epoxide hydrolase 2 (a.k.a. soluble epoxide hydrolase or sEH) with in vitro and in vivo efficacy [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Anandan SK, Webb HK, Chen D, Wang YX, Aavula BR, Cases S, Cheng Y, Do ZN, Mehra U, Tran V et al.. (2011)
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. Bioorg Med Chem Lett, 21 (3): 983-8. [PMID:21211973] |
2. Codony S, Pujol E, Pizarro J, Feixas F, Valverde E, Loza MI, Brea JM, Saez E, Oyarzabal J, Pineda-Lucena A et al.. (2020)
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: In Vivo Evaluation in a Murine Model of Acute Pancreatitis. J Med Chem, 63 (17): 9237-9257. [PMID:32787085] |
3. Du F, Sun W, Morisseau C, Hammock BD, Bao X, Liu Q, Wang C, Zhang T, Yang H, Zhou J et al.. (2021)
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis. Eur J Med Chem, 223: 113678. [PMID:34218083] |
4. Jones PD, Tsai HJ, Do ZN, Morisseau C, Hammock BD. (2006)
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase. Bioorg Med Chem Lett, 16 (19): 5212-6. [PMID:16870439] |