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Synonyms: compound (+)-10r [PMID: 26774927] | example 20 [WO2014023643]
Compound class: Synthetic organic
Comment: (S)-ARN2508 is a dual inhibitor of fatty acid amide hydrolase (FAAH) and COX enzyme activities , claimed in patent WO2014023643 . The compound series developed by Migliore et al. (2015)  is based on a hybrid scaffold combining structural motifs of the FAAH inhibitor URB597 and the COX inhibitor flurbiprofen. From this series, the (S) enantiomer was found to inhibit both enzymes, whereas the (R) enantiomer ((R)-ARN2508) only inhibited FAAH.
Ligand Activity Visualisation Charts
These 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.✖
1. DE Vivi M, Scaparelli R, Cavalli A, Migliore M, Piomelli D, Habrant D, Favia. (2014)
Multitarget FAAH and COX inhibitors and therapeutical uses thereof.
Patent number: WO2014023643 A1. Assignee: Fondazione Istituto Italiano Di Tecnologia. Priority date: 06/08/2012. Publication date: 13/02/2014.
2. Grim TW, Ghosh S, Hsu KL, Cravatt BF, Kinsey SG, Lichtman AH. (2014)
Combined inhibition of FAAH and COX produces enhanced anti-allodynic effects in mouse neuropathic and inflammatory pain models.
Pharmacol. Biochem. Behav., 124: 405-11. [PMID:25058512]
3. Migliore M, Habrant D, Sasso O, Albani C, Bertozzi SM, Armirotti A, Piomelli D, Scarpelli R. (2016)
Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.
Eur J Med Chem, 109: 216-37. [PMID:26774927]
4. Palermo G, Favia AD, Convertino M, De Vivo M. (2016)
The Molecular Basis for Dual Fatty Acid Amide Hydrolase (FAAH)/Cyclooxygenase (COX) Inhibition.
ChemMedChem, 11 (12): 1252-8. [PMID:26593700]
5. Sasso O, Migliore M, Habrant D, Armirotti A, Albani C, Summa M, Moreno-Sanz G, Scarpelli R, Piomelli D. (2015)
Multitarget fatty acid amide hydrolase/cyclooxygenase blockade suppresses intestinal inflammation and protects against nonsteroidal anti-inflammatory drug-dependent gastrointestinal damage.
FASEB J., 29 (6): 2616-27. [PMID:25757568]