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 [3], claimed in patent WO2014023643 [1]. The compound series developed by Migliore et al. (2015) [3] 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 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. ✖ |
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No information available. |
Mechanism Of Action and Pharmacodynamic Effects ![]() |
FAAH catalyzes the hydrolysis of anandamide, generating arachidonic acid (AA), which is the substrate of COX. Multi-targeted agents that simultaneously act to inhibit FAAH and COX are being investigated as novel anti-inflammatory therapeutics for the treatment of pain [4]. Concomitant inhibition of FAAH and COX enhances the analgesic effect of NSAIDs ('coxibs') [2], and in addition FAAH inhibition reduces the adverse gastrointestinal side effects caused by COX inhibition [5]. |