Synonyms: compound (-)-10r [PMID: 26774927] | example 19 [WO2014023643]
Compound class:
Synthetic organic
Comment: (R)-ARN2508 is an experimental inhibitor of fatty acid amide hydrolase (FAAH) [2], claimed in patent WO2014023643 [1]. The compound series developed by Migliore et al. (2015) [2] is based on a hybrid scaffold combining structural motifs of the FAAH inhibitor URB597 and the COX inhibitor flurbiprofen. The (S) enantiomer ((S)-ARN2508) inhibits both FAAH and COX enzyme activities, whereas this (R) enantiomer only inhibits 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. ✖ |
|
Bioactivity Comments |
When tested, the racemic mixture of (R) and (S) ARN2508 (compound 10r in [2]) gave IC50 values of 31nM for FAAH, 12nM for COX1 and 430nM for COX2 [2]. Note that the (S) enantiomer is the much more potent COX inhibitor, being ~14000 times more potent for COX1 and 1900 times more potent for COX2 than the (R) enantiomer. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|