Compound class:
Synthetic organic
Comment: Compound 25 is a dual agonist of the ligand-activated transcription factors, farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor (PPAR) δ [1] . It was designed to explore the potential of simultaneous activation of peripheral PPARδ-mediated activity and hepatic FXR mechanisms for the treatment of nonalcoholic steatohepatitis (NASH).
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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Bioactivity Comments |
Compound 25 exhibits selectivity for its intended targets compared to related nuclear receptors: at 10 μM compound 25, RARα, RXRα, PPARα, PPARγ and LXRα were activated by only 4% [1]. |
Selectivity at nuclear hormone receptors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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