Compound class:
Synthetic organic
Comment: Triple modulator 10 has been developed as an anti-inflammatory agent with intentionally designed-in polypharamcology [1]. Structurally it is a derivative of the cysteinyl-leukotriene receptor antagonist, anti-asthma drug zafirlukast and its exploits off-target effects of this drug. Triple modulator 10 is a cysteinyl leukotriene receptor 1 (CysLT1R) antagonist, a peroxisome proliferator-activated receptor γ (PPARγ) agonist and a soluble epoxide hydrolase (sEH) inhibitor.
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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Immunopharmacology Comments |
Triple modulator 10 is a derivative of the cysteinyl-leukotriene receptor antagonist, anti-asthma drug zafirlukast [1]. It is rationally designed polypharamcological tool has been designed to simultaneously modulate several proteins that are known to be involved in the complex pathophysiological processes that underlie inflammatory diseases. In doing so, it is hoped that this approach may be used to improve therapeutic efficacy in chronic inflammatory conditions that have proven refractory to current therapies. |