Synonyms: TAK-242 | TAK242
Compound class:
Synthetic organic
Comment: Resatorvid (TAK242) was first identified as an inhibitor of inflammatory mediator production in LPS treated mouse macrophages [2]. Subsequent work found that this action was attributable to the compound's activity as a Toll-like receptor 4 (TLR4) antagonist [1].
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 |
In vitro, resatorvid inhibits cytokine production in human PBMCs without antagonizing the binding of LPS to the CD14/TLR4/MD-2 complex [1]. Resatorvid inhibits cytokine production from mouse RAW264.7 cells stimulated with various TLR4 agonists, but not TRL2, -3 or -9 agonists, confirming it as a selective TLR4 antagonist [1]. The Ii et al. paper [1] does not provide binding assay-derived data quantifying TLR4-resatorvid antagonism, all confirmatory work involved measuring inhibition of agonist-induced cytokine expression or secretion. We have tagged TLR4 as the primary molecular target for resatorvid based on this study. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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