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Synonyms: compound 20 [PMID: 36279149] | GDC2394
Compound class: Synthetic organic
Comment: GDC-2394 is a potent NLRP3 inhibitor . It binds to an allosteric pocket in NLRP3's NACHT domain. GDC-2394 inhibits activated NLRP3 inflammasome-mediated production of IL-1β and IL-18 in vitro (IC50s 16 nM and 17 nM respectively, in human monocyte-derived macrophages), and orally administered GDC-2394 reduces inflammation in animal models.
Ligand Activity Visualisation Charts
These 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.✖
|NLRP3 inhibitors are being exploited as immunomodulators, specifically to reduce inflammation that's driven by IL-1β and IL-18.