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Compound class: Synthetic organic
Comment: BTP2 (YM-58483) is a small molecule store-operated Ca2+ release-activated Ca2+ (CRAC) channel inhibitor .
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.✖
|CRAC channels form a network essential for activation of the adaptive immune response. They are expressed mainly bt non-excitable cells including T-lymphocytes and mast cells. Activation of CRAC channels in the plasma membranes of these cells results in alteration in NFAT-dependent expression of several cytokines including interleukin-2. Inhibition of calcium influx by altering CRAC channel activity has potential as an effective strategy for the treatment of autoimmune and inflammatory diseases, whilst minimising the adverse effects (nephrotoxicity and neurotoxicity) commonly produced by calcineurin inhibitors used as immunosuppressive agents.
CRAC channels have been implicated in the pathogenesis of rheumatoid arthritis (RA), and inhibitors investigated as clinical candidates for this disease, and others . BTP2 (YM-58483) is a CRAC channel inhibitor. However, despite showing some anti-inflammatory activity in RA models, YM-58483 was associated with safety issues including hepatic and renal toxicity, and hyperglycemia in mice .