Synonyms: example 36 [US20120053150A1] | GSK7975A
Compound class:
Synthetic organic
Comment: GSK-7975A was designed as a calcium-release activated calcium (CRAC) channel inhibitor [2]. The structure is claimed as Example 36 in Glaxo patent US20120053150A1 [1]. GSK-7975A inhibits (blocks) the Orai1 component of the CRAC channel complex [4].
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 |
GSK-7975A completely inhibits calcium influx through CRAC channels in vitro [2]. GSK-7975A was used to show that CRAC channel activity is essential for mast cell and T cell function. The rat channel displays a similar pharmacology to human CRAC channels, so this compound is suitable for in vivo rat studies with translational potential to human. |
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