Compound class:
Synthetic organic
Comment: GSK1016790A is an activator (agonist) of the transient receptor potential cation channel, TRPV4.
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 |
GSK1016790A inhibits TNF-α-induced monocyte adhesion to human endothelial cells. In vivo, GSK1016790A reduces atherosclerotic plaque formation in ApoE deficient mice, indicative of a potential for TRPV4 activation to be used as a therapeutic approach to treat atherosclerosis [3]. |
Selectivity at ion channels | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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