- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Compound 6 is reported as a selective inhibitor of the calcium-activated non-selective cation channel TRPM4 . To date (August 2018) this is the first report of a selective sub‐micromolar TRPM4 inhibitor. It will facilitate experiments to better understand the role of TRPM4 function in human diseases, and help provide clues for clinical lead development.
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.✖
1. Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J et al.. (2018)
Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Br J Pharmacol, 175 (12): 2504-2519. [PMID:29579323]
2. Stokłosa P, Borgström A, Hauert B, Baur R, Peinelt C. (2021)
Investigation of Novel Small Molecular TRPM4 Inhibitors in Colorectal Cancer Cells.
Cancers (Basel), 13 (21). [PMID:34771564]