- Guide to PHARMACOLOGY
Synonyms: TG 100-115 | TG 100115 | TG100-115
Compound class: Synthetic organic
Comment: TG-100-115 is an isozyme-selective inhibitor of phosphatidylinositol-3-kinase (PI3K). The discovery and synthesis of this compound is described in , where it is compound 6. It has subsequently been reported to inhibit the kinase activity of the TRPM7 ion channel, an action that suppresses breast cancer cell migration and invasion .
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. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011)
Comprehensive analysis of kinase inhibitor selectivity.
Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]
2. Palanki MS, Dneprovskaia E, Doukas J, Fine RM, Hood J, Kang X, Lohse D, Martin M, Noronha G, Soll RM et al.. (2007)
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.
J Med Chem, 50 (18): 4279-94. [PMID:17685602]
3. Song C, Bae Y, Jun J, Lee H, Kim ND, Lee KB, Hur W, Park JY, Sim T. (2017)
Identification of TG100-115 as a new and potent TRPM7 kinase inhibitor, which suppresses breast cancer cell migration and invasion.
Biochim Biophys Acta Gen Subj, 1861 (4): 947-957. [PMID:28161478]
4. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010)
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Chem Biol, 17 (11): 1241-9. [PMID:21095574]