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Compound class: Synthetic organic
Comment: Compound 34 is a potent inhibitor of the protein kinase ERN1 (endoplasmic reticulum to nucleus signaling 1) . ERN1 is also known as IRE1, and is an endoplasmic reticulum stress sensor which signals to the nucleus in response to abnormal levels of unfolded proteins. Compound 34 inhibits the RNAse domain of the protein, like other salicylaldehyde-containing molecules.
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. Ranatunga S, Tang CH, Kang CW, Kriss CL, Kloppenburg BJ, Hu CC, Del Valle JR. (2014)
Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity.
J. Med. Chem., 57 (10): 4289-301. [PMID:24749861]