Synonyms: PP242 | TORKinib
Compound class:
Synthetic organic
Comment: PP-242 is a selective mTOR inhibitor, which inhibits both mTOR containing protein complexes, mTORC1 and mTORC2. The discovery of PP-242 is described in [1], where it is compound 13.
PubChem entry CID 57347681 represents an alternative tautomer of this compound. ![]() 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 |
Although PP-242 is a mTOR inhibitor, its cellular effects differ from those of sirolimus (aka rapamycin), offering a new pharmacological tool to investigate the role of mTOR in normal physiology and pathophysiology. In a screen for activity of PP-242 against a panel of kinases, >70% inhibition was measured for only five other kinases using 1μM compound [1]. These five are RET, PRKCA, JAK2, PRKCB2 and PASK (in decreasing level of inhibition). |
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