Synonyms: Example 59 [WO2018121550]
Compound class:
Synthetic organic
Comment: Compound 5d is a potent, 4-methylquinazoline-based pan-PI3K inhibitor [1]. It is one of the examples claimed in patent WO2018121550A1 from the Institute of Pharmaceutical Research, Chinese Academy of Medical Sciences [2].
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 |
Compound 5d blocks phosphorylation of the main effectors downstream of PI3K [1]. It potently inhibits proliferation of mouse MLg2908 lung fibroblasts (IC50 5 nM). Compound 5d was found to inhibit only PI3Ks in panel of 97 kinases. |
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