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Compound class: Synthetic organic
Comment: Compound 15 is an orally available PI3K inhibitor with selectivity for the PI3Kγ isoform . This is a new isoindolinone chemotype that has not previously been used for the design of PI3K inhibitors.
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.✖
|PI3Kγ is a class I PI3K that is predominantly expressed in leukocytes and which is a long-standing target of drug discovery for inflammatory pathologies that are characterised by a high influx of inflammatory effector cells. Isoform selectivity is essential for successful (safe) drug development because PI3Kα is known to affect glucose and insulin signalling .|