Compound class:
Synthetic organic
Comment: Compound 52 is reported as a potent and selective PI3Kδ inhibitor [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 52 is active in cellular assays measuring inhibition of T cell activation and IFNγ production [2] In a kinase profile screen, off-targets with IC50s in the nanomolar range (IC50 in parentheses) are PI3Kγ (41 nM), MINK1 (66 nM), PI3Kα (370 nM), MLCK (510 nM) and CLK4 (700 nM). |
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