Synonyms: IC87114
Compound class:
Synthetic organic
Comment: IC-87114 is a selective inhibitor of PI3Kδ [1-2].
Given that PI3Kδ is preferentially expressed in cells of hemopoietic lineage and is involved in neutrophil chemotaxis we have tagged this ligand as having immunopharmacology relevance. Using this chemical tool in in vitro chemotaxis experiments reveals that PI3Kδ activity is required for the directional component of chemotaxis, but is not required for random movement [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 |
IC-87114 is 58-fold more selective for PI3Kδ compared to PI3Kγ, and >100-fold selective over PI3Kα and PI3Kβ [2]. With respect to protein kinases, 100 μM IC-87114 did not significantly inhibit p38 MAPK, CHK1, DNA-PK, or cSrc. |
Selectivity at enzymes | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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