Compound class:
Synthetic organic
Comment: Compound 20f [PMID: 28520415] is reported as a selective inhibitor of PI3Kδ that was specifically designed as an inhalation drug with potential immunomodulatory effects, and which could be effective as a treatment of airway inflammation [1]. It has limited oral bioavailability and systemic exposure, but is retained in lung tissue in vivo following intratracheal delivery.
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 20f inhibits PI3Kδ with an IC50 of ~1.3 nM in a cellular assay [1]. It is selective for PI3Kδ over PI3K&dbeta;, PI3Kα and PI3Kγ. In vitro IC50s for the latter two isoforms are 630 nM and 200 nM respectively. Compound 20f shows no inhibitory activity >50% against a screening panel of 345 kinases. It exhibits no hERG liability (<20% inhibition at 11 μM). |
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