- Advanced search
- Immuno Portal
- Malaria Portal
Compound class: Synthetic organic
Comment: AZ2 is a highly selective inhibitor of the lipid kinase PI3Kγ . It represents a novel chemotype that binds to a conserved part of the ATP-binding pocket (Type I inhibitor-like), but once bound the inhibitor induces a DFG-out (active state) conformational change and rearrangement of the activation loop (analogous to Type II protein kinase inhibitors). This mechanism occurs only in PI3Kγ. Analogues of this novel class of PI3Kγ inhibitors, with enhanced pharmacokinetic properties and in vivo potency (e.g. AZD3458), have been reported .
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.✖
1. Gangadhara G, Dahl G, Bohnacker T, Rae R, Gunnarsson J, Blaho S, Öster L, Lindmark H, Karabelas K, Pemberton N et al.. (2019)
A class of highly selective inhibitors bind to an active state of PI3Kγ.
Nat Chem Biol, 15 (4): 348-357. [PMID:30718815]
2. Pemberton N, Mogemark M, Arlbrandt S, Bold P, Cox RJ, Gardelli C, Holden NS, Karabelas K, Karlsson J, Lever S et al.. (2018)
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.
J Med Chem, 61 (12): 5435-5441. [PMID:29852070]