Synonyms: AZD 9668 | AZD-9668 | AZD9668 | KB-105160
Compound class:
Synthetic organic
Comment: AZD9668 is a potent, selective and reversible inhibitor of human neutrophil elastase. It was developed as having the potential to be effective for neutrophil-driven inflammatory lung diseases, such as bronchiectasis and COPD [2]. Since the phase II studies did not show clear efficacy for COPD this compound is now listed in the AstraZeneca Open Innovation Clinical Compound Bank for repurposing proposals.
There is ambiguity on PubChem in the assigned nomenclature and stuctures for this compound, as CID 71587812 has been incorrectly assigned alvelestat as a synonym. 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 |
In contrast with ONO6818, an inhibitor that binds covalently to NE, AZD9668 exhibited a more rapid association and dissociation rate, and its interaction with NE was fully reversible. It also generally showed greater specificity than ONO6818 or sivelestat for NE over other neutrophil-derived serine proteases, particularly Pr-3 and pancreatic elastase [2]. Approximately 90 analogues are listed in a patent [1] where this is example 94, but only limited SAR data is included. |
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