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Compound class: Synthetic organic
Comment: Compound 15 is a small molecule, ADP analogue-based CD73 (ecto-5'-nucleotidase) inhibitor . Mechanisms to inhibit CD73 activity are being exploited for immuno-oncology potential, and are exemplified by the progress of the anti-CD73 monoclonal oleclumab and the small molecule inhibitor AB680 into clinical trials as treatments for advanced solid tumours.
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.✖
|CD73 hydrolyzes AMP to adenosine, and thus regulates the extracellular concentration of adenosine. It is expressed by lymphocytes, endothelial, and epithelial cells, and expression is upregulated under hypoxic or inflammatory conditions, and in various cancers. Elevated CD73 in tumours leads to increased levels of adenosine which impairs antitumour immunity and promotes tumour growth and metastasis. Mechanisms to inhibit CD73 activity are being exploited for immuno-oncology potential, and are exemplified by the progress of the anti-CD73 monoclonal oleclumab and the small molecule inhibitor AB680 into clinical trials as treatments for solid tumours.|