Synonyms: compound 10 [PMID: 31895563] [1]
Compound class:
Synthetic organic
Comment: Compound 10 is an inhibitor of sphingosine kinase 2 [1]. This compound exploits a novel side cavity on the kinase to provide enhanced potency and selectivity. The PubChem entry for this compound originated via SureChEMBL patent extraction, and is derived from patent WO2017172989A1 from researchers at Virginia Tech [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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Immunopharmacology Comments |
Blockade of SphK2 activity in vivo causes an elevation of blood S1P levels. S1P signalling and synthesis (via sphingosine kinases) are actively pursued therapeutic modalities, with potential applications across a broad range of cellular processes, including modulating fibrosis, inhibiting tumour growth, angiogenesis, and endothelial cell chemotaxis, and for treating inflammatory and autoimmune diseases and disorders. Compound 10 provides a pharmacological tool to help explore the outcomes of selective SphK2 inhibition in normal and pathological settings, that is suitable for both in vitro and in vivo studies. |