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Synonyms: compound 22a [PMID: 22397330] | PF 543 | sphingosine kinase 1 Inhibitor II
Compound class: Synthetic organic
Comment: PF-543 is a selective inhibitor of sphingosine kinase-1 . It is >100-fold selective for SphK1 over the SphK2 isoform.
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. Schnute ME, McReynolds MD, Carroll J, Chrencik J, Highkin MK, Iyanar K, Jerome G, Rains JW, Saabye M, Scholten JA et al.. (2017)
Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
J. Med. Chem., 60 (6): 2562-2572. [PMID:28231433]
2. Schnute ME, McReynolds MD, Kasten T, Yates M, Jerome G, Rains JW, Hall T, Chrencik J, Kraus M, Cronin CN et al.. (2012)
Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1.
Biochem. J., 444 (1): 79-88. [PMID:22397330]