Synonyms: AC-5216 | XBD-173 | XBD173
Compound class:
Synthetic organic
Comment: Emapunil (XBD173) is an orally bioavailable translocator protein (TSPO) phenylpurine ligand. TSPO was originally identified as a molecular target for the development of new anxiolytic drugs [1-2,5]. More recently, TSPO is being pursued as a novel neuroimmunodulatory target for disease-modifying benefit in secondary progressive MS (SPMS), based on preclinical evidence of immunomodulatory effects on monocytes/macrophages and microglia that appear to induce a reparative phenotype in these immune cell types [3-4].
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 human brain samples the TSPO binding affinity of emapunil (XBD173) varies depending on the expression profile of binding sites [3]. Some individuals express a protein with either a high or low affinity binding site, and others express both so the detected overall binding affinity lies between the high and low values. |
Selectivity at other protein targets | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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