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Synonyms: BCX-7353 | BCX7353 | Orladeyo®
berotralstat is an approved drug (FDA (2020), EMA (2021))
Compound class: Synthetic organic
Comment: Berotralstat (BCX7353) is an orally bioavailable inhibitor of plasma kallikrein, a proteinase that is encoded by the KLKB1 gene in humans . Plasma kallikrein cleaves Lys-Arg and Arg-Ser bonds in (human) kininogen to release bradykinin. Inhibition of this activity is exploited to reduce bradykinin levels in human disease where abnormally elevated bradykinin induces pathologic vascular permeability and swelling, as seen in patients with hereditary angioedema (HAE; caused by loss of C1 inhibitor SERPING1 expression).
The 'flat' structure of berotralstat with no specified stereochemistry is claimed as compound 52h in Biocryst Pharmaceuticals' patent WO2015134998A1 .
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.✖
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