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Compound class: Synthetic organic
Comment: Compound 4d is reported as an irreversible, non-peptide inhibitor of kallikrein proteins . This compound appears to be patent protected by US-9006466-B2 .
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.✖
|No information available.
|Mechanism Of Action and Pharmacodynamic Effects
|Kallikrein inhibitors are being investigated as novel therapeutics for certain skin diseases such as Netherton syndrome, an autosomal recessive disorder caused by deficiency of the endogenous serine protease inhibitor lympho-epithelial Kazal-type-related inhibitor (LEKTI- protein product of the SPINK5 gene) . Deficiency of such endogenous inhibitors results in unopposed serine protease activity which can have a pathological outcome. Hence the development of serine protease inhibitors with clinical utility.