Synonyms: inhibitor A1 [PMID: 28604669]
Compound class:
Synthetic organic
Comment: GSK180 is a potent and selective competitive inhibitor of kynurenine 3-monooxygenase (KMO) [1], an enzyme involved in tryptophan metabolism. The structure is a derivative of the enzyme substrate kynurenine.
Currently the only X-ray crystal structure available is for GSK180 in complex with the Pseudomonas fluorescens KMO homologue (PDB ID 5FN0). 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 biochemical assays GSK180 shows negligible activity against other enzymes in the tryptophan pathway, or against a panel of >50 unrelated proteins. In vivo, GSK180 provides therapeutic protection against multiple organ dysfunction syndrome (MODS) in a rat model of acute pancreatitis [1]. |
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