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Compound class: Synthetic organic
Comment: LYS006 is one of the chemical structures claimed in a Novartis patent as inhibitors of leukotriene A4 hydrolase (LTA4H) . Both the (R) and (S) stereoisomers are claimed (examples 3 and 29 respectively). Both isomers have similar inhibitory potency in vitro. The (3S)-enantiomer was disclosed as LYS006 in 2021 , and at that point we modified our record to reflect this updated information. LYS006 is being developed for immunomodulatory action that can be applied to acute and chronic inflammation and autoinflammatory disorders.
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. Bollbuck B, Merkert C, Miltz W, Roehn T. (2015)
Heteroaryl butanoic acid derivatives as lta4h inhibitors.
Patent number: WO2015092740A1. Assignee: Novartis Ag. Priority date: 20/12/2013. Publication date: 25/06/2015.
2. Markert C, Thoma G, Srinivas H, Bollbuck B, Lüönd RM, Miltz W, Wälchli R, Wolf R, Hinrichs J, Bergsdorf C et al.. (2021)
Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase.
J Med Chem, 64 (4): 1889-1903. [PMID:33592148]