Compound class:
Synthetic organic
Comment: Compound 2m is reported as a competitive inhibitor of the 5-lipoxygenase (5-LOX) enzyme. It was developed for anti-inflammatory potential [4]. 2m was the most active inhibtor identified from the thiazole series in this pharmacophore modeling study. The thiazole series of compounds was designed with the aim of reducing the hepatotoxicity that is associated with N-hydroxyurea class 5-LOX inhibitors [3] such as zileuton, atreleuton (ABT-761; PubChem CID 3086671) [1] and MLN-977 (PubChem CID 9905233) [2]. 2m is devoid of radical scavenging activity.
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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Immunopharmacology Comments |
Human 5-LOX is a key enzyme that is targeted for asthma and inflammation using inhibitor compounds. The first 5-LOX inhibitor to reach the clinic was zileuton. |