Synonyms: compound 9 [PMID: 25260492]
Compound class:
Synthetic organic
Comment: LY3023703 is a selective inhibitor of prostaglandin E synthase (mPGES-1), an inducible enzyme that regulates the biosynthesis of proinflammatory PGE2 downstream of the cyclooxygenases (COX 1 and 2) [1]. It was developed as a potential treatment for inflammatory pain. Clinical development of LY3023703 was terminated at phase 1 because a reactive metabolite (generated from its 2-Aminoimidazole functional group) caused drug-induced liver injury [2].
![]() 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 |
mPGES-1 inhibitors are being investigated for anti-inflammatory action that is more targeted towards reduction of PGE2 biosynthesis than COX inhibitors. Despite preclinical efficacy, this compound failed at phase 1 due to liver injury that was induced by a reactive metabolite from its chemical skeleton. |