Synonyms: compound 1 [PMID: 32584034] | X165
Compound class:
Synthetic organic
Comment: X-165 is a potent, selective, and bioavailable small molecule inhibitor of the LPA synthetic phosphodiesterase, autotaxin [1]. Autotaxin inhibitors are investigated for their anti-fibrotic potential, and X-165 was developed for potential to treat idiopathic pulmonary fibrosis (IPF). Analysis of autotaxin/X-165 complex crystals revealed that this compound binds to a site on the enzyme that is distinct from the binding site of exisiting inhibitors. Its binding pose shares some similarity with that of ziritaxestat (GLPG1690), but retains crucial differences.
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 |
X-165 inhibitsthe production of LPA in human and mouse plasma at nanomolar levels and has demonstrated efficacy in a mouse model of human lung fibrosis [1]. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
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