Synonyms: compound 67 [PMID: 20942471] | GKT 136901 | GKT-136901
Compound class:
Synthetic organic
Comment: GKT136901 was identified as a lead compound in a high-throughput screening and medicinal chemistry campaign that was designed to identify novel NOX4-selective inhibitors [1]. It is an orally active compound that is suitable for investigating the preclinical potential of NOX4 inhibitors for the treatment of fibrotic diseases and cancers in which NOX4 activity has been implicated.
![]() 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 |
GKT136901 is selective for NOX4 and NOX1, compared to NOX2 [1]. It has no hERG liability (0% inhibition at 1 μM), and limited CYP450 enzyme liability (CYP3A4 IC50 >20 μM, and CYP1A, CYP2C19, CYP2C9 and CYP2D6 IC50s all >25 μM). |
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