Compound class:
Synthetic organic
Comment: Compound 18 is the most potent of a SAR series of covalent inhibitors of NF-κB-inducing kinase (NIK; MAP3K14) [1]. NIK is a key enzyme in the noncanonical NF-κB pathway. Compound 18 binds irreversibly to Cys444 within the back pocket of the kinase's active site.
![]() 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 |
In a screening panel of 40 kinases, 1 μM compound 18 inhibited MLK1, HER4, SGK1, TAK1, PDGFRA, BTK, RIPK2 Aurora B, VEGFR, and SIK2 by >50%, but the uniqueness of Cys444 in NIK is expected to confer high selectivity for the endogenously expressed kinase [1]. Compound 18 inhibits NIK (MAP3K14) activity in vitro, however its antiproliferative activity in tumour cell lines was fairly weak and was likely to offer limited efficacy against cancer cells in situ. |
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