NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an effect on IKKbeta, led to a optimization process that identified the aminopyrazole as a low μM selective NIK inhibitor. Compound effectively inhibited the NIK-dependent activation of the NF-κB pathway in tumour cells, confirming its selective inhibitory profile.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6071728 | PMC |
| http://dx.doi.org/10.1039/c8md00068a | DOI Listing |
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