- Guide to PHARMACOLOGY
Synonyms: CX 4945 | CX-4945 | CX4945
Compound class: Synthetic organic
Comment: Silmitasertib (CX-4945) is a a potent and selective inhibitor of CK2 (casein kinase 2) [4-5]. CX-4945 is described in the same article as CX-5011 and CX-5279 .
Silmitasertib, via inhibition of CK2, was found to produce an in vitro antiviral effect (IC50 = 2.34 μM;) . In conjunction with data supporting a physical interaction  and co-localization of CK2 with SARS-CoV-2 N protein, and evidence of potential role of CK2 in remodeling extracellular matrix upon infection , it can be hypothesised that the CK2 pathway is hijacked by SARS-CoV-2. Thus, it makes pharmacological sense that silmitasertib should be considered for investigation as an anti-SARS-CoV-2 therapeutic.
Ligand Activity Visualisation Charts
These 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.✖
|CX-4945 induces apoptosis in cancer cells and inhibits molecular mechanisms underlying angoigenesis in HUVEC cells . Low nanomolar IC50s are reported (in ascending value) for several other kinases including death-associated protein kinase 3 (DAPK3), fms-related tyrosine kinase 3 (FLT3), TANK-binding kinase 1 (TBK1), CDC-like kinase 3 (CLK3), homeodomain interacting protein kinase 3 (HIPK3), Pim-1 proto-oncogene (PIM1) and cyclin dependent kinase 1 (CDK1/cyclinB) .|
|Selectivity at enzymes|
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