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Synonyms: LY-2228820 | LY-2228820 free base | LY2228820
Compound class: Synthetic organic
Comment: Ralimetinib was developed as a potent and selective, ATP-competitive inhibitor of p38 MAPK α and β (MAPK14 and MAPK11 respectively) [3,6]. The compound is delivered orally as the dimesylate salt (PubChem CID 11570805). It is compound 40 in Mader et al. (2008) .
In 2023, a report in Cell Chemical Biology demonstrated that the anticancer activity of ralimetinib is in fact due to inhibition of EGFR function, despite the compound being >30-fold less potent against EGFR than it is against p38α . This study found that sensitivity of tumour cells to ralimetinib was retained when p38α and p38β genes were knocked-out, and that the EGFRT790M (gatekeeper) mutation conferred resistance to both ralimetinib and the approved EGFR inhibitor gefitinib. The cocrystal structure of ralimetinib bound to the EGFR confirmed the EGFR hypothesis.
SARS-CoV-2: p38 MAPK activity has been reported to be upregulated following SARS-CoV-2 infection of host cells in vitro. Ralimetinib produces an antiviral effect with an IC50 of 873 nM .
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.✖
|Compound class||Synthetic organic|
|International Nonproprietary Names|
|LY-2228820 | LY-2228820 free base | LY2228820|
|CAS Registry No.||862505-00-8|
|GtoPdb PubChem SID||249565642|
|RCSB PDB Ligand||YXT|
|Search Google for chemical match using the InChIKey||XPPBBJCBDOEXDN-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||XPPBBJCBDOEXDN|
|Search PubMed clinical trials||ralimetinib|
|Search PubMed titles||ralimetinib|
|Search PubMed titles/abstracts||ralimetinib|
|UniChem Compound Search for chemical match using the InChIKey||XPPBBJCBDOEXDN-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||XPPBBJCBDOEXDN-UHFFFAOYSA-N|