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Synonyms: compound 47 [PMID: 27433829] | EGF-816 | EGF816
Compound class: Synthetic organic
Comment: EGF816 is an irreversible and selective inhibitor of EGFRs harbouring gatekeeper T790M, and sensitising L858R mutations, whilst sparing the wild-type receptor (such compounds are termed third generation EGFR tyrosine kinase inhibitors) . It has been developed to overcome acquired resistance to, and side-effect liabilities of first and second generation EGFR inhibitors in non-small-cell lung cancer (NSCLC). Small-molecule EGFR T790M inhibitors and the development of novel compounds in the discovery pipeline are reviewed by Song et al. (2016) .
EGF816 is claimed in Novartis' patent WO2015085482 , where it is named (R,E)-N-(7-chloro-l-(l-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-lH-benzo[d]imidazol-2-yl)-2-methylisonicotinamide, which resolves to the IUPAC name presented here.
Preclinical characterisation is reported in .
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|
|compound 47 [PMID: 27433829] | EGF-816 | EGF816|
|GtoPdb PubChem SID||315661280|
|Search Google for chemical match using the InChIKey||IOMMMLWIABWRKL-WUTDNEBXSA-N|
|Search Google for chemicals with the same backbone||IOMMMLWIABWRKL|
|Search PubMed clinical trials||nazartinib|
|Search PubMed titles||nazartinib|
|Search PubMed titles/abstracts||nazartinib|
|UniChem Compound Search for chemical match using the InChIKey||IOMMMLWIABWRKL-WUTDNEBXSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||IOMMMLWIABWRKL-WUTDNEBXSA-N|