Compound class:
Synthetic organic
Comment: C34 is a fourth generation EGFR inhibitor that is designed to overcome EGFRC797S mutation-mediated resistance to third-generation irreversible inhibitors such as osimertinib [1]. The C797S mutation negates the ability of the acrylamide warhead of osimertinib to form its covalent bond with Cys797 and this leads to severely diminished therapeutic efficacy.
![]() 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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References |
1. Zhu Y, Ye X, Shen H, Li J, Cai Z, Min W, Hou W, Dong H, Wu Y, Wang L et al.. (2023)
Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.3c01165 |