- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: WZ4002 is a third generation EGFR inhibitor tool compound which potently inhibits the T790M EGFR mutant and suppresses the growth of cells bearing this mutation [1-2].
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.✖
1. Sakuma Y, Yamazaki Y, Nakamura Y, Yoshihara M, Matsukuma S, Nakayama H, Yokose T, Kameda Y, Koizume S, Miyagi Y. (2012)
WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors.
Lab Invest, 92 (3): 371-83. [PMID:22157722]
2. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R et al.. (2009)
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Nature, 462 (7276): 1070-4. [PMID:20033049]