- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: This compound is a cell-permeable, potent, reversible, and ATP-competitive inhibitor of EGFR and ERBB2 .
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. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011)
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]
2. Cockerill S, Stubberfield C, Stables J, Carter M, Guntrip S, Smith K, McKeown S, Shaw R, Topley P, Thomsen L et al.. (2001)
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Bioorg Med Chem Lett, 11 (11): 1401-5. [PMID:11378364]
3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013)
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
Biochem J, 451 (2): 313-28. [PMID:23398362]
4. Huang H, Jia Q, Ma J, Qin G, Chen Y, Xi Y, Lin L, Zhu W, Ding J, Jiang H et al.. (2009)
Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors.
Eur J Med Chem, 44 (5): 1982-8. [PMID:19041163]