Compound class:
Synthetic organic
Comment: Compound 6g was desigend as a dual epidermal growth factor receptor (EGFR) kinase and tubulin polymerization inhibitor [1]. It binds to the colchicine site on tubulin which is expected to translate to antimitotic activity and it should mediate a vascular-disrupting effect via EGFR inhibition.
![]() 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. Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Schiaffino Ortega S, Chayah M, Kimatrai Salvador M, Lopez-Cara LC, Brancale A et al.. (2019)
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors. J Med Chem, 62 (3): 1274-1290. [PMID:30633509] |