Compound class:
Synthetic organic
Comment: Compound 5e is a potent FMS-like tyrosine kinase 3 (FLT3, a type III receptor tyrosine kinase) inhibitor that is in preclinical evaluation for the treatment of acute myelogenous leukemia (AML) [3].
![]() 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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Bioactivity Comments |
Compound 5e potently kills MV4-11 and MOLM13 FLT3-driven AML cells [3]. The EC50 for MV4-11 killing is 25nM. 5e is active against wild-type and mutant forms of FLT3, with a Kd of 1.4nM for the common ITD mutation. 5e exhibits some off-target activity: it is ~10-fold selective for FLT3 over PDGFRB and JAK1, and inhibits several other kinases with Kd values <500nM (CLK1, CSF1R, EPHB6, JAK2, PIK4CB, TYK2) [3]. |
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