Compound class:
Synthetic organic
Comment: Compound 18e is an optimised, orally bioavailable dual Janus kinase 2 (JAK2)/fms related tyrosine kinase 3 (FLT3) inhibitor [1]. It exhibits anti-tumour activity in vitro and in vivo.
![]() 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 18e has 37-fold and 56-fold selectivity for JAK2 over JAK1 and JAK3, respectively in biochemical assay. Selectivity for JAK2 is higher in cellular assays [1]. It inhibits proliferation of Ba/F3-JAK2V617F cells and JAK2V617F-overexpressing SET-2 cells with IC50s of 145 and 270 nM, respectively. It retains inhibitory activity for the FLT3D835Y mutation (IC50 4 nM). In vivo, compound 18e inhibits tumour growth in the MV4-11 and SET-2 xenograft tumour models. |
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Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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