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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Immunopharmacology Comments |
Compound 18e inhibits JAK-mediated cytokine-induced (IL-2, IL-6, GM-CSF) STAT3/5 phosphorylation in human PBMCs: IL-2 induced pSTAT5 via JAK1/3 IC50 112 nM IL-6 induced pSTAT3 via JAK1 IC50 94 nM GM-CSF induced pSTAT5 via JAK2 IC50 10 nM |