Synonyms: compound 21 [Taniguchi et al., 2019]
Compound class:
Synthetic organic
Comment: DS21360717 is a potent inhibitor of FER tyrosine kinase [1]. It was designed by Daiichi Sankyo to inhibit protumourigenic activity of FER as a novel anticancer therapy. It was discovered through high-throughput screening, scaffold hopping and SAR-based chemical modification.
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 |
DS21360717 exhibits antitumour efficacy in a subcutaneous tumour model in a dose-dependent manner [1]. From a screening panel of 68 kinases, 200 nM DS21360717 inhibited 16 of them by >90%: FER (108), FES (103), ALK (95), FLT3 (105), FMS (96), KIT (96), PYK2 (99), ROS (92), SYK (102), TRKA (96), CDK2/CycA2 (98), CHK2 (97), HGK (93), IRAK4 (103), MLK1 (91), and TSSK1 (94) (% inhibition in parentheses) . |
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