Compound class:
Synthetic organic
Comment: Compound 2 is representative analog developed in a medicinal chemistry study to optimise inhibition of LCK proto-oncogene, Src family tyrosine kinase (Lck) [1].
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 |
This compound shows no selectivity against other Src-family kinases or Janus kinase 3 (JAK3), presumably because all of these kinases share a high level of homology in their ATP binding domains [1]. In contrast, compound 2 does not inhibit any of receptor tyrosine or serine/threonine kinases tested [1]. Note that we have mapped the IC50 values reported in [1] to human enzymes, although source species for the tested kinases is not specified in the article. Further Src-family kinase inhibitors are reported in [2]. |
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