633328-96-8Relevant articles and documents
Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors
Gr?dler, Ulrich,Busch, Michael,Leuthner, Birgitta,Raba, Michael,Burgdorf, Lars,Lehmann, Martin,Linde, Nina,Esdar, Christina
supporting information, (2020/09/18)
Triazolo[4,5-d]pyrimidin-5-amines were identified from kinase selectivity screening as novel ERK3 inhibitors with sub-100 nanomolar potencies in a biochemical assay using MK5 as substrate and with an attractive kinase selectivity profile. ERK3 crystal structures clarified the inhibitor binding mode in the ATP pocket with impact on A-loop, GC-loop and αC-helix conformations suggesting a potential structural link towards MK5 interaction via the FHIEDE motif. The inhibitors also showed sub-100 nM potencies in a cellular ERK3 NanoBRET assay and with excellent correlation to the biochemical IC50s. This novel series provides valuable tool compounds to further investigate the biological function and activation mechanism of ERK3.
SPIROINDOLINONES AS DDR1 INHIBITORS
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Page/Page column 123, (2017/09/07)
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 262-263, (2012/08/27)
Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.