1196156-84-9Relevant articles and documents
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5
Nguyen, Duy,Lemos, Clara,Wortmann, Lars,Eis, Knut,Holton, Simon J.,Boemer, Ulf,Moosmayer, Dieter,Eberspaecher, Uwe,Weiske, Joerg,Lechner, Christian,Prechtl, Stefan,Suelzle, Detlev,Siegel, Franziska,Prinz, Florian,Lesche, Ralf,Nicke, Barbara,Nowak-Reppel, Katrin,Himmel, Herbert,Mumberg, Dominik,Von Nussbaum, Franz,Nising, Carl F.,Bauser, Marcus,Haegebarth, Andrea
, p. 928 - 940 (2019)
The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. Herein, we report the identification of a highly potent and selective ERK5 inhibitor BAY-885 by high-throughput screening and subsequent structure-based optimization. ERK5 is a key integrator of cellular signal transduction, and it has been shown to play a role in various cellular processes such as proliferation, differentiation, apoptosis, and cell survival. We could demonstrate that inhibition of ERK5 kinase and transcriptional activity with a small molecule did not translate into antiproliferative activity in different relevant cell models, which is in contrast to the results obtained by RNAi technology.
IDENTIFICATION AND USE OF ERK5 INHIBITORS
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Page/Page column 105-106, (2019/10/01)
The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 and R3 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer disorders, as a sole agent or in combination with other active ingredients.