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HTS for Identification of Inhibitors against the ERK Signaling Pathway using a Homogenous Cell-based Assay.

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Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 May 18 [updated 2010 Sep 2].

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The ERK phosphorylation signaling pathway plays a significant role in regulation of cellular functions. The anomalous activation of the ERK pathway in cancer has been shown to promote cell proliferation, differentiation, development and survival. The probe ML102 (CID-2303746) has been identified in a cell-based ERK phosphorylation assay as an inhibitor of the ERK phosphorylation signaling pathway. In addition, the probe has satisfied the project goals of a novel chemotype that is a highly potent and cell-membrane permeable selective inhibitor of EGFR kinase.

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