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- W3034990744 abstract "Doublecortin-like kinase 1 (DCLK1) is a serine/threonine kinase that is overexpressed in gastrointestinal cancers, including esophageal, gastric, colorectal, and pancreatic cancers. DCLK1 is also used as a marker of tuft cells, which regulate type II immunity in the gut. However, the substrates and functions of DCLK1 are understudied. We recently described the first selective DCLK1/2 inhibitor, DCLK1-IN-1, developed to aid the functional characterization of this important kinase. Here we describe the synthesis and structure–activity relationships of 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one DCLK1 inhibitors, resulting in the identification of DCLK1-IN-1." @default.
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- W3034990744 date "2020-06-12" @default.
- W3034990744 modified "2023-10-15" @default.
- W3034990744 title "Synthesis and Structure–Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6<i>H</i>-benzo[<i>e</i>]pyrimido[5,4-<i>b</i>][1,4]diazepin-6-one Scaffold" @default.
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- W3034990744 doi "https://doi.org/10.1021/acs.jmedchem.0c00596" @default.
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