Showing 1,441 - 1,460 results of 227,229 for search '(( 50 ((we decrease) OR (mean decrease)) ) OR ( 10 ((ng decrease) OR (a decrease)) ))', query time: 1.55s Refine Results
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    GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) by F. Anthony Romero (2452198)

    Published 2017
    “…Structure–activity relationship studies coupled with further structure-based design targeting the LPF shelf, BC loop, and KAc regions allowed us to significantly increase potency and selectivity, resulting in the identification of non-CNS penetrant <b>19</b> (GNE-781, TR-FRET IC<sub>50</sub> = 0.94 nM, BRET IC<sub>50</sub> = 6.2 nM; BRD4(1) IC<sub>50</sub> = 5100 nΜ) that maintained good in vivo PK properties in multiple species. …”
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