Search alternatives:
ng decrease » nn decrease (Expand Search), _ decrease (Expand Search), gy decreased (Expand Search)
we decrease » _ decrease (Expand Search), nn decrease (Expand Search), teer decrease (Expand Search)
a decrease » _ decrease (Expand Search), _ decreased (Expand Search), _ decreases (Expand Search)
ng decrease » nn decrease (Expand Search), _ decrease (Expand Search), gy decreased (Expand Search)
we decrease » _ decrease (Expand Search), nn decrease (Expand Search), teer decrease (Expand Search)
a decrease » _ decrease (Expand Search), _ decreased (Expand Search), _ decreases (Expand Search)
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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)
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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