Advancements in the Development of non-BET Bromodomain ...
TP-238 is a CECR2 binder (KD = 10 nM), also active on BPTF and BRD9 with KD = 120nM and 1.1 ?M, respectively, (Ycas et al., 2020). GSK4027 binds to the. PCAF ...
Reevaluation of bromodomain ligands targeting BAZ2ATP-238 was reported as a CECR2/BPTF chemical probe by Takeda and the Structural Genomics Consortium (SGC), with 12-fold higher selectivity for CECR2 (Kd = 10 nM) ... The Optimisation of Potent ATAD2 and CECR2 Bromodomain ...The ATAD2 and CECR2 bromodomains are exciting targets for drug discovery and, consequently, inhibitors for both bromodomains are starting to appear in the ... design-of-class-i-iv-bromodomain-targeting-degraders-for-chromatin ...TP-238 is a high affinity inhibitor of CECR2 so we selected compounds 8 and 9 as potential degraders of. CECR2 over molecules 4 and 5. Encouragingly, we ...
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