ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K d s of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1) , BRD2(2) , BRD3(1) , BRD3(2) , BRD4(1) , and BRD4(2) , respectively. (Pink: BET ligand ( HY-78695 ); Blue: VHL ligand ( HY-112078 ); Black: linker).
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