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. 2024 Nov 28;146(49):33675–33711. doi: 10.1021/jacs.4c11556

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© 2024 The Authors. Published by American Chemical Society

Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/).

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Live cell ternary complex formation between VHL or CRBN with 26 or 27 and BRD4. NanoBRET kinetic ternary complex formation in endogenous HiBiT-BRD4 HEK293 cells stably expressing LgBiT and transiently expressing (A) HaloTag-VHL or (B) HaloTag-CRBN. Cells were pretreated with 1 μM of proteasome inhibitor MG132, and subsequently treated with 0.01, 0.1, and 1 μM of 26, 27 or DMSO control. Donor and acceptor signal was continuously monitored for 3.5 h after compound addition. N = 1 biological replicate, data is presented as mean values with error bars representing the S.D. of technical triplicates.