Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assays and IC50 Measurements

ZZ Zijun Zhou
XL Xiaoming Li
ZL Zhiqing Liu
LH Lixun Huang
YY Yuying Yao
LL Liuyou Li
JC Jian Chen
RZ Rongxin Zhang
JZ Jia Zhou
LW Lijing Wang
QZ Qian-Qian Zhang
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The binding affinities and IC50 values of the tested BET family member inhibitors for the BRD4 and BRD2 proteins bromodomains (BDs) were detected using a commercially available TR-FRET assay kits (Cayman Chemical, Ann Arbor, MI, USA) according to the manufacturer’s instructions and our recent publications (Borysko et al., 2018; Liu et al., 2018; Liu et al., 2020). The specificity of the designed and synthesized compounds for BRD4 was also evaluated through comparison with those for BRD2.

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