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. Author manuscript; available in PMC: 2018 Nov 20.
Published in final edited form as: J Med Chem. 2018 Oct 16;61(20):9316–9334. doi: 10.1021/acs.jmedchem.8b01248

Table 1.

ALPHAScreen Analysis of Compounds V, VII, VIII, and IX against 7 of 8 BET Bromodomains

graphic file with name nihms-995406-t0002.jpg R X IC50 by ALPHAScreen (μM)
BRD4 BRD3 BRD2 BRDT
D1 D2 D1 D2 D1 D2 D1
V graphic file with name nihms-995406-t0003.jpg C 1.8 >100 11.2 >100 29 67 5.3
VII graphic file with name nihms-995406-t0004.jpg N 27 75 51 110 43 30 36
VIII graphic file with name nihms-995406-t0005.jpg N 160 102 200 310 >250 260 110
IX graphic file with name nihms-995406-t0006.jpg N 1.3 0.56 0.77 2.4 1.8 12 1.6