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. Author manuscript; available in PMC: 2023 Dec 27.

Published in final edited form as: Curr Res Chem Biol. 2023 Nov 7;3:100047. doi: 10.1016/j.crchbi.2023.100047

Table 1.

Binding of I-BET151 and its derivatives to bromodomain proteins measured by SPR. The standard error is reported.

hBRD4

ID	SPR K_D, μM	R_max

I-BET151	0.036 ± 0.022	217 ± 11
AP-08-188	0.29 ± 0.17	135 ± 27
AP-09-187	8.5 ± 4.1	173 ± 20
AP-09-008	6.1 ± 3.6	14.2 ± 1.8
AP-09-191	60 ± 26	200 (locked)

TbBdf2
ID	SPR K_D, μM	R_max

I-BET151	33 ± 25	100 (locked)
AP-08-188	45 ± 31	85 ± 35
AP-09-187
AP-09-008	1.68 ± 0.34	27.1 ± 1.2
AP-09-191	44 ± 31	200 (locked)

TbBdf3
ID	SPR K_D, μM	R_max

I-BET151	37 ± 22	100 (locked)
AP-08-188	30 ± 21	143 ± 51
AP-09-187
AP-09-008	1.43 ± 0.32	36.9 ± 1.9
AP-09-191	56 ± 31	200 (locked)