. Author manuscript; available in PMC: 2022 Mar 1.

Published in final edited form as: Med Res Rev. 2021 Oct 11;42(2):710–743. doi: 10.1002/med.21859

TABLE 1.

Summary of BET small-molecule inhibitors and dual-target inhibitors

Type	Inhibitors	Crystal structure of BET protein				PDB code of other targets	Clinical phase	NCT identifier^a
Type	Inhibitors	PDB code	Positions	Released date	Resolution (Å)	PDB code of other targets	Clinical phase	NCT identifier^a
BET small-molecule inhibitors	JQ1	3MXF¹⁵	42–168	2010.10.06	1.60	NA	NA	NA
	I-BET762	3P5O²⁶	44–168	2010.11.17	1.60	NA	II	NCT01943851
	I-BET151	3ZYU⁶	44–168	2011.11.02	1.50	NA	NA	NA
	CPI-0610	5HLS²⁷	42–168	2016.02.10	2.18	NA	I	NCT02157636 NCT01949883
	PFI-1	4E96²⁸	44–168	2012.04.18	1.92	NA	NA	NA
	I-BET726	4BJX²⁹	44–168	2013.10.02	1.59	NA	NA	NA
	RVX-208	4MR6³⁰	346–455	2013.11.27	1.67	NA	III	NCT02586155
	ABBV-744	6E6J³¹	348–455	2019.07.31	2.44	NA	I	NCT03360006
BET dual-target inhibitors	Dinaciclib	4O70³²	44–168	2014.03.05	1.55	4KD1³³	III	NCT01580228
	Flavopiridol	4O71³²	44–168	2014.03.05	1.36	3BLR³⁴	II	NCT00023894, NCT00464633, NCT00003256
	BI-2536	4O74³⁵	44–168	2014.02.26	1.73	2RKU³⁶	II	NCT00701766, NCT00376623, NCT00706498, NCT00710710
	TG101348	4OGJ³⁵	44–168	2014.02.26	1.65	NA	II	NCT04282187
	TG101209	4O76³²	44–168	2014-03-05	1.70	4JI9³⁷	NA	NA
	SF2523	5U28³⁸	44–180	2017.02.08	1.80	NA	NA	NA
	SF2558HA	5U2C³⁸	342–460	2017.02.08	3.30	NA	NA	NA
	SB610251B	4O7E³²	44–168	2014.03.05	1.85	NA	NA	NA
	SB202190	4O77³²	44–168	2014.03.05	2.00	NA	NA	NA
	JWG-047	6CIS³⁹	44–166	2018.08.29	1.51	NA	NA	NA
	GW612286X	4O78³²	44–168	2014.03.05	1.34	3CJF⁴⁰	NA	NA
	NU7441	4O72³²	44–168	2014.03.05	1.40	NA	NA	NA
	SB409514	4O7A³²	44–168	2014.03.05	1.34	NA	NA	NA
	TW9	6YQN⁴¹	44–168	2020.05.06	1.05	NA	NA	NA

Abbreviation: NA, not available.