The Ligandable Human Proteome

Bromodomain-containing protein 4

Index	Ligand Name	Structure	PDB code	Compound Potency nM
1	89d	BRD4_BD2_A-1497627	5uex	1.5
2	88m	BRD4_BD2_A-1412838	5uey	5.1
3	9s3	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 1-(2R,4S)-2-methyl-4-(phenylamino)-6-4-(piperidin-1-ylmethyl)phenyl-1,2,3,4- tetrahydroquinolin-1-yl-ethan-1-one	5acy	6.4
4	5w1	Crystal structure of the first bromodomain of human BRD4 in complex with MA4-022-2	5f62	6.8
5	wsh	Crystal Structure of the Second Bromodomain of Human Brd4 with the inhibitor GW841819X	2yem	15.5
6	0s6	BRD4_BD2_A-1107604	5ueu	16.7
7	73b	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH GSK1324726A (I-BET726)	4bjx	22
8	r78	Crystal structure of the first bromodomain of human BRD4 in complex with BI 2536	4o74	25
9	5w0	Crystal structure of the first bromodomain of human BRD4 in complex with MA4-022-1	5f61	35
10	0s6	Crystal structure of the first bromodomain of human BRD4 in complex with MS417 inhibitor	4f3i	36.1
11	r78	Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor BI-2536	4ogi	37
12	62g	Crystal structure of the first bromodomain of human BRD4 bound to CPI-0610	5hls	39
13	bmf	Crystal structure of the first bromodomain of human BRD4 in complex with bromosporine (BSP)	5igk	41.8
14	5vz	Crystal structure of the first bromodomain of human BRD4 in complex with SG3-014	5f60	43
15	4ld	BRD4 bromodomain 2 in complex with gamma-carboline-containing compound, number 18.	4z93	44.6
16	jq1	Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor JQ1	3mxf	49
17	ies	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH I-BET295	4cl9	50
18	tvu	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 7-(3,4-dimethoxyphenyl)-N-(1,1-dioxo-1-thian-4-yl)-5-methyl-4-oxo-4H,5H-thieno-3,2-c-pyridine-2- carboxamide	4uix	50.1
19	wsh	Crystal Structure of the First Bromodomain of Human Brd4 with the inhibitor GW841819X	2yel	52.5
20	eam	Crystal Structure of the First Bromodomain of Human Brd4 in complex with IBET inhibitor	3p5o	55.2
21	bnm	Brd4 Bromodomain 1 complex with its novel inhibitors	4qr5	60
22	5mj	Crystal Structure of the First Bromodomain of Human BRD4 in Complex With Cyclic Vinylogous Amide Inhibitor MS402	5ula	77
23	5vy	Crystal structure of the first bromodomain of human BRD4 in complex with MA2-014	5f5z	86
24	1gh	Crystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A)	3zyu	100
25	6tb	CRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH DB-1-264-2	5kj0	130
26	1m3	Crystal structure of the first bromodomain of human BRD4 in complex with TG101209	4o76	130
27	nue	Crystal structure of the first bromodomain of human BRD4 in complex with MS267 inhibitor	4nue	150
28	2ta	Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor TG-101348	4ogj	164
29	82y	BRD4 first bromodomain (BD1) in complex with dual PI3 kinase (PI3K) inhibitor SF2558HA	5u2f	193
30	21q	Crystal Structure of BRD4(1) bound to inhibitor XD14	4lyw	237
31	bnk	Brd4 Bromodomain 1 complex with its novel inhibitors	4qr4	250
32	69g	BRD4 in complex with Cpd4 ((E)-3-(6-(but-2-en-1-yl)-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethylbenzamide)	5i88	250
33	837	BRD4 first bromodomain (BD1) in complex with dual PI3 kinase (PI3K) inhibitor SF2535	5u2e	277
34	83t	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH IBET-295	4clb	280
35	2ta	Crystal structure of the first bromodomain of human BRD4 in complex with TG101348	4ps5	290
36	3x0	Discovery of benzotriazolo diazepines as orally-active inhibitors of BET bromodomains: Crystal structure of BRD4 with CPI-13	4x2i	350
37	1h3	Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand	4j0s	382
38	1h2	Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand	4j0r	386
39	62v	Crystal structure of the first bromodomain of human BRD4 bound to benzoisoxazoloazepine 3	5hm0	440
40	9bm	The first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand	4bw3	500
41	56m	First bromodomain of BRD4 bound to inhibitor XD27	5d25	500
42	3p2	Crystal Structure of the first bromodomain of human BRD4 in complex with a novel inhibitor UMB32 (N-TERT-BUTYL-2-[4-(3,5-DIMETHYL-1,2-OXAZOL-4-YL) PHENYL]IMIDAZO[1,2-A]PYRAZIN-3-AMINE)	4wiv	550
43	08k	Crystal Structure of the first bromodomain of human BRD4 in complex with a benzo-triazepine ligand (BzT-7)	3u5l	640
44	9gy	Benzopiperazine BET bromodomain inhibitor in complex with BD1 of Brd4	5vom	790
45	l28	First bromodomain of BRD4 bound to inhibitor XD28	5d26	810
46	7uu	Complex structure of the first bromodomain of BRD4 with an inhibitor that containing a 2H-chromen-2-one ring	5wuu	810
47	57f	First bromodomain of BRD4 bound to inhibitor XD35	5d3l	880
48	89g	BRD4_BD2_A-1342843	5uez	970
49	1k0	Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-OH)	4mr3	1142
50	1k0	Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-208)	4mr4	1142
51	s5b	The first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand	4bw1	1260
52	np8	NN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-5-methoxypyridin-3-yl-3- methyl-8-piperidin-4-ylamino-1,2-dihydro-1,7-naphthyridin-2-one	5a5s	1260
53	579	First bromodomain of BRD4 bound to inhibitor XD44	5d3s	1300
54	bnj	Brd4 Bromodomain 1 complex with its novel inhibitors	4qr3	1400
55	5nq	FIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR 3-Butyl-8-(6-butyl-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-ylsulfanylmethyl)-7-ethyl-3,7-dihydropurine-2,6-dione	5egu	1400
56	5gd	X-ray crystal structure of human BRD4(BD1) in complex with RVX297 to 1.12 A resolution	5dw2	1440
57	1k0	X-ray crystal structure of bromodomain complex to 1.24 A resolution	4j3i	1800
58	5d1	FIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR 4-[(1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)oxy]-N-({1-[(3-methylphe methyl]piperidin-4-yl}methyl)butanamide	5dlz	1800
59	5ou	FIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR 3-(4-Chlorobenzyl)-7-ethyl-3,7-dihydropurine-2,6-dione	5eis	1800
60	14x	Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolin ligand	4hbx	1900
61	5d2	FIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR N-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-1-{3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl}piperidine-4-carboxamide	5dlx	2000
62	7e7	Crystal structure of BRD4 BROMODOMAIN 1 IN COMPLEX WITH LIGAND 2	5m3a	2000
63	1a9	Brd4 Bromodomain 1 complex with 3-CYCLOHEXYL-N-{3-(2-OXO-2,3-DIHYDRO-1,3-THIAZOL-4-YL)-5-[(THIOPHEN-2-YLSULFONYL)AMINO]PHENYL}PROPANAMIDE inhibitor	4hxl	2200
64	e0b	Crystal Structure of the first bromodomain of human BRD4 in complex with benzo[cd]indol-2(1H)-one ligand	5d0c	2340
65	08h	Crystal Structure of the first bromodomain of human BRD4 in complex with Alprazolam	3u5j	2460
66	2re	Crystal structure of the first bromodomain of human BRD4 in complex with SB 202190	4o77	2500
67	5v2	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(1,1-dioxo-1-thian-4-yl)- 5-methyl-4-oxo-7-3-(trifluoromethyl)phenyl-4H,5H-thieno-3,2-c- pyridine-2-carboximidamide	4uiy	2510
68	30m	Crystal structure of the first bromodomain of human BRD4 in complex with Olinone	4qb3	3400
69	13f	Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolin ligand	4hby	4400
70	sav	Crystal structure of the first bromodomain of human BRD4 in complex with GW612286X	4o78	4600
71	14z	Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazoline ligand	4hbw	4800
72	78j	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 8-(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-ylamino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one	5a85	5010
73	l33	First bromodomain of BRD4 bound to inhibitor XD33	5d3j	5700
74	l26	First bromodomain of BRD4 bound to inhibitor XD26	5d24	5800
75	uth	The first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand	4bw2	6310
76	rmr	Trimethoxy-ring inhibitor in complex with the first bromodomain of BRD4	5h21	6400
77	2n0	Crystal Structure of the first bromodomain of human BRD4 in complex with compound B13	4pce	7000
78	57e	First bromodomain of BRD4 bound to inhibitor XD41	5d3p	7400
79	57g	First bromodomain of BRD4 bound to inhibitor XD29	5d3h	7900
80	77x	Structure of the first bromodomain of BRD4 with a pyrazolo[4,3-c]pyridin fragment	5luu	8630
81	l40	First bromodomain of BRD4 bound to inhibitor XD40	5d3n	9200
82	6xw	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-(5-aminopyridin-3-yl)-8-(((3R,4R)-3-((1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methoxy)piperidin-4-yl)amino)-3-methyl-1,7-naphthyridin-2(1H)-one	5lj2	1e+004
83	2rk	Crystal structure of the first bromodomain of human BRD4 in complex with SB-614067-R	4o7c	1e+004
84	56y	First bromodomain of BRD4 bound to inhibitor XD47	5d3t	1.2e+004
85	2rq	Crystal structure of the first bromodomain of human BRD4 in complex with SB-251527	4o7f	1.3e+004
86	6xh	BRD4 bromodomain in complex with Cpd59 ((S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)ethanone)	5ku3	1.3e+004
87	cpb	Crystal structure of the first bromodomain of human BRD4 in complex with FLAVOPIRIDOL	4o71	1.8e+004
88	2rf	Crystal structure of the first bromodomain of human BRD4 in complex with SB-409514	4o7a	1.9e+004
89	1qk	Crystal structure of the first bromodomain of human BRD4 in complex with DINACICLIB	4o70	1.9e+004
90	n1d	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 7-(3,4-dimethoxyphenyl)-2-(4-methanesulfonylpiperazine-1-carbonyl)-5-methyl-4H,5H-thieno-3,2-c- pyridin-4-one	4uiz	1.995e+004
91	2rj	Crystal structure of the first bromodomain of human BRD4 in complex with SB-284847-BT	4o7b	2e+004
92	loc	Crystal Structure of BRD4(1) bound to Colchicine	4lzr	2e+004
93	y80	Crystal structure of human BRD4(1) in complex with 4-[(2E)-3-(4-methoxyphenyl)-2-phenylprop-2-enoyl]-3,4-dihydroquinoxalin-2(1H)-one (compound 19a)	4yh3	2.6e+004
94	y81	Crystal structure of human BRD4(1) in complex with 4-[(5-phenylpyridin-3-yl)carbonyl]-3,4-dihydroquinoxalin-2(1H)-one (compound 19d)	4yh4	2.6e+004
95	5nv	First domain of human bromodomain BRD4 in complex with inhibitor 8-(5-Amino-1H-[1,2,4]triazol-3-ylsulfanylmethyl)-3-(4-chlorobenzyl)-7-ethyl-3,7-dihydropurine-2,6-dione	5ei4	2.64e+004
96	6xx	N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 8-(((3R,4R,5S)-3-((4,4-difluorocyclohexyl)methoxy)-5-methoxypiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one	5lj1	3.16e+004
97	2sj	Crystal Structure of BRD4(1) bound to Colchiceine	4lys	4.6e+004
98	h4c	Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains	4c66	7.94e+004
99	25k	Crystal Structure of the first bromodomain of human BRD4 in complex with a 5-methyl-triazolopyrimidine ligand	4men	1.25e+005
100	89j	BRD4_BD2-A-35165	5uf0	1.6e+005